Maximum percent of inhibition of binding was determined
|
None
|
100.0
%
|
|
Maximum percent of inhibition of binding was determined
|
None
|
100.0
%
|
|
Compound was evaluated for ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 1
|
None
|
4.9e-06
nM
|
|
Compound was evaluated for ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 1
|
None
|
0.022
nM
|
|
Ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 2
|
None
|
0.01
nM
|
|
Ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 2
|
None
|
10.0
nM
|
|
Ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 3.
|
None
|
430.0
nM
|
|
Ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 3.
|
None
|
5.2
nM
|
|
Inhibition of [3H]epibatidine binding at the alpha beta nicotinic AChR in male rat cerebral cortex
|
Rattus norvegicus
|
1.5
nM
|
|
Binding affinity at CCR was determined by displacement of [3H]cytisine from rat brain
|
Rattus norvegicus
|
1.1
nM
|
|
Binding affinity at CCR was determined by displacement of [3H]nicotine from rat brain
|
Rattus norvegicus
|
1.4
nM
|
|
Equilibrium dissociation constant (Kd) was determined
|
Mus musculus
|
1.41
nM
|
|
Binding affinity towards Nicotinic acetylcholine receptor by the displacement of [3H]-nicotine from rat cortical membranes
|
None
|
2.4
nM
|
|
The compound was tested for the inhibition of binding of [3H]epibatidine to central nicotinic acetylcholine receptor (nAChR) in rat brain.
|
None
|
5.0
nM
|
|
Binding affinity at NAChRs was determined by measuring the displacement of ([3H]Nic) from a preparation of rat cortical membranes.
|
Rattus norvegicus
|
4.0
nM
|
|
In vitro displacement of [3H]methylcarbamylcholine from nicotinic acetylcholine receptor in rat brain cortex
|
None
|
6.6
nM
|
|
Inhibition of (-)-[3H]nicotine binding to rat brain membranes
|
Rattus norvegicus
|
7.0
nM
|
|
Inhibition of [3H]MCC binding to rat brain membranes
|
Rattus norvegicus
|
3.0
nM
|
|
Inhibitory concentration required for in vitro binding affinity to cholinergic central Nicotinic acetylcholine receptor on rat brain cortex by using [3H]MCC
|
Rattus norvegicus
|
4.0
nM
|
|
Binding affinity against Nicotinic Acetylcholine Receptor was determined by measuring the displacement of [3H]cytisine from a preparation of whole rat brain.
|
Rattus norvegicus
|
1.0
nM
|
|
Binding affinity for Nicotinic acetylcholine receptor site in rat cortex was determined using [3H]MCC as radioligand
|
None
|
8.4
nM
|
|
Binding affinity towards nicotinic acetylcholine receptor (nACh) using [3H](-)-nicotine as radioligand in rat brain
|
Rattus norvegicus
|
2.4
nM
|
|
Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand
|
Rattus norvegicus
|
13.0
nM
|
|
Binding affinity towards nicotinic acetylcholine receptor using [3H]nicotine as radioligand in rat brain homogenates
|
None
|
1.3
nM
|
|
Ability to displace [3H](-)-cytisine from nicotinic acetylcholine receptor (nAChR) in a whole rat brain preparation
|
None
|
1.15
nM
|
|
Inhibition of [3H]MCC binding to torpedo electroplax membranes
|
Torpedo
|
1.0
nM
|
|
inhibition of (-)-[3H]nicotine binding to torpedo electroplax membranes
|
Torpedo
|
4.0
nM
|
|
Binding affinity against nicotinic acetylcholine receptor using [3H]epibatidine as radioligand in rat brain tissue
|
None
|
27.0
nM
|
|
Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta2
|
None
|
12.0
nM
|
|
In vitro ability to displace tritiated nicotine from rat brain binding sites, and calcium flux (c.f)
|
Rattus norvegicus
|
4.0
nM
|
|
Binding affinity towards nicotinic acetylcholine receptor alpha2-beta2 using [3H]epibatidine
|
Rattus norvegicus
|
12.0
nM
|
|
Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand
|
Rattus norvegicus
|
15.0
nM
|
|
Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta4
|
None
|
112.0
nM
|
|
Binding affinity towards Nicotinic acetylcholine receptor alpha2-beta4 using [3H]epibatidine
|
Rattus norvegicus
|
112.0
nM
|
|
Binding affinity against nicotinic acetylcholine receptor alpha2-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells
|
None
|
103.0
nM
|
|
In vitro Binding affinity towards alpha-3 (PC12) nAChR was determined
|
None
|
220.0
nM
|
|
Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta2
|
None
|
47.0
nM
|
|
Inhibitory concentration required for in vitro binding affinity to Nicotinic acetylcholine receptor alpha3-beta2 expressed on cell line sf 9 by using [3H]-MCC
|
Rattus norvegicus
|
3.8
nM
|
|
Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta2 using [3H]epibatidine
|
Rattus norvegicus
|
47.0
nM
|
|
Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand
|
Rattus norvegicus
|
43.0
nM
|
|
Binding affinity to Nicotinic acetylcholine receptor alpha3-beta4 using +/-[3H]epibatidine as radioligand in pig adrenal gland
|
Sus scrofa
|
73.0
nM
|
|
Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta4
|
None
|
443.0
nM
|
|
Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta4 using [3H]epibatidine
|
Rattus norvegicus
|
443.0
nM
|
|
Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand
|
Rattus norvegicus
|
530.0
nM
|
|
Binding affinity against nicotinic acetylcholine receptor alpha3-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells
|
None
|
320.0
nM
|
|
Potency to displace [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 immuno-isolated from M10 cells
|
Gallus gallus
|
2.0
nM
|
|
Inhibitory concentration required for in vitro binding affinity to Nicotinic acetylcholine receptor alpha4-beta2 expressed on cell line sf 21 by using [3H]-MCC
|
None
|
4.2
nM
|
|
Affinity at alpha4-beta2 nACh receptors in rat brain (minus cerebellum) homogenates.
|
None
|
1.3
nM
|
|
Affinity for Nicotinic acetylcholine receptor alpha4-beta2 tested by analogue-induced inhibition of [3H]NIC binding to rat striatal membranes
|
None
|
1.0
nM
|
|
Compound was evaluated for functional potencies and efficacies at ratNicotinic acetylcholine receptor alpha4-beta2
|
None
|
590.0
nM
|
|
Displacement of [3H]cytisine from Nicotinic acetylcholine receptor alpha4-beta2 in rat forebrain
|
Rattus norvegicus
|
0.94
nM
|
|
Binding affinity in rat forebrain against Nicotinic acetylcholine receptor alpha4-beta2
|
None
|
2.3
nM
|
|
Binding potency for Nicotinic acetylcholine receptor alpha4-beta2 (rat brain)
|
None
|
1.05
nM
|
|
Inhibition of binding of [3H]nicotine to Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortical membranes
|
None
|
1.0
nM
|
|
Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta2
|
None
|
10.0
nM
|
|
The compound was evaluated for percentage inhibition of binding of [3H]- nicotine to Nicotinic acetylcholine receptor alpha4-beta2 in Rat Cerebral Cortical Membranes
|
None
|
1.0
nM
|
|
Binding affinity for nicotinic acetylcholine receptor alpha4-beta2 was evaluated by its ability to inhibit [3H]NIC binding to rat brain membranes
|
Rattus norvegicus
|
1.4
nM
|
|
Inhibition of [3H]epibatidine binding at the nicotinic acetylcholine receptor alpha4-beta2 in male rat cerebral cortex
|
Rattus norvegicus
|
1.5
nM
|
|
Non-specific binding in presence of 300 uM nicotine at nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortex membranes
|
Rattus norvegicus
|
1.01
nM
|
|
In vitro binding affinity by inhibiting [3H]dopamine release in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2
|
Rattus norvegicus
|
7.3
nM
|
|
Binding affinity to Nicotinic acetylcholine receptor alpha4-beta2 using +/-[3H]epibatidine as radioligand in rat brain
|
Rattus norvegicus
|
0.84
nM
|
|
Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 using [3H]epibatidine
|
Rattus norvegicus
|
10.0
nM
|
|
Binding affinity towards nicotinic acetylcholine receptor alpha4-beta2 from rat brain homogenates
|
None
|
2.1
nM
|
|
Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand
|
Rattus norvegicus
|
12.0
nM
|
|
In vitro binding affinity by inhibiting [3H]cytisine binding in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2
|
Rattus norvegicus
|
8.0
nM
|
|
In vitro binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 using [3H]cytisine in rat brain
|
Rattus norvegicus
|
1.0
nM
|
|
Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes
|
Rattus norvegicus
|
1.0
nM
|
|
Affinity for nicotinic acetylcholine receptor alpha4-beta2
|
None
|
1.2
nM
|
|
Binding affinity at heteropentameric Nicotinic acetylcholine receptor alpha4-beta2 subtype using [3H]bungarotoxin as radioligand
|
None
|
4.0
nM
|
|
Binding affinity against nicotinic acetylcholine receptor alpha4-beta2 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells
|
None
|
9.1
nM
|
|
Binding affinity towards nicotinic acetylcholine receptor alpha4-beta2
|
None
|
2.0
nM
|
|
In vitro Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 was determined
|
None
|
2.3
nM
|
|
Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta4
|
None
|
40.0
nM
|
|
Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta4 using [3H]epibatidine
|
Rattus norvegicus
|
40.0
nM
|
|
Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand
|
Rattus norvegicus
|
46.0
nM
|
|
Binding affinity against nicotinic acetylcholine receptor alpha4-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells
|
None
|
129.0
nM
|
|
In vitro Binding affinity towards alpha-7 nAChR was determined
|
None
|
480.0
nM
|
|
Affinity for alpha-7 neuronal nicotinic acetylcholine receptor subtype determined by inhibition of [3H]-MLA binding to rat brain membranes
|
None
|
770.0
nM
|
|
Binding affinity in rat hippocampi against Nicotinic acetylcholine receptor alpha7
|
None
|
480.0
nM
|
|
Binding affinity nicotinic acetylcholine receptor alpha-7 was evaluated by its ability to inhibit [3H]methyllycaconitine ([3H]-MLA) binding to rat brain membranes
|
None
|
450.0
nM
|
|
Binding affinity to subtype Nicotinic acetylcholine receptor alpha-7 using [125I]-alpha-BTX as radioligand in rat brain
|
None
|
130.0
nM
|
|
Binding affinity at homopentameric Nicotinic acetylcholine receptor alpha-7 subtype using [3H]S-(-)-nicotine as radioligand
|
None
|
620.0
nM
|
|
The compound was evaluated for its binding affinity towards nicotinic acetylcholinergic (n ACh) receptor using [3H]nicotine as the radioligand in rat brain
|
Rattus norvegicus
|
2.1
nM
|
|
Compound was tested for its binding affinity against nicotinic receptor in synaptic membrane fractions from rat cerebral cortices.
|
Rattus norvegicus
|
16.0
nM
|
|
Binding affinity against Nicotinic acetylcholine receptor using [3H](-)-nicotine radioligand
|
None
|
1.2
nM
|
|
Compound was evaluated for functional potencies and efficacies at rat nAChR subtype DA release
|
Rattus norvegicus
|
40.0
nM
|
|
Inhibition of [3H](-)-nicotine binding to recombinant rat alpha4-beta2 nAChR.
|
None
|
3.8
nM
|
|
Binding affinity towards alpha4-beta2 measured by using the inhibition of [3H]NIC binding to rat striatal membrane
|
None
|
1.0
nM
|
|
Binding affinity towards alpha-7 neuronal nicotinic acetylcholine receptor (nAChRs) measured by using the inhibition of [3H]-MLA binding to whole brain membrane
|
None
|
340.0
nM
|
|
Binding affinity values obtained by measuring the displacement of radioligand [3H](-)-cytisine from a preparation of whole rat brain
|
Rattus norvegicus
|
1.0
nM
|
|
In vitro binding affinity to neuronal nAChRs was determined by measuring the displacement of [3H]cytisine in rat brain
|
None
|
1.1
nM
|
|
Tested for neuronal nicotinic acetylcholine receptor (nAChR) binding in a whole rat brain preparation using [3H]cystine as the radioligand.
|
Rattus norvegicus
|
1.0
nM
|
|
Tested for the binding affinity against neuronal nicotinic acetylcholine receptors from whole rat brain
|
None
|
1.15
nM
|
|
Binding affinity towards rat alpha2-beta4 nACh receptor expressed in HEK293 cells using [3H]EB as radioligand
|
Rattus norvegicus
|
130.0
nM
|
|
Dissociation constant for nicotinic acetylcholine receptor alpha4-beta2 of mouse M10 cells; n=3
|
Mus musculus
|
3.08
nM
|
|
Dissociation constant for nicotinic acetylcholine receptor alpha 7 from human neuroblastoma SH-SY5Y cells; n=3
|
Homo sapiens
|
1.06
nM
|
|
Inhibition of [3H]-MLA binding to alpha-7 nicotinic acetylcholine receptor of rat brain membrane
|
Rattus norvegicus
|
770.0
nM
|
|
Inhibition of [3H]MLA binding to alpha4-beta2 nicotinic acetylcholine receptor of rat brain membrane
|
Rattus norvegicus
|
1.0
nM
|
|
Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta4
|
None
|
40.0
nM
|
|
Inhibition of [3H]nicotine binding to nicotinic acetylcholine receptor alpha4-beta2 of rat cortex
|
Rattus norvegicus
|
0.95
nM
|
|
Inhibition of alpha beta[3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cerebral cortex
|
Rattus norvegicus
|
1.5
nM
|
|
Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha2-beta2
|
None
|
12.0
nM
|
|
Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha2-beta4
|
None
|
112.0
nM
|
|
Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha3-beta2
|
None
|
47.0
nM
|
|
Inhibition of [3H]epibatidine binding to nicotinic acetylcholine receptor alpha3-beta4 of human IMR32 cells
|
Homo sapiens
|
530.0
nM
|
|
Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha3-beta4
|
Rattus norvegicus
|
443.0
nM
|
|
Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha4-beta2
|
Rattus norvegicus
|
10.0
nM
|
|
Binding affinity against nicotinic acetylcholine receptor alpha4-beta2 in human HEK293 cells using [3H]- nicotine as radioligand
|
Homo sapiens
|
1.6
nM
|
|
Inhibition of [3H]-nicotine binding to nicotinic acetylcholine receptor alpha4-beta2 in rat cortex
|
Rattus norvegicus
|
0.95
nM
|
|
Binding affinity for nicotinic acetylcholine receptor alpha4-beta2 from mouse M10 cells; n=3
|
Mus musculus
|
2.5
nM
|
|
Inhibition of [3H]epibatidine binding to nicotinic acetylcholine receptor alpha3-beta4 of IMR32 cells
|
Homo sapiens
|
530.0
nM
|
|
Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortex
|
Rattus norvegicus
|
1.5
nM
|
|
Inhibition of [125 I]-alpha Bungarotoxin binding to alpha 7 nicotinic acetylcholine receptor of rat cortex membranes
|
Rattus norvegicus
|
460.0
nM
|
|
Inhibition of [3H](-)-nicotine binding to rat brain (minus cerebellum) Nicotinic acetylcholine receptor alpha4-beta2
|
Rattus norvegicus
|
35.0
nM
|
|
Inhibition of [3H]epibatidine binding to alpha 4 beta 2 nicotinic acetylcholine receptor of rat cortex membranes
|
Rattus norvegicus
|
2.0
nM
|
|
In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta2 using 0.5 nM [3H]epibatidine
|
Rattus norvegicus
|
12.0
nM
|
|
In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta4 using 0.5 nM [3H]epibatidine
|
Rattus norvegicus
|
110.0
nM
|
|
In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 using 0.5 nM [3H]epibatidine
|
Rattus norvegicus
|
47.0
nM
|
|
In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 using 0.5 nM [3H]epibatidine
|
Rattus norvegicus
|
440.0
nM
|
|
In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 using 0.5 nM [3H]epibatidine
|
Rattus norvegicus
|
10.0
nM
|
|
In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 using 0.5 nM [3H]epibatidine
|
Rattus norvegicus
|
40.0
nM
|
|
Binding affinity for human Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK 293 cells using [3H]nicotine
|
Homo sapiens
|
1.6
nM
|
|
Binding affinity to human Nicotinic acetylcholine receptor alpha3-beta4 expressed in IMR32 cells using [3H]epibatidine
|
Homo sapiens
|
530.0
nM
|
|
Binding affinity for rat brain Nicotinic acetylcholine receptor alpha4-beta2 using [3H]S-(-)-nicotine
|
Rattus norvegicus
|
1.8
nM
|
|
Binding affinity to human Nicotinic acetylcholine receptor alpha7 expressed in IMR32 cells using [3H]alpha-bungarotoxin
|
Homo sapiens
|
630.0
nM
|
|
Analgesic activity in mice at 10 mg/kg, sc by acetic acid writhing test
|
Mus musculus
|
100.0
%
|
|
Analgesic activity in mice at 5 mg/kg, sc by acetic acid writhing test
|
Mus musculus
|
88.0
%
|
|
Displacement of [3H]epibatidine from alpha-4-beta-2 nACHR in rat cerebral cortex
|
Rattus norvegicus
|
1.5
nM
|
|
Displacement of [125I]iodo-MLA from alpha-7 nAChR in rat cerebral cortex
|
Rattus norvegicus
|
750.0
nM
|
|
Displacement of [3H]alpha-Bungarotoxin from alpha-7 nAChR in rat brain cortex membranes
|
Rattus norvegicus
|
234.0
nM
|
|
Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat brain cortex membrane
|
Rattus norvegicus
|
4.0
nM
|
|
Displacement of [3H]cytisine from alpha-4-beta-2 in rat cerebral cortical membrane
|
Rattus norvegicus
|
0.9333
nM
|
|
Displacement of [3H]cytisine from alpha-4-beta-2 in rat cerebral cortical membrane
|
Rattus norvegicus
|
0.94
nM
|
|
Agonist activity at rat striatal tissue assessed as dopamine release
|
Rattus norvegicus
|
199.53
nM
|
|
Agonist activity at rat striatal tissue assessed as dopamine release
|
Rattus norvegicus
|
200.0
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha-4-beta-2 nAChR in HEK293 cell line
|
Rattus norvegicus
|
6.2
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha-4-beta-2 nAChR in HEK293 cell line
|
Rattus norvegicus
|
6.31
nM
|
|
Displacement of [3H]epibatidine from recombinant rat alpha-3-beta-4 nAChr in HEK293 cell line
|
Rattus norvegicus
|
220.0
nM
|
|
Displacement of [3H]epibatidine from recombinant rat alpha-3-beta-4 nAChr in HEK293 cell line
|
Rattus norvegicus
|
199.53
nM
|
|
Displacement of [3H]epibatidine from recombinant rat alpha-4-beta-4 nAChr in HEK293 cell line
|
Rattus norvegicus
|
33.0
nM
|
|
Displacement of [3H]epibatidine from recombinant rat alpha-4-beta-4 nAChr in HEK293 cell line
|
Rattus norvegicus
|
31.62
nM
|
|
Displacement of [3H]cytisine from alpha-4-beta-2 nAChR in rat cerebral cortex
|
Rattus norvegicus
|
6.8
nM
|
|
Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat cerebral cortex
|
Rattus norvegicus
|
3.0
nM
|
|
Displacement of [3H]alpha-bungarotoxin from alpha-7 nAChR in rat cerebral cortex
|
Rattus norvegicus
|
450.0
nM
|
|
Displacement of [3H]cytisine from neuronal nicotinic acetylcholine receptor in rat brain membrane
|
Rattus norvegicus
|
1.0
nM
|
|
Displacement of [3H]cytisine from neuronal nicotinic acetylcholine receptor in rat brain membrane
|
Rattus norvegicus
|
0.9333
nM
|
|
Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR
|
Homo sapiens
|
1.5
nM
|
|
Displacement of [3H]cytisine from alpha-4-beta-2 nAChR in rat brain membrane
|
Rattus norvegicus
|
7.0
nM
|
|
Displacement of [3H]ACE from Aplysia AChBP expressed in HEK293S cells by scintillation proximity assay
|
Aplysia
|
415.0
nM
|
|
Displacement of [3H]EPI from Aplysia AChBP expressed in HEK293S cells by scintillation proximity assay
|
Aplysia
|
260.0
nM
|
|
Displacement of [3H]cystisine from nicotinic alpha-4-beta-2 receptor in rat brain
|
Rattus norvegicus
|
4.0
nM
|
|
Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat cerebral cortex
|
Rattus norvegicus
|
1.5
nM
|
|
Displacement of [125I]iodoMLA from alpha-7 nAChR in rat cerebral cortex
|
Rattus norvegicus
|
670.0
nM
|
|
Displacement of [3H]NMCI from nicotinic acetylcholine receptor
|
None
|
0.9
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha4beta2 nAChR expressed in HEK293 cells
|
Rattus norvegicus
|
22.0
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha4beta2 nAChR expressed in HEK293 cells
|
Rattus norvegicus
|
19.95
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha-3-beta-4 nAChR expressed in HEK293 cells
|
Rattus norvegicus
|
600.0
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha-3-beta-4 nAChR expressed in HEK293 cells
|
Rattus norvegicus
|
630.96
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha-4-beta-4 nAChR expressed in HEK293 cells
|
Rattus norvegicus
|
150.0
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha-4-beta-4 nAChR expressed in HEK293 cells
|
Rattus norvegicus
|
158.49
nM
|
|
Displacement of [3H]epibatidine from alpha-4-beta-2 nAchR in rat brain cortex membrane
|
Rattus norvegicus
|
4.0
nM
|
|
Displacement of [125I]alpha-Bungarotoxin from alpha-7 nAchR in rat brain cortex membrane
|
Rattus norvegicus
|
234.0
nM
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
-3.7
%
|
|
Displacement of [3H]cytisine from alpha4beta2 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane
|
Rattus norvegicus
|
0.94
nM
|
|
Displacement of [3H]A585539 from alpha7 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane
|
Rattus norvegicus
|
176.0
nM
|
|
Displacement of [125I]alpha-bungarotoxin from Lymnaea stagnalis His-tagged AchBP
|
Lymnaea stagnalis
|
63.1
nM
|
|
Displacement of [3H]epibatidine from Aplysia californica AchBP
|
Aplysia californica
|
398.11
nM
|
|
Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane
|
Rattus norvegicus
|
0.94
nM
|
|
Displacement of [3H]epibatidine from rat alpha2beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
|
Rattus norvegicus
|
12.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha2beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
|
Rattus norvegicus
|
110.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
|
Rattus norvegicus
|
47.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
|
Rattus norvegicus
|
440.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
|
Rattus norvegicus
|
10.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
|
Rattus norvegicus
|
40.0
nM
|
|
Displacement of L-[3H]Nicotine from alpha4beta2 nAChR in rat brain homogenate by rapid filtration method
|
Rattus norvegicus
|
1.65
nM
|
|
Displacement of [3H]MLA from alpha7 nAChR in rat brain homogenate by liquid scintillation spectrophotometry
|
Rattus norvegicus
|
330.0
nM
|
|
Displacement of [3H]nicotine from alpha4beta2 nAChR in rat brain homogenate by liquid scintillation spectrophotometry
|
Rattus norvegicus
|
1.4
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cerebral cortex after 4 hrs by scintillation counting
|
Rattus norvegicus
|
1.5
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2 nicotinic receptor expressed in human HEK293 cells
|
None
|
9.46
nM
|
|
Displacement of [3H]epibatidine from alpha3beta4 nicotinic receptor expressed in human HEK293 cells
|
None
|
394.0
nM
|
|
Displacement of [3H]epibatidine from alpha6/4beta4 nicotinic receptor expressed in human HEK293 cells
|
None
|
168.0
nM
|
|
Agonist activity at human nAChR alpha4beta2 in human SH-EP1 cells assessed as induction in rubidium efflux
|
Homo sapiens
|
300.0
nM
|
|
Displacement of [3H]epibatidine from rat nAChR alpha2beta2
|
Rattus norvegicus
|
5.5
nM
|
|
Displacement of [3H]epibatidine from rat nAChR alpha2beta4
|
Rattus norvegicus
|
70.0
nM
|
|
Displacement of [3H]epibatidine from rat nAChR alpha3beta2
|
Rattus norvegicus
|
29.0
nM
|
|
Displacement of [3H]epibatidine from rat nAChR alpha4beta2
|
Rattus norvegicus
|
4.9
nM
|
|
Displacement of [3H]epibatidine from rat forebrain nAChR alpha4beta2
|
Rattus norvegicus
|
9.8
nM
|
|
Displacement of [3H]epibatidine from rat nAChR alpha4beta4
|
Rattus norvegicus
|
23.0
nM
|
|
Displacement of [3H]epibatidine from rat nAChR alpha3beta4
|
Rattus norvegicus
|
260.0
nM
|
|
Inactivation of nAChR alpha4beta2 in human SH-EP1 cells
|
Homo sapiens
|
430.0
nM
|
|
Binding affinity to Lymnaea stagnalis His6-AChBP expressed in Bac-to-Bac baculovirus expression system by surface plasmon resonance biosensor assay
|
Lymnaea stagnalis
|
478.63
nM
|
|
Displacement of [3H]epibatidine from Lymnaea stagnalis His6-AChBP expressed in Bac-to-Bac baculovirus expression system
|
Lymnaea stagnalis
|
331.13
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK292 cells after 3 hrs
|
Rattus norvegicus
|
481.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK292 cells after 3 hrs
|
Rattus norvegicus
|
11.1
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cortical membranes by beta counting
|
Rattus norvegicus
|
2.0
nM
|
|
Displacement of [125I]-alpha-Bungarotoxin from alpha7 nAChR rat cortical membranes by gamma counting
|
Rattus norvegicus
|
469.0
nM
|
|
Inhibition of rat neuronal-type nicotinic acetylcholine receptor
|
Rattus norvegicus
|
10.0
nM
|
|
Displacement of [3H]-cytisine from nAChR in rat brain membranes
|
Rattus norvegicus
|
4.7
nM
|
|
Displacement of [3H]-epibatidine from histidine-tagged Lymnaea stagnalis AChBP expressed in Sf9 cells after 1.5 hrs by liquid scintillation counting
|
Lymnaea stagnalis
|
316.23
nM
|
|
Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as increase of carbamylcholine-induced 86Rb+ ion efflux by liquid scintillation counting
|
Homo sapiens
|
290.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta4 nAChR receptor
|
Rattus norvegicus
|
23.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta2 nAChR receptor
|
Rattus norvegicus
|
4.9
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta4 nAChR receptor
|
Rattus norvegicus
|
260.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha2beta4 receptor
|
Rattus norvegicus
|
70.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta2 receptor
|
Rattus norvegicus
|
29.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha2beta2 receptor
|
Rattus norvegicus
|
5.5
nM
|
|
Antagonist activity at human alpha4beta2 nAChR expressed in SH-EP1 cells assessed as inhibition of carbamylcholine-induced 86Rb+ ion efflux by liquid scintillation counting
|
Homo sapiens
|
430.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta2 receptor expressed in HEK cells
|
Rattus norvegicus
|
4.9
nM
|
|
DRUGMATRIX: Nicotinic Acetylcholine radioligand binding (ligand: [125I] Epibatidine)
|
None
|
12.0
nM
|
|
DRUGMATRIX: Nicotinic Acetylcholine radioligand binding (ligand: [125I] Epibatidine)
|
None
|
4.123
nM
|
|
Partial agonist activity at Nicotinic acetylcholine alpha4beta2 receptor in rat striatum assessed as [3H]dopamine release by beta counting
|
Rattus norvegicus
|
67.0
nM
|
|
Partial agonist activity at Nicotinic acetylcholine alpha4beta2 receptor in rat striatum assessed as [3H]dopamine release by beta counting
|
Rattus norvegicus
|
67.61
nM
|
|
Displacement of [3H]epibatidine from Lymnaea stagnalis acetylcholine binding protein expressed using baculoviral system after 1.5 hrs by scintillation counting
|
Lymnaea stagnalis
|
316.23
nM
|
|
Displacement of [3H]epibatidine from human nAChR alpha4beta2 receptor expressed in human HEK293T cells by scintillation counting
|
Homo sapiens
|
12.59
nM
|
|
Displacement of [3H] epibatidine from rat alpha2beta2 nAChR by beta scintillation counting
|
Rattus norvegicus
|
5.5
nM
|
|
Displacement of [3H] epibatidine from rat alpha2beta4 nAChR by beta scintillation counting
|
Rattus norvegicus
|
70.0
nM
|
|
Displacement of [3H] epibatidine from rat alpha3beta2 nAChR by beta scintillation counting
|
Rattus norvegicus
|
29.0
nM
|
|
Displacement of [3H] epibatidine from rat alpha3beta4 nAChR by beta scintillation counting
|
Rattus norvegicus
|
260.0
nM
|
|
Displacement of [3H] epibatidine from rat alpha4beta2 nAChR by beta scintillation counting
|
Rattus norvegicus
|
4.9
nM
|
|
Displacement of [3H] epibatidine from rat alpha4beta2* nAChR in rat forebrain by beta scintillation counting
|
Rattus norvegicus
|
9.8
nM
|
|
Displacement of [3H] epibatidine from rat alpha4beta4 nAChR by beta scintillation counting
|
Rattus norvegicus
|
23.0
nM
|
|
Agonist activity at human alpha4beta2 nAChR expressed in SH-EP1 cells assessed as 86Rb+ ion efflux after 9.5 mins by flip-plate technique
|
Homo sapiens
|
290.0
nM
|
|
Antagonist activity at human alpha4beta2 nAChR expressed in SH-EP1 cells assessed as inhibition of carbamylcholine induced 86Rb+ ion efflux preincubated for 10 mins prior to carbamylcholine-induction measured after 5 mins by flip-plate technique
|
Homo sapiens
|
430.0
nM
|
|
Displacement of [3H]MLA from alpha7* nAChR in Sprague-Dawley rat brain P2 membrane after 120 mins by liquid scintillation counting
|
Rattus norvegicus
|
129.0
nM
|
|
Displacement of [3H]epibatidine from alpha3beta4* nAChR in calf adrenal P1 membrane after 90 mins by liquid scintillation counting
|
Bos taurus
|
75.3
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2* nAChR in Sprague-Dawley rat brain P2 membrane after 90 mins by liquid scintillation counting
|
Rattus norvegicus
|
0.85
nM
|
|
Agonist activity at alpha4beta 2 nAChR
|
Homo sapiens
|
1.0
nM
|
|
Inhibition of electric eel AChE at 2 mg/ml by Ellman's method
|
Electrophorus electricus
|
15.6
%
|
|
Inhibition of horse BChE at 2 mg/ml by Ellman's method
|
Equus caballus
|
1.2
%
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting
|
Homo sapiens
|
6.9
%
|
|
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
11.0
%
|
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
-16.5
%
|
|
Displacement of [3H]epibatidine from rat alpha2beta2 nACHR
|
Rattus norvegicus
|
5.5
nM
|
|
Displacement of [3H]epibatidine from rat alpha2beta4 nACHR
|
Rattus norvegicus
|
70.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta2 nACHR
|
Rattus norvegicus
|
29.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta4 nACHR
|
Rattus norvegicus
|
260.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta2 nACHR
|
Rattus norvegicus
|
4.9
nM
|
|
Displacement of [3H]epibatidine from rat forebrain alpha4beta2* nACHR
|
Rattus norvegicus
|
9.8
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta4 nACHR
|
Rattus norvegicus
|
23.0
nM
|
|
Agonist activity at human alpha4beta2 nACHR expressed in SH-EP1 cells by 86Rb+ efflux assay
|
Homo sapiens
|
290.0
nM
|
|
Inhibition of human alpha4beta2 nACHR expressed in SH-EP1 cells by 86Rb+ efflux assay
|
Homo sapiens
|
430.0
nM
|
|
Displacement of [3H]epibatidine from alpha3beta4 nAChR in human SH-SY5Y cells after 2 hrs by liquid scintillation counting
|
Homo sapiens
|
400.0
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2 nAChR in Sprague-Dawley rat cortex after 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
2.0
nM
|
|
Displacement of [3H]nicotine from alpha4beta2 nAChR in human SH-EP1 cells after 2 hrs by liquid scintillation assay
|
Homo sapiens
|
2.0
nM
|
|
Displacement of [125I]-epibatidine from alpha3beta4 nAChR in mouse cortical membranes
|
Mus musculus
|
167.0
nM
|
|
Displacement of [125I]-epibatidine from alpha4beta2 nAChR in mouse cortical membranes
|
Mus musculus
|
3.5
nM
|
|
Displacement of [125I]-alpha-Btx from alpha7 nAChR in mouse hippocampal membranes
|
Mus musculus
|
244.0
nM
|
|
Displacement of [3H]epibatidine from Lymnaea stagnalis AChBP
|
Lymnaea stagnalis
|
496.0
nM
|
|
Displacement of [3H]epibatidine from Aplysia californica AChBP
|
Aplysia californica
|
598.0
nM
|
|
Displacement of [3H]nicotine human alpha4beta2 nAChR in SH-EP1 cell membranes
|
Homo sapiens
|
2.0
nM
|
|
Antagonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting
|
Homo sapiens
|
426.58
nM
|
|
Antagonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting
|
Homo sapiens
|
427.0
nM
|
|
Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as stimulation of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting
|
Homo sapiens
|
295.12
nM
|
|
Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells assessed as stimulation of 86Rb+ efflux preincubated for 10 mins by liquid scintillation counting
|
Homo sapiens
|
295.0
nM
|
|
Displacement of [3H]Epibatidine from alpha4beta2 nAChR in rat brain by PDSP assay
|
Rattus norvegicus
|
9.8
nM
|
|
Binding affinity to alpha4beta4 nAChR by PDSP assay
|
None
|
23.0
nM
|
|
Binding affinity to alpha4beta2 nAChR by PDSP assay
|
None
|
4.9
nM
|
|
Binding affinity to alpha3beta4 nAChR by PDSP assay
|
None
|
260.0
nM
|
|
Binding affinity to alpha3beta2 nAChR by PDSP assay
|
None
|
29.0
nM
|
|
Binding affinity to alpha2beta4 nAChR by PDSP assay
|
None
|
70.0
nM
|
|
Binding affinity to alpha2beta2 nAChR by PDSP assay
|
None
|
5.5
nM
|
|
Displacement of [3H]epibatidine from alpha4beta4 nAChR after 4 hrs by liquid scintillation counting analysis
|
None
|
23.0
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2* nAChR in rat forebrain after 4 hrs by liquid scintillation counting analysis
|
Rattus norvegicus
|
9.8
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2 nAChR after 4 hrs by liquid scintillation counting analysis
|
None
|
4.9
nM
|
|
Displacement of [3H]epibatidine from alpha3beta4 nAChR after 4 hrs by liquid scintillation counting analysis
|
None
|
260.0
nM
|
|
Displacement of [3H]epibatidine from alpha3beta2 nAChR after 4 hrs by liquid scintillation counting analysis
|
None
|
29.0
nM
|
|
Displacement of [3H]epibatidine from alpha2beta4 nAChR after 4 hrs by liquid scintillation counting analysis
|
None
|
70.0
nM
|
|
Displacement of [3H]epibatidine from alpha2beta2 nAChR after 4 hrs by liquid scintillation counting analysis
|
None
|
5.5
nM
|
|
Displacement of [3H]cytisine from alpha4beta2 nAChR in Sprague-Dawley rat brain homogenate after 75 mins by scintillation counting
|
Rattus norvegicus
|
2.83
nM
|
|
Binding affinity to freshwater snail Lymnaea stagnalis AChBP assessed as [3H]EPI binding by radioligand binding assay
|
Lymnaea stagnalis
|
100.0
nM
|
|
Binding affinity to salt water mollusc Aplysia californica AChBP Y55W mutant assessed as [3H]acetamiprid binding by radioligand binding assay
|
Aplysia californica
|
30.0
nM
|
|
Binding affinity to recombinant Gallus gallus (chicken) alpha4beta2 nicotinic acetylcholine receptor assessed as [3H]NIC binding by radioligand binding assay
|
Gallus gallus
|
1.9
nM
|
|
Inhibition of alpha4beta2 nicotinic acetylcholine receptor (unknown origin)
|
Homo sapiens
|
1.05
nM
|
|
Inhibition of [3H]nicotine binding to alpha4 nicotinic acetylcholine receptor in Mus musculus (mouse) M10 cells co-expressing beta2 nicotinic acetylcholine receptor subunits
|
Mus musculus
|
7.0
nM
|
|
Inhibition of [3H]nicotine binding to alpha3 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells co-expressing beta2beta4alpha5 Nicotinic acetylcholine receptor subunits
|
Homo sapiens
|
45.0
nM
|
|
Displacement of [3H]IMD from nAChR in Myzus persicae 4106A (green peach aphid) membrane after 70 min
|
Myzus persicae
|
800.0
nM
|
|
Displacement of [3H]-methyl-SFX from nAChR in Myzus persicae 4106A (green peach aphid) membrane after 70 min
|
Myzus persicae
|
146.0
nM
|
|
Displacement of [3H]nicotine from nAChR in Sprague-Dawley Rattus norvegicus (rat) whole brain homogenates
|
Rattus norvegicus
|
9.6
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha4beta4 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis
|
Rattus norvegicus
|
141.25
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha4beta4 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis
|
Rattus norvegicus
|
140.0
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha3beta4 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis
|
Rattus norvegicus
|
251.19
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha3beta4 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis
|
Rattus norvegicus
|
250.0
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha4beta2 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis
|
Rattus norvegicus
|
7.586
nM
|
|
Displacement of [3H]epibatidine from rat recombinant alpha4beta2 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis
|
Rattus norvegicus
|
7.6
nM
|
|
Displacement of [3H]epibatidine from Lymnaea stagnalis AChBP linked to ion channel portion of 5-HT3A receptor expressed in HEK293 cells after 4 hrs by scintillation counting analysis
|
Lymnaea stagnalis
|
83.18
nM
|
|
Displacement of [3H]epibatidine from Lymnaea stagnalis AChBP linked to ion channel portion of 5-HT3A receptor expressed in HEK293 cells after 4 hrs by scintillation counting analysis
|
Lymnaea stagnalis
|
83.0
nM
|
|
Desensitization of human alpha4beta2 nACHR expressed in HEK293 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins measured after 2 hrs by liquid scintillation counting analysis
|
Homo sapiens
|
370.0
nM
|
|
Displacement of [3H]-Epibatidine from rat alpha7 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis
|
Rattus norvegicus
|
517.0
nM
|
|
Displacement of [3H]-Epibatidine from rat alpha4beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis
|
Rattus norvegicus
|
40.0
nM
|
|
Displacement of [3H]-Epibatidine from rat alpha4beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis
|
Rattus norvegicus
|
10.0
nM
|
|
Displacement of [3H]-Epibatidine from rat alpha3beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis
|
Rattus norvegicus
|
440.0
nM
|
|
Displacement of [3H]-Epibatidine from rat alpha3beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis
|
Rattus norvegicus
|
47.0
nM
|
|
Displacement of [3H]-Epibatidine from rat alpha2beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis
|
Rattus norvegicus
|
110.0
nM
|
|
Displacement of [3H]-Epibatidine from rat alpha2beta2 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis
|
Rattus norvegicus
|
12.0
nM
|
|
Agonist activity at alpha4beta2 nAChR in rat brain striatal slices assessed as release of [3H]dopamine release
|
Rattus norvegicus
|
220.0
nM
|
|
Displacement of [125I]alpha-bungarotoxin from alpha7 nAChR from rat hippocampus
|
Rattus norvegicus
|
230.0
nM
|
|
Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in HEK cells
|
Homo sapiens
|
260.0
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cortex
|
Rattus norvegicus
|
10.0
nM
|
|
Displacement of [3H]cytisine from human alpha4beta2 nAChR overexpressed in human SHEP cells after 75 mins by liquid scintillation spectrometric analysis
|
Homo sapiens
|
0.6
nM
|
|
Displacement of [3H]cytisine from human alpha4beta2 nAChR overexpressed in human SHEP cells after 75 mins by liquid scintillation spectrometric analysis
|
Homo sapiens
|
1.2
nM
|
|
Displacement of [3H]Epibatidine from human alpha3beta4 nACHR expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis
|
Homo sapiens
|
400.0
nM
|
|
Displacement of [3H]Nicotine from alpha4beta2 nACHR in human SHEP1 cell membranes after 2 hrs by liquid scintillation counting analysis
|
Homo sapiens
|
2.0
nM
|
|
Antagonist activity at human alpha6/alpha3beta2beta3 nAChR expressed in human SHEP1 cells assessed as inhibition of carbamylcholine-induced 86Rb+ ion efflux preincubated for 10 mins by liquid scintillation counting analysis
|
Homo sapiens
|
84.8
nM
|
|
Antagonist activity at human alpha4beta2 nACHR expressed in human SHEP1 cells assessed as inhibition of carbamylcholine-induced 86Rb+ ion efflux preincubated for 10 mins by liquid scintillation counting analysis
|
Homo sapiens
|
430.0
nM
|
|
Agonist activity at human alpha6/alpha3beta2beta3 nAChR expressed in human SHEP1 cells assessed as stimulation of 86Rb+ ion efflux after 5 mins by liquid scintillation counting analysis
|
Homo sapiens
|
127.0
nM
|
|
Agonist activity at human alpha4beta2 nACHR expressed in human SHEP1 cells assessed as stimulation of 86Rb+ ion efflux after 5 mins by liquid scintillation counting analysis
|
Homo sapiens
|
290.0
nM
|
|
Displacement of [3H]Epibatidine from rat alpha4beta4 nACHR by liquid scintillation counting analysis
|
Rattus norvegicus
|
23.0
nM
|
|
Displacement of [3H]Epibatidine from alpha4beta2 nACHR in rat forebrain by liquid scintillation counting analysis
|
Rattus norvegicus
|
9.8
nM
|
|
Displacement of [3H]Epibatidine from rat alpha4beta2 nACHR by liquid scintillation counting analysis
|
Rattus norvegicus
|
4.9
nM
|
|
Displacement of [3H]Epibatidine from rat alpha3beta4 nACHR by liquid scintillation counting analysis
|
Rattus norvegicus
|
260.0
nM
|
|
Displacement of [3H]Epibatidine from rat alpha3beta2 nACHR by liquid scintillation counting analysis
|
Rattus norvegicus
|
29.0
nM
|
|
Displacement of [3H]Epibatidine from rat alpha2beta4 nACHR by liquid scintillation counting analysis
|
Rattus norvegicus
|
70.0
nM
|
|
Displacement of [3H]Epibatidine from rat alpha2beta2 nACHR by liquid scintillation counting analysis
|
Rattus norvegicus
|
5.5
nM
|
|
Displacement of [125I]-alpha-bungarotoxin from alpha7 nAChR in rat hippocampus membranes
|
Rattus norvegicus
|
234.0
nM
|
|
Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cortex hippocampus
|
Rattus norvegicus
|
4.0
nM
|
|
Antagonist activity at human alpha4beta2 nAChR assessed as inhibition of nicotine-induced [86Rb+] efflux preincubated for 10 mins before nicotine exposure by cell-based liquid scintillation counting
|
Homo sapiens
|
370.0
nM
|
|
Displacement of [3H]epibatidine from nAChR in rat forebrain
|
Rattus norvegicus
|
12.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha7 nAChR expressed in HEK293 cells after 4 hrs
|
Rattus norvegicus
|
520.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta4 nAChR expressed in HEK293 cells after 4 hrs
|
Rattus norvegicus
|
40.0
nM
|
|
Displacement of [3H]epibatidine from human alpha4beta2 nAChR after 4 hrs by cell-based assay
|
Homo sapiens
|
10.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK293 cells after 4 hrs
|
Rattus norvegicus
|
440.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta2 nAChR expressed in HEK293 cells after 4 hrs
|
Rattus norvegicus
|
47.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha2beta4 nAChR expressed in HEK293 cells after 4 hrs
|
Rattus norvegicus
|
110.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha2beta2 nAChR expressed in HEK293 cells after 4 hrs
|
Rattus norvegicus
|
12.0
nM
|
|
Displacement of [3H]-epibatidine from alpha4beta2* nAChR in Sprague-Dawley rat cerebral cortex after 4 hrs by liquid scintillation counting analysis
|
Rattus norvegicus
|
1.5
nM
|
|
Displacement of [125I]-alpha-BTX from rat alpha7 nAChR after 4 hrs by liquid scintillation counting analysis
|
Rattus norvegicus
|
610.0
nM
|
|
Displacement of [3H]epibatidine from rat forebrain alpha2beta2 nAChR by competition binding assay
|
Rattus norvegicus
|
5.5
nM
|
|
Displacement of [3H]epibatidine from rat forebrain alpha2beta4 nAChR by competition binding assay
|
Rattus norvegicus
|
70.0
nM
|
|
Displacement of [3H]epibatidine from rat forebrain alpha3beta2 nAChR by competition binding assay
|
Rattus norvegicus
|
29.0
nM
|
|
Displacement of [3H]epibatidine from rat forebrain alpha3beta4 nAChR by competition binding assay
|
Rattus norvegicus
|
260.0
nM
|
|
Displacement of [3H]epibatidine from rat forebrain alpha4beta2 nAChR by competition binding assay
|
Rattus norvegicus
|
4.9
nM
|
|
Displacement of [3H]epibatidine from rat forebrain alpha4beta2* nAChR by competition binding assay
|
Rattus norvegicus
|
9.8
nM
|
|
Displacement of [3H]epibatidine from rat forebrain alpha4beta4 nAChR by competition binding assay
|
Rattus norvegicus
|
23.0
nM
|
|
Agonist activity at human alpha4beta2 nAChR expressed in SH-EP1 cells by [86Rb+] ion efflux assay
|
Homo sapiens
|
300.0
nM
|
|
Agonist activity at human alpha4beta2 nAChR expressed in SH-EP1 cells by [86Rb+] ion efflux assay
|
Homo sapiens
|
316.23
nM
|
|
Inactivation of human alpha4beta2 nAChR expressed in SH-EP1 cells by [86Rb+] ion efflux assay
|
Homo sapiens
|
430.0
nM
|
|
Inactivation of human alpha4beta2 nAChR expressed in SH-EP1 cells by [86Rb+] ion efflux assay
|
Homo sapiens
|
398.11
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta2 nAChR transfected in HEK293 cell membrane
|
Rattus norvegicus
|
11.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha4beta4 nAChR transfected in HEK293 cell membrane
|
Rattus norvegicus
|
51.0
nM
|
|
Displacement of [3H]epibatidine from rat alpha3beta4 nAChR transfected in HEK293 cell membrane
|
Rattus norvegicus
|
230.0
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cortex membranes by liquid scintillation counting method
|
Rattus norvegicus
|
4.0
nM
|
|
Displacement of [125I]]-alpha-bungarotoxin from alpha7 nAChR in rat hippocampus membranes by liquid scintillation counting method
|
Rattus norvegicus
|
234.0
nM
|
|
Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in HEK293 cell membranes by liquid scintillation counting method
|
Homo sapiens
|
261.0
nM
|
|
Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cerebral cortex homogenates after 4 hrs by liquid scintillation counting
|
Rattus norvegicus
|
1.5
nM
|
|
Displacement of [3H]epibatidine from immunoimmobilized alpha4beta2 nAChR in Sprague-Dawley rat striatal membranes by liquid scintillation counting
|
Rattus norvegicus
|
2.1
nM
|
|
Displacement of [3H]epibatidine from immunoimmobilized alpha6beta2 nAChR in Sprague-Dawley rat striatal membranes by liquid scintillation counting
|
Rattus norvegicus
|
3.3
nM
|
|
Displacement of [125I]alpha-bungarotoxin from alpha7 nAChR in Sprague-Dawley rat hippocampus membrane homogenates by gamma counting
|
Rattus norvegicus
|
250.0
nM
|
|
Binding affinity to Lymnaea stagnalis AChBP after 300 seconds by SPR biosensor analysis
|
Lymnaea stagnalis
|
320.0
nM
|
|
Binding affinity to Lymnaea stagnalis AChBP after 300 seconds by SPR biosensor analysis
|
Lymnaea stagnalis
|
316.23
nM
|
|
Displacement of [3H]epibatidine from rat neuronal acetylcholine receptor subunit alpha4beta2 expressed in HEK293 cell membranes incubated for 4 hrs by scintillation counting method
|
Rattus norvegicus
|
13.0
nM
|
|
Displacement of [3H]epibatidine from rat neuronal acetylcholine receptor subunit alpha4beta2 expressed in HEK293 cell membranes incubated for 4 hrs by scintillation counting method
|
Rattus norvegicus
|
14.13
nM
|
|
Displacement of [3H]epibatidine from rat neuronal acetylcholine receptor subunit alpha4beta4 expressed in HEK293 cell membranes incubated for 4 hrs by scintillation counting method
|
Rattus norvegicus
|
72.0
nM
|
|
Displacement of [3H]epibatidine from rat neuronal acetylcholine receptor subunit alpha4beta4 expressed in HEK293 cell membranes incubated for 4 hrs by scintillation counting method
|
Rattus norvegicus
|
72.44
nM
|
|
Displacement of [3H]epibatidine from rat neuronal acetylcholine receptor subunit alpha3beta4 expressed in HEK293 cell membranes incubated for 4 hrs by scintillation counting method
|
Rattus norvegicus
|
290.0
nM
|
|
Displacement of [3H]epibatidine from rat neuronal acetylcholine receptor subunit alpha3beta4 expressed in HEK293 cell membranes incubated for 4 hrs by scintillation counting method
|
Rattus norvegicus
|
288.4
nM
|
|
Agonist activity at mouse neuronal acetylcholine receptor subunit alpha4beta2 expressed in HEK293T cells by FMP assay
|
Mus musculus
|
720.0
nM
|
|
Agonist activity at mouse neuronal acetylcholine receptor subunit alpha4beta2 expressed in HEK293T cells by FMP assay
|
Mus musculus
|
724.44
nM
|
|
Agonist activity at alpha4beta2 nAChR in Sprague-Dawley rat striatal slices assessed as increase in [3H]-Dopamine release after 5 mins by microbeta counting
|
Rattus norvegicus
|
210.0
nM
|
|
Displacement of [3H]cytisine from Wistar rat cerebral cortex alpha4beta2* nAChR incubated for 75 mins by competition binding assay
|
Rattus norvegicus
|
2.3
nM
|
|
Displacement of [3H]-epibatidine from alpha4beta2-nACHR in rat cerebral cortex membranes preincubated for 30 mins followed by overnight incubation with [3H]-epibatine
|
Rattus norvegicus
|
4.0
nM
|
|
Displacement of [3H]-epibatine from human alpha3beta4-nACHR expressed in HEK243 cell membranes preincubated for 5 mins followed by overnight incubation with [3H]-epibatine by liquid scintillation counting analysis
|
Homo sapiens
|
260.0
nM
|
|
[3H]-Epibatidine Radioligand Binding Assay: Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm^2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris.HCl buffer (pH 7.4, 4 °C.). The cell suspension was centrifuged at 10,000×g for 5 min and the pellet was collected. The cell pellet was then homogenized in 10 mL buffer with a polytron homogenizer and centrifuged at 36,000 g for 10 min at 4 °C. The membrane pellet was resuspended in fresh buffer, and aliquots of the membrane preparation were used for binding assays. The concentration of [3H]-epibatidine used was ~500 pM for competition binding assays. Nonspecific binding was assessed in parallel incubations in the presence of 300 μM nicotine. Bound and free ligands were separated by vacuum filtration through Whatman GF/C filters treated with 0.5% polyethylenimine. The filter-retained radioactivity was measured by liquid scintillation counting. Specific binding was defined as the difference between total binding and nonspecific binding. Data from competition binding assays were analyzed using Prism 5 (GraphPad Software, San Diego, Calif.). The Kd values for [3H]-epibatidine used for calculating Ki values of nAChR subtypes were 0.02 nM for α2β2, 0.08 nM for α2β4, 0.03 nM for α3β2, 0.3 nM for α3β4, 0.04 nM for α4β2, 0.09 nM for α4β4, 1.8 nM for α7 and 0.05 for rat forebrain.
|
None
|
12.0
nM
|
|
[3H]-Epibatidine Radioligand Binding Assay: Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm^2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris.HCl buffer (pH 7.4, 4 °C.). The cell suspension was centrifuged at 10,000×g for 5 min and the pellet was collected. The cell pellet was then homogenized in 10 mL buffer with a polytron homogenizer and centrifuged at 36,000 g for 10 min at 4 °C. The membrane pellet was resuspended in fresh buffer, and aliquots of the membrane preparation were used for binding assays. The concentration of [3H]-epibatidine used was ~500 pM for competition binding assays. Nonspecific binding was assessed in parallel incubations in the presence of 300 μM nicotine. Bound and free ligands were separated by vacuum filtration through Whatman GF/C filters treated with 0.5% polyethylenimine. The filter-retained radioactivity was measured by liquid scintillation counting. Specific binding was defined as the difference between total binding and nonspecific binding. Data from competition binding assays were analyzed using Prism 5 (GraphPad Software, San Diego, Calif.). The Kd values for [3H]-epibatidine used for calculating Ki values of nAChR subtypes were 0.02 nM for α2β2, 0.08 nM for α2β4, 0.03 nM for α3β2, 0.3 nM for α3β4, 0.04 nM for α4β2, 0.09 nM for α4β4, 1.8 nM for α7 and 0.05 for rat forebrain.
|
None
|
110.0
nM
|
|
[3H]-Epibatidine Radioligand Binding Assay: Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm^2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris.HCl buffer (pH 7.4, 4 °C.). The cell suspension was centrifuged at 10,000×g for 5 min and the pellet was collected. The cell pellet was then homogenized in 10 mL buffer with a polytron homogenizer and centrifuged at 36,000 g for 10 min at 4 °C. The membrane pellet was resuspended in fresh buffer, and aliquots of the membrane preparation were used for binding assays. The concentration of [3H]-epibatidine used was ~500 pM for competition binding assays. Nonspecific binding was assessed in parallel incubations in the presence of 300 μM nicotine. Bound and free ligands were separated by vacuum filtration through Whatman GF/C filters treated with 0.5% polyethylenimine. The filter-retained radioactivity was measured by liquid scintillation counting. Specific binding was defined as the difference between total binding and nonspecific binding. Data from competition binding assays were analyzed using Prism 5 (GraphPad Software, San Diego, Calif.). The Kd values for [3H]-epibatidine used for calculating Ki values of nAChR subtypes were 0.02 nM for α2β2, 0.08 nM for α2β4, 0.03 nM for α3β2, 0.3 nM for α3β4, 0.04 nM for α4β2, 0.09 nM for α4β4, 1.8 nM for α7 and 0.05 for rat forebrain.
|
None
|
47.0
nM
|
|
[3H]-Epibatidine Radioligand Binding Assay: Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm^2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris.HCl buffer (pH 7.4, 4 °C.). The cell suspension was centrifuged at 10,000×g for 5 min and the pellet was collected. The cell pellet was then homogenized in 10 mL buffer with a polytron homogenizer and centrifuged at 36,000 g for 10 min at 4 °C. The membrane pellet was resuspended in fresh buffer, and aliquots of the membrane preparation were used for binding assays. The concentration of [3H]-epibatidine used was ~500 pM for competition binding assays. Nonspecific binding was assessed in parallel incubations in the presence of 300 μM nicotine. Bound and free ligands were separated by vacuum filtration through Whatman GF/C filters treated with 0.5% polyethylenimine. The filter-retained radioactivity was measured by liquid scintillation counting. Specific binding was defined as the difference between total binding and nonspecific binding. Data from competition binding assays were analyzed using Prism 5 (GraphPad Software, San Diego, Calif.). The Kd values for [3H]-epibatidine used for calculating Ki values of nAChR subtypes were 0.02 nM for α2β2, 0.08 nM for α2β4, 0.03 nM for α3β2, 0.3 nM for α3β4, 0.04 nM for α4β2, 0.09 nM for α4β4, 1.8 nM for α7 and 0.05 for rat forebrain.
|
None
|
440.0
nM
|
|
[3H]-Epibatidine Radioligand Binding Assay: Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm^2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris.HCl buffer (pH 7.4, 4 °C.). The cell suspension was centrifuged at 10,000×g for 5 min and the pellet was collected. The cell pellet was then homogenized in 10 mL buffer with a polytron homogenizer and centrifuged at 36,000 g for 10 min at 4 °C. The membrane pellet was resuspended in fresh buffer, and aliquots of the membrane preparation were used for binding assays. The concentration of [3H]-epibatidine used was ~500 pM for competition binding assays. Nonspecific binding was assessed in parallel incubations in the presence of 300 μM nicotine. Bound and free ligands were separated by vacuum filtration through Whatman GF/C filters treated with 0.5% polyethylenimine. The filter-retained radioactivity was measured by liquid scintillation counting. Specific binding was defined as the difference between total binding and nonspecific binding. Data from competition binding assays were analyzed using Prism 5 (GraphPad Software, San Diego, Calif.). The Kd values for [3H]-epibatidine used for calculating Ki values of nAChR subtypes were 0.02 nM for α2β2, 0.08 nM for α2β4, 0.03 nM for α3β2, 0.3 nM for α3β4, 0.04 nM for α4β2, 0.09 nM for α4β4, 1.8 nM for α7 and 0.05 for rat forebrain.
|
None
|
10.0
nM
|
|
[3H]-Epibatidine Radioligand Binding Assay: Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm^2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris.HCl buffer (pH 7.4, 4 °C.). The cell suspension was centrifuged at 10,000×g for 5 min and the pellet was collected. The cell pellet was then homogenized in 10 mL buffer with a polytron homogenizer and centrifuged at 36,000 g for 10 min at 4 °C. The membrane pellet was resuspended in fresh buffer, and aliquots of the membrane preparation were used for binding assays. The concentration of [3H]-epibatidine used was ~500 pM for competition binding assays. Nonspecific binding was assessed in parallel incubations in the presence of 300 μM nicotine. Bound and free ligands were separated by vacuum filtration through Whatman GF/C filters treated with 0.5% polyethylenimine. The filter-retained radioactivity was measured by liquid scintillation counting. Specific binding was defined as the difference between total binding and nonspecific binding. Data from competition binding assays were analyzed using Prism 5 (GraphPad Software, San Diego, Calif.). The Kd values for [3H]-epibatidine used for calculating Ki values of nAChR subtypes were 0.02 nM for α2β2, 0.08 nM for α2β4, 0.03 nM for α3β2, 0.3 nM for α3β4, 0.04 nM for α4β2, 0.09 nM for α4β4, 1.8 nM for α7 and 0.05 for rat forebrain.
|
Rattus norvegicus
|
40.0
nM
|
|
[3H]-Epibatidine Radioligand Binding Assay: Briefly, cultured cells at >80% confluence were removed from their flasks (80 cm^2) with a disposable cell scraper and placed in 10 mL of 50 mM Tris.HCl buffer (pH 7.4, 4 °C.). The cell suspension was centrifuged at 10,000×g for 5 min and the pellet was collected. The cell pellet was then homogenized in 10 mL buffer with a polytron homogenizer and centrifuged at 36,000 g for 10 min at 4 °C. The membrane pellet was resuspended in fresh buffer, and aliquots of the membrane preparation were used for binding assays. The concentration of [3H]-epibatidine used was ~500 pM for competition binding assays. Nonspecific binding was assessed in parallel incubations in the presence of 300 μM nicotine. Bound and free ligands were separated by vacuum filtration through Whatman GF/C filters treated with 0.5% polyethylenimine. The filter-retained radioactivity was measured by liquid scintillation counting. Specific binding was defined as the difference between total binding and nonspecific binding. Data from competition binding assays were analyzed using Prism 5 (GraphPad Software, San Diego, Calif.). The Kd values for [3H]-epibatidine used for calculating Ki values of nAChR subtypes were 0.02 nM for α2β2, 0.08 nM for α2β4, 0.03 nM for α3β2, 0.3 nM for α3β4, 0.04 nM for α4β2, 0.09 nM for α4β4, 1.8 nM for α7 and 0.05 for rat forebrain.
|
Rattus norvegicus
|
517.0
nM
|
|
Functional Assay: IC50(10′): The functional properties of the ligands were determined by 86Rb+ efflux assays in cells expressing α3β4 and α4β2 nAChR subtypes. The functional activity of each ligand was measured for its agonism, antagonism and desensitization ability. Agonist activity for each of the ligands was tested at eight different concentrations. The responses were compared to that stimulated by 100 μM (−)-nicotine, a near maximally effective concentration. The potency (IC50(0′)) of each ligand as an antagonist was derived from the full concentration-effect curves. We determined the desensitization potency of each ligand by pre-treating cells with the test compound for 10 minutes before 100 μM (−)-nicotine was applied. The potency of a ligand to desensitize the receptor after a 10 minute exposure (IC50(10′) was obtained with full concentration-effect curves using at least 8 concentrations of the ligand.
|
None
|
370.0
nM
|
|
Displacement of [3H]cytisine from alpha4beta2 nAChR expressed in human recombinant SH-SY5Y cell membranes after 120 mins
|
Homo sapiens
|
1.5
nM
|
|
Displacement of [3H]epibatidine from rat cerebral cortex membrane alpha4beta2* nAChR pretreated for 5 mins followed by [3H]epibatidine addition after overnight incubation by beta counter
|
Rattus norvegicus
|
4.0
nM
|
|
Displacement of [125I]alpha-bungarotoxin from rat hippocampus membrane alpha7* nAChR pretreated for 5 mins followed by [125I]alpha-bungarotoxin addition after overnight incubation by gamma counter
|
Rattus norvegicus
|
234.0
nM
|
|
Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in HEK293 cells pretreated for 5 mins followed by [3H]epibatidine addition after overnight incubation by beta counter
|
Homo sapiens
|
261.0
nM
|
|
Agonist activity at alpha4beta2 nAChR (unknown origin)
|
Homo sapiens
|
0.045
nM
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
-15.48
%
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
6.98
%
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
-4.81
%
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
-4.09
%
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
11.55
%
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
1.61
%
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
-2.7
%
|
|
Displacement of [3H]-cytisine from alpha4beta2* nAChR in Wistar rat cerebral cortex membranes after 75 mins
|
Rattus norvegicus
|
2.31
nM
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
22.06
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.06
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.06
%
|
|
Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in CHOK1 cell membrane by microbeta scintillation counting method
|
Homo sapiens
|
2.2
nM
|
|
Binding affinity to rat alpha4beta2 nAChR
|
Rattus norvegicus
|
4.1
nM
|
|
Displacement of [3H]cytisine from rat brain nAChR using radiolabelled compound
|
Rattus norvegicus
|
7.8
nM
|
|
Displacement of [3H]cytisine from human alpha4beta2 nAChR by Cheng-Prusoff equation analysis
|
Homo sapiens
|
1.6
nM
|
|
Displacement of [3H]cytisine from human alpha4beta2 nAChR by radioligand competition analysis
|
Homo sapiens
|
4.9
nM
|
|
Binding affinity to Sprague-Dawley rat brain nAChR incubated for 90 min by scatchard analysis
|
Rattus norvegicus
|
0.89
nM
|
|
Agonist activity at nAChR in rat striatal synaptosomes assessed as [3H]dopamine release
|
Rattus norvegicus
|
100.0
nM
|
|
Agonist activity at alpha4beta2 nAChR in rat thalamic synaptosomes assessed as increase in 86Rb efflux
|
Rattus norvegicus
|
591.0
nM
|
|
Agonist activity at alpha4beta2 nAChR in rat frontal cortex membrane
|
Rattus norvegicus
|
77.0
nM
|
|
Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat frontal cortex membrane by scintillation counting method
|
Rattus norvegicus
|
11.0
nM
|
|
Agonist activity at human brain alpha4beta2 nAChR expressed in CHO cells by patch clamp electrophysiological assay
|
Homo sapiens
|
800.0
nM
|
|
Displacement of 3H-cytisine from Sprague-Dawley rat brain alpha4beta2 nAChR by liquid scintillation counting method
|
Rattus norvegicus
|
2.0
nM
|
|
Displacement of 3H-cytisine from rat brain alpha4beta2 nAChR by radioligand binding assay
|
Rattus norvegicus
|
5.6
nM
|
|
Binding affinity to alpha3beta4 nAChR (unknown origin)
|
Homo sapiens
|
530.0
nM
|
|
Agonist activity at alpha4beta2 nAChR (unknown origin)
|
Homo sapiens
|
1.0
nM
|
|
Binding affinity to rat alpha7 nAChR
|
Rattus norvegicus
|
400.0
nM
|
|
Displacement of [125I]alpha-bungarotoxin from alpha7nAChR in rat hippocampus membranes preincubated for 5 mins followed by [125I]alpha-bungarotoxin addition and measured after overnight incubation by liquid scintillation beta counter analysis
|
Rattus norvegicus
|
234.0
nM
|
|
Displacement of [3H]-epibatidine from human alpha3beta4 transfected in HEK293 cell membranes preincubated for 5 mins followed by [3H]-epibatidine addition and measured after overnight incubation by liquid scintillation beta counter analysis
|
Homo sapiens
|
261.0
nM
|
|
Displacement of [3H]-Epibatidine from alpha4beta2 nAChR in rat cerebral cortex membrane preincubated for 5 mins followed by [3H]-Epibatidine addition and measured after overnight incubation by liquid scintillation beta counter analysis
|
Rattus norvegicus
|
4.0
nM
|
|
Displacement of [125I] alpha bungarotoxin from human neuronal alpha4beta2 nAChR expressed in human SH-SY5Y cell membrane measured after 120 mins by Topcount scintillation counting method
|
Homo sapiens
|
1.5
nM
|
|