Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampal membranes
|
Rattus norvegicus
|
7.0
nM
|
|
Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of bovine hippocampus.
|
Bos taurus
|
3.1
nM
|
|
Binding affinity of compound towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT (0.5 nM) ligand in hippocampus + frontal bovine was determined
|
None
|
8.6
nM
|
|
Ability to displace [3H]-DPAT from 5-hydroxytryptamine 1A receptor in homogenates of bovine hippocampus.
|
None
|
6.6
nM
|
|
In vitro binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT in human CYP3A4 assay
|
None
|
25.0
nM
|
|
Binding affinity towards rat 5-hydroxytryptamine 1A receptor was evaluated using [3H]8-OH-DPAT as radioligand
|
None
|
30.0
nM
|
|
Binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampus membranes using [3H]8-OH-DPAT as radioligand
|
None
|
30.0
nM
|
|
Binding affinity to 5-hydroxytryptamine 1A receptor of rat hippocampus with [3H]8-OH-DPAT as radioligand
|
None
|
11.0
nM
|
|
Binding affinity against 5-hydroxytryptamine 1A (5-HT1A) receptor in rat hippocampus membranes
|
None
|
60.0
nM
|
|
Binding affinity to 5-hydroxytryptamine 1A receptor in rat hippocampus membranes,3H-8-OH-DPAT and buspirone for nonspecific binding (NSB)
|
None
|
60.0
nM
|
|
In vitro inhibition of [3H]8-OH-DPAT binding to rat 5-HT 1a receptors.
|
None
|
50.0
nM
|
|
In vitro ability to inhibit binding of radioligand [3H]8-OH-DPAT to 5-hydroxytryptamine 1A receptor in rat cerebral cortex
|
None
|
12.8
nM
|
|
In vitro binding affinity measured on serotonin 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand.
|
None
|
12.8
nM
|
|
In vitro binding affinity towards the 5-hydroxytryptamine 1A receptor was evaluated
|
None
|
24.0
nM
|
|
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
|
None
|
52.0
nM
|
|
Binding affinity against human 5-hydroxytryptamine 1A receptor
|
None
|
15.0
nM
|
|
Binding affinity for 5-hydroxytryptamine 1A receptor with [3H]5-HT
|
Rattus norvegicus
|
46.1
nM
|
|
Binding affinity by measuring displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor in rat hippocampus
|
None
|
15.0
nM
|
|
Binding affinity towards 5-hydroxytryptamine 1A receptor in the rat brain (hippocampus) using [3H]8-OH-DPAT
|
Rattus norvegicus
|
12.3
nM
|
|
Binding affinity against rat hippocampal 5-hydroxytryptamine 1A (5-HT1A) receptor determined using [3H]8-OH-DPAT as radioligand
|
None
|
15.0
nM
|
|
Binding was determined on 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
|
None
|
32.0
nM
|
|
Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101
|
None
|
5.0
nM
|
|
Binding affinity at 5-hydroxytryptamine 1A receptor in rat cerebral cortex membranes by [3H]8-OH-DPAT displacement.
|
None
|
20.5
nM
|
|
Binding affinity towards rat 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand.
|
None
|
20.5
nM
|
|
In vitro ability to displace [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor sites of rat brain cortex.
|
None
|
15.4
nM
|
|
In vitro ability to inhibit [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor of rat hippocampus
|
None
|
10.0
nM
|
|
Evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain
|
None
|
15.0
nM
|
|
Binding affinity towards 5-hydroxytryptamine 1A receptor using receptor binding assay
|
None
|
7.13
nM
|
|
Effect against 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at 0.1 uM dose
|
Rattus norvegicus
|
84.0
%
|
|
Effect on 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at dose of 0.1 uM + 1 uM 5-HT.
|
None
|
43.0
%
|
|
Effect on 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at dose of 10 uM
|
None
|
73.0
%
|
|
Effect on 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at dose of 1 uM
|
None
|
75.0
%
|
|
Effect on 5-hydroxytryptamine 1A receptor mediated inhibition of VIP-stimulated cAMP production at dose of 1 uM+ 10 uM 5-HT.
|
None
|
64.0
%
|
|
Binding affinity against rat 5-hydroxytryptamine 1A receptor
|
None
|
9.3
nM
|
|
In vitro inhibition of [3H]spiperone binding to 5-hydroxytryptamine 1A receptor from rat hippocampal tissue.
|
None
|
10.0
nM
|
|
Antagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptor
|
None
|
10.0
nM
|
|
Inhibitory affinity constant against 5-hydroxytryptamine 1A receptor
|
None
|
13.8
nM
|
|
Binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 from rat hippocampus
|
Rattus norvegicus
|
5.0
nM
|
|
Binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
|
None
|
21.88
nM
|
|
Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement
|
None
|
19.95
nM
|
|
In vitro ability to inhibit binding of radioligand [3H]8-OH-DPAT to 5-hydroxytryptamine 1A receptor in rat cerebral cortex
|
None
|
14.79
nM
|
|
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
|
Rattus norvegicus
|
17.0
nM
|
|
In vitro binding affinity measured on serotonin 5-hydroxytryptamine 2 receptor using [3H]ketanserin as radioligand.
|
None
|
10.0
nM
|
|
Binding affinity against 5-hydroxytryptamine 2 receptor
|
None
|
178.0
nM
|
|
Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor
|
Rattus norvegicus
|
391.0
nM
|
|
The compound was tested for its binding affinity towards 5-hydroxytryptamine 2 receptor by displacing [3H]ketanserin radioligand in rat cerebral cortex
|
None
|
174.0
nM
|
|
Compound was evaluated for binding affinity against 5-hydroxytryptamine 2A receptor using [3H]ketanserin as a radioligand
|
None
|
482.0
nM
|
|
Compound was evaluated for the binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]-ketanserin radioligand.
|
None
|
482.0
nM
|
|
Binding affinity towards alpha-1 adrenergic receptor using [3H]prazosin radioligand.
|
None
|
367.0
nM
|
|
The compound was tested for its binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]WB-4101 radioligand in rat cerebral cortex
|
None
|
138.0
nM
|
|
Percent inhibition of Alpha-1 adrenergic receptor by 1 uM of compound
|
None
|
33.0
%
|
|
Antagonistic activity at Alpha-1 adrenergic receptor was performed on ring segments of rabbit thoracic aorta contracted by noradrenaline.
|
Oryctolagus cuniculus
|
575.44
nM
|
|
Binding affinity at Alpha-1 adrenergic receptor in rat cerebral cortex membranes by [3H]prazosin displacement.
|
None
|
367.0
nM
|
|
Percent inhibition of GABA-A benzodiazepine receptor at 1 uM
|
Rattus norvegicus
|
0.0
%
|
|
Percent inhibition of Beta adrenergic receptor by 1 uM of compound
|
None
|
0.0
%
|
|
Binding affinity for DA2 receptor
|
None
|
90.0
nM
|
|
Binding affinity towards rat Dopamine receptor D2 was evaluated using [3H]- spiroperidol as radioligand
|
None
|
280.0
nM
|
|
Binding affinity against Dopamine receptor D2 in rat striatal membrane using [3H]spiroperidol as radioligand
|
None
|
280.0
nM
|
|
Binding affinity to Dopamine receptor D2 in of rat striatum membrane with [3H]- raclopride as radioligand
|
None
|
55.0
nM
|
|
Inhibition of [3H]raclopride binding to Dopamine receptor D2 of bovine striatum
|
Bos taurus
|
44.0
nM
|
|
Inhibition of [3H]spiperone binding to dopamine receptor from rat corpus striatal membranes
|
None
|
120.0
nM
|
|
Displacement of [3H]U-86170 from human D2-dopamine receptor expressed in CHO K1 cells
|
Homo sapiens
|
13.0
nM
|
|
In vitro ability to inhibit binding of radioligand [3H]spiroperidol to dopamine D2 receptor in rat striatal membrane
|
None
|
41.69
nM
|
|
Inhibition of binding of radioligand [3H]spiroperidol to dopamine D2 receptor in rat striatal membranes
|
None
|
222.0
nM
|
|
In vitro binding affinity measured on dopamine receptor D2 using [3H]spiroperidol as radioligand.
|
None
|
226.0
nM
|
|
In vitro binding affinity towards the dopamine receptor D2 at 10 e-6 M
|
None
|
265.0
nM
|
|
Inhibition of [3H]spiperone binding to Dopamine receptor D3 in bovine cortex
|
Bos taurus
|
660.0
nM
|
|
Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone
|
None
|
367.0
nM
|
|
Compound was evaluated for binding affinity against Dopamine receptor D2 using [3H]raclopride as a radioligand
|
None
|
852.0
nM
|
|
Binding affinity towards dopamine receptor D2 using [3H]-raclopride radioligand.
|
None
|
852.0
nM
|
|
In vitro ability to inhibit [3H]spiperone binding to dopamine receptor D2 of rat limbic structures
|
None
|
119.0
nM
|
|
In vitro inhibition of [3H]spiperone binding to Dopamine receptor D2 from rat brain limbic tissue
|
None
|
119.0
nM
|
|
Inhibitory activity against rat limbic tissue Dopamine receptor D2
|
None
|
119.0
nM
|
|
Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum
|
None
|
367.0
nM
|
|
Neuronal protective effect of compound against ischemic brain damage in rat t-MCAO model
|
Rattus norvegicus
|
53.0
%
|
|
The compound was tested for affinity towards sigma-3 receptor
|
None
|
36.31
nM
|
|
In vitro binding affinity measured on sigma opioid receptor using [3H]DTG as radioligand
|
Cavia porcellus
|
263.0
nM
|
|
Inhibition of [3H]DTG binding to sigma receptor in rat hippocampus
|
Rattus norvegicus
|
48.0
nM
|
|
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM
|
Cavia porcellus
|
2.0
%
|
|
Inhibitory concentration against Dopamine receptor D2 in rat striatum membrane using [3H]raclopride as radioligand
|
Rattus norvegicus
|
55.0
nM
|
|
Inhibitory concentration against 5-hydroxytryptamine 1A receptor in rat hippocampus membrane using [3H]-8-OH-DPAT as radioligand
|
Rattus norvegicus
|
11.0
nM
|
|
Displacement of [3H]8-OH-DPAT from human 5HT1A receptor in HEK293 cells
|
Homo sapiens
|
20.0
nM
|
|
Displacement of [3H]prazosin from adrenergic alpha-1 receptor in rat cerebral cortex cells
|
Rattus norvegicus
|
367.0
nM
|
|
Binding affinity to D2 receptor by radioligand binding assay
|
Homo sapiens
|
13.0
nM
|
|
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
|
Homo sapiens
|
80.0
nM
|
|
Affinity for 5HT1A receptor
|
Homo sapiens
|
17.0
nM
|
|
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus
|
Rattus norvegicus
|
15.0
nM
|
|
Displacement of [3H]prazosin from adrenergic receptor alpha1 in CRL:CD(SD)BR-COBS rat brain cortex
|
Rattus norvegicus
|
600.0
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
|
24.7
%
|
|
Displacement of [3H]8-OH-DPAT from human 5HT1A receptor
|
Homo sapiens
|
15.0
nM
|
|
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
|
Homo sapiens
|
41.0
nM
|
|
Displacement of [3H]ketanserin from 5HT2A receptor
|
None
|
851.0
nM
|
|
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat hippocampal membranes
|
Rattus norvegicus
|
3.8
nM
|
|
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat hippocampal membrane
|
Rattus norvegicus
|
36.0
nM
|
|
Binding affinity to 5HT1A receptor
|
None
|
10.0
nM
|
|
Binding affinity to 5HT1A receptor
|
None
|
24.0
nM
|
|
Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in CHO cells by liquid scintillation counting
|
None
|
20.0
nM
|
|
Inhibition of human FAAH at 1 uM
|
Homo sapiens
|
4.81
%
|
|
Displacement of [3H]DPAT from 5HT1A receptor in Wistar rat hippocampus using 2 x 10' -7 by liquid scintillation counting
|
Rattus norvegicus
|
63.0
mg kg-1
|
|
Displacement of [3H]DPAT from 5HT1A receptor in Wistar rat hippocampus using 2 x 10' -8 by liquid scintillation counting
|
Rattus norvegicus
|
87.0
mg kg-1
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
16.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
9.307
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
653.0
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
529.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
750.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
477.0
nM
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
504.0
nM
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
212.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
323.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
108.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
44.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
15.0
nM
|
|
TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Buspirone: 100 uM) in MDR1-expressing MDCKII cells
|
None
|
24.1
%
|
|
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
|
33.3
%
|
|
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
|
-5.6
%
|
|
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
|
-13.9
%
|
|
Displacement of [3H]5-carboxamidotryptamine to human 5HT1A expressed in HEK293 cells by filter binding assay
|
Homo sapiens
|
21.0
nM
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
70.0
%
|
|
Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr
|
Homo sapiens
|
12.0
nM
|
|
Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
|
Homo sapiens
|
22.0
nM
|
|
Displacement of [3H]-8-OH-DPAT from 5-HT1AR in rat hippocampus
|
Rattus norvegicus
|
20.0
nM
|
|
Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells
|
Homo sapiens
|
20.0
nM
|
|
Displacement of [3H]-8-OH-DPAT from 5HT1A receptor (unknown origin)
|
Homo sapiens
|
34.3
nM
|
|
Displacement of [3H]methylspiperone from human D2 receptor expressed in HEK cells
|
Homo sapiens
|
484.0
nM
|
|
Binding affinity to 5-HT1A (unknown origin)
|
Homo sapiens
|
4.78
nM
|
|
Displacement of [3H]-8-OH-DPAT from human 5HT1AR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
|
Homo sapiens
|
20.0
nM
|
|
Agonist activity at 5HT1A receptor (unknown origin)
|
Homo sapiens
|
8.9
nM
|
|
Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method
|
Homo sapiens
|
20.0
nM
|
|
Displacement of [3H]methylspiperone from human D2 receptor expressed in HEK-GIRK-M4 cell membrane by radioligand binding assay
|
Homo sapiens
|
484.0
nM
|
|
Binding affinity to 5HT1A receptor (unknown origin)
|
Homo sapiens
|
4.0
nM
|
|
Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
|
Homo sapiens
|
21.0
nM
|
|
Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
|
Homo sapiens
|
34.3
nM
|
|
Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counter method
|
Homo sapiens
|
32.36
nM
|
|
Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counter method
|
Homo sapiens
|
32.2
nM
|
|
Displacement of [3H]-8-OH-DPAT from human 5-HT1A expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay
|
Homo sapiens
|
20.0
nM
|
|
Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells after 1 hr by microbeta scintillation counting method
|
Homo sapiens
|
32.2
nM
|
|
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
|
Homo sapiens
|
840.0
nM
|
|
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT1A receptor expressed in HEK293T cell membranes incubated for 90 mins by scintillation counting method
|
Homo sapiens
|
50.0
nM
|
|
Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method
|
Homo sapiens
|
5.012
nM
|
|
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
|
Homo sapiens
|
15.14
nM
|
|
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
|
Homo sapiens
|
72.44
nM
|
|
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
|
Homo sapiens
|
186.21
nM
|
|
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
|
Homo sapiens
|
38.02
nM
|
|
Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method
|
Homo sapiens
|
5.012
nM
|
|
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay
|
Homo sapiens
|
15.14
nM
|
|
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
|
Homo sapiens
|
72.44
nM
|
|
Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay
|
Homo sapiens
|
186.21
nM
|
|
Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
|
Homo sapiens
|
20.0
nM
|
|