|
Binding affinity for rat 5-hydroxytryptamine transporter.
|
None
|
126.0
nM
|
|
|
Inhibitory activity against [3H]- 5-hydroxytryptamine reuptake in whole rat brain minus cerebellum
|
Rattus norvegicus
|
73.0
nM
|
|
|
Binding affinity was determined at the dopamine transporter labeled with radioligand [125 I] RTI-55 in nonstandard conditions
|
None
|
2.63
nM
|
|
|
Reuptake inhibition was determined at the dopamine transporter labeled with radioligand [3H]dopamine in nonstandard conditions on brain membranes obtained from rat
|
None
|
1.75
nM
|
|
|
Inhibition of [3H]DA reuptake in rat caudate homogenate.
|
None
|
7.3
nM
|
|
|
Affinity was evaluated using [3H]DA (radioligand) on Cloned human Dopamine transporter expressed in HEK cells
|
None
|
26.0
nM
|
|
|
Affinity was evaluated using [3H]WIN-35428 (radioligand) on Cloned human Dopamine transporter expressed in HEK cells
|
None
|
43.0
nM
|
|
|
Competitive binding versus [N-methyl-3H]WIN-35428 in murine kidney cells transfected with human dopamine transporter
|
None
|
0.36
nM
|
|
|
In vitro binding affinity at dopamine transporter in rat striatum by [3H]WIN-35428 displacement.
|
None
|
10.6
nM
|
|
|
Binding affinity for rat Dopamine transporter.
|
None
|
3.7
nM
|
|
|
Binding affinity at dopamine transporter from rat striatal membrane tissue by [3H]CFT displacement.
|
None
|
6.0
nM
|
|
|
Binding affinity towards dopamine transporter in rat striatum using [3H]WIN-35 428 as radioligand
|
None
|
10.6
nM
|
|
|
Binding affinity was determined at the dopamine transporter labeled with radioligand [125 I] RTI-55
|
None
|
3.7
nM
|
|
|
Binding against Dopamine transporter using radioligand as [3H]GBR 12935
|
None
|
5.5
nM
|
|
|
Inhibition of dopamine DA reuptake
|
None
|
4.3
nM
|
|
|
Compound was tested for its ability to inhibit the neurotransmitter dopamine-DA reuptake system using [3H]dopamine as radioligand
|
None
|
4.3
nM
|
|
|
Compound was tested for its ability to inhibit the uptake of [3H]dopamine in DAT (dopamine transporter system) expressing cell line
|
None
|
4.3
nM
|
|
|
Binding affinity at the dopamine transporter in rast striatum by [3H]WIN-35428 displacement.
|
None
|
10.6
nM
|
|
|
IC50 value was evaluated using [3H]WIN-35428 (radioligand) on Dopamine transporter in rat striatum.
|
None
|
19.3
nM
|
|
|
Inhibition of binding of 3[H] WIN-35 428 to Dopamine transporter (DAT) of rat striatum.
|
None
|
10.6
nM
|
|
|
Inhibition of binding of [3H]WIN-35 428 to (DAT) dopamine transporter in rat striatum
|
None
|
10.6
nM
|
|
|
Inhibition of uptake from dopamine transporter in rat striatum using [3H]DA as radioligand
|
None
|
6.63
nM
|
|
|
Inhibitory activity against dopamine transporter (DAT) labeled with [3H]WIN-35428 in rat brain striatal membrane.
|
None
|
14.0
nM
|
|
|
In vitro inhibition of [3H]WIN-35 428 binding to dopamine transporter on rat striatal membranes.
|
None
|
14.0
nM
|
|
|
Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter.
|
None
|
1.0
nM
|
|
|
Inhibition of [3H]BTCP binding to the dopamine transporter.
|
None
|
4.0
nM
|
|
|
Inhibition of [3H]GBR-12935 binding to the dopamine transporter.
|
None
|
3.0
nM
|
|
|
Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter.
|
None
|
24.0
nM
|
|
|
Inhibition of [3H]WIN-35428 binding to the dopamine transporter.
|
None
|
33.0
nM
|
|
|
Inhibition of [3H]cocaine binding to the dopamine transporter.
|
None
|
36.0
nM
|
|
|
Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]-5-HT on synaptosomes obtained from whole rat brain minus cerebellum.
|
None
|
73.0
nM
|
|
|
Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]dopamine on synaptosomes obtained from rat caudate.
|
None
|
7.3
nM
|
|
|
Inhibition of Dopamine uptake in male Sprague-Dawley rats using [3H]DA ligand
|
Rattus norvegicus
|
2.3
nM
|
|
|
Affinity at rat dopamine transporter using [125I]RTI-55 displacement.
|
None
|
3.7
nM
|
|
|
Binding affinity against Dopamine transporter using [125]RTI-55
|
None
|
3.7
nM
|
|
|
Binding affinity against dopamine transporter labelled with [125I]- RTI-55 in rat.
|
None
|
3.7
nM
|
|
|
Binding affinity against dopamine transporter was determined by the displacement of [3H]WIN-35428 radioligand in rat brain
|
None
|
11.9
nM
|
|
|
Binding affinity at Dopamine transporter by displacing [3H]WIN-35428 from rat caudate putamen
|
None
|
11.9
nM
|
|
|
Binding affinity towards dopamine transporter (DAT)
|
None
|
3.7
nM
|
|
|
Binding affinity for dopamine transporter
|
None
|
3.7
nM
|
|
|
Affinity for rat dopamine transporter using [3H]WIN-35428 displacement.
|
None
|
11.6
nM
|
|
|
Compound was evaluated for its ability to displace [3H]WIN-35428 binding in rat caudate-putamen
|
None
|
11.6
nM
|
|
|
Displacement of [3H]WIN-35428 from dopamine transporter of rat caudate putamen tissue
|
Rattus norvegicus
|
12.0
nM
|
|
|
In vitro binding affinity towards dopamine transporter in rat striatal membranes by [3H]GBR-12395 displacement.
|
None
|
0.06
nM
|
|
|
Inhibition of [3H]dopamine uptake via rat dopamine receptor.
|
None
|
4.3
nM
|
|
|
Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes
|
None
|
0.88
nM
|
|
|
Inhibitory constant towards reuptake of [125I]-13 from dopamine transporter in rat striatal membranes
|
None
|
10.4
nM
|
|
|
Binding affinity Sprague-Dawley rats using [3H]WIN-35428 ligand
|
None
|
12.0
nM
|
|
|
Binding affinity to dopamine transporter (DAT) using [3H]WIN-35428 as a radioligand
|
None
|
12.02
nM
|
|
|
Binding affinity at dopamine transporter from rat caudate-putamen tissue by [3H]WIN-35428 displacement.
|
None
|
12.0
nM
|
|
|
The inhibition of reuptake against dopamine transporter
|
None
|
4.3
nM
|
|
|
Binding affinity towards dopamine transporter (DAT) by using [125I]RTI-55 radioligand
|
None
|
3.7
nM
|
|
|
Inhibition of binding of [3H]- nisoxatine to Norepinephrine transporter (NET) of rat cerebral cortex.
|
None
|
496.0
nM
|
|
|
Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum
|
None
|
496.0
nM
|
|
|
Compound was tested for the inhibition of norepinephrine (NE) reuptake
|
None
|
79.0
nM
|
|
|
Affinity at norepinephrine transporter (NET) in rat striatum, using [3H]- nisoxatine as radioligand
|
None
|
496.0
nM
|
|
|
Binding affinity towards norepinephrine transporter in rat striatum using [3H]nisoxetine as radioligand
|
None
|
496.0
nM
|
|
|
Binding affinity at the norepinephrine transporter in rat striatum by [3H]nisoxetine displacement.
|
None
|
496.0
nM
|
|
|
Inhibition of [3H]norepinephrine uptake at the rat norepinephrine transporter.
|
None
|
79.0
nM
|
|
|
Inhibition of DAT uptake was determined by measuring the [3H]DA accumulation in rat striatal synaptosomes
|
Rattus norvegicus
|
6.63
nM
|
|
|
Inhibition of [3H]- DA (Dopamine) uptake in rat striatal synaptosomes
|
Rattus norvegicus
|
6.63
nM
|
|
|
Inhibition of [3H]DA dopamine (DA) reuptake activity
|
Rattus norvegicus
|
6.63
nM
|
|
|
Reuptake inhibition of [3H]-labeled dopamine (DA) in rat.
|
Rattus norvegicus
|
7.3
nM
|
|
|
Reuptake inhibition of [3H]-5-HT (5-HT) in rat.
|
None
|
73.0
nM
|
|
|
Compound was evaluated for its ability to block the [3H]-Dopamine uptake in rat caudate-putamen
|
Rattus norvegicus
|
5.0
nM
|
|
|
Inhibition of 5-HT reuptake from rat caudate using [3H]5-HT
|
Rattus norvegicus
|
73.0
nM
|
|
|
Inhibition of Dopamine reuptake from rat caudate using [3H]DA
|
Rattus norvegicus
|
4.3
nM
|
|
|
Inhibition of binding of [3H]- citalopram to Serotonin transporter (SERT) of rat cerebral cortex.
|
None
|
132.0
nM
|
|
|
Binding affinity for serotonin transporter
|
None
|
130.0
nM
|
|
|
The compound was tested for affinity towards sigma-3 receptor
|
None
|
1.0
nM
|
|
|
Affinity was evaluated using [3H]citalopram (radioligand) on human serotonin transporter expressed in HEK cells
|
None
|
741.0
nM
|
|
|
In vitro binding affinity at serotonin transporter in rat striatum by [3H]- citalopram displacement.
|
None
|
132.0
nM
|
|
|
Binding affinity at serotonin transporter from rat brain striatal membrane by [3H]citalopram displacement.
|
None
|
82.0
nM
|
|
|
Binding affinity towards serotonin transporter in rat striatum using [3H]citalopram as radioligand
|
None
|
132.0
nM
|
|
|
Binding affinity was determined at the Serotonin transporter labeled with radioligand [125 I] RTI-55
|
Rattus norvegicus
|
126.0
nM
|
|
|
Binding affinity of Sigma opioid receptor type 1 in Guinea pig brain membranes using [3H]pentazocine ligand
|
None
|
318.0
nM
|
|
|
Binding affinity of Sigma opioid receptor type 2 in rat liver membranes using [3H]DTG ligand
|
Rattus norvegicus
|
116.0
nM
|
|
|
Inhibition of [3H]5-HT reuptake at rat serotonin transporter
|
None
|
73.0
nM
|
|
|
Compound was tested for its ability to inhibit the neurotransmitter serotonin-5-HT reuptake system using [3H]5-HT as radioligand
|
None
|
70.0
nM
|
|
|
Binding affinity at serotonin transporter in rat striatum by [3H]citalopram displacement.
|
None
|
132.0
nM
|
|
|
IC50 value was evaluated using [3H]citalopram (radioligand) on serotonin transporter in rat striatum.
|
None
|
87.0
nM
|
|
|
Inhibition of binding of [3H]citalopram to (SERT) serotonin transporter in rat striatum
|
None
|
132.0
nM
|
|
|
Inhibitory activity against serotonin transporter (SERT) labeled with [3H]-citalopram in rat brain striatal membrane.
|
None
|
86.6
nM
|
|
|
In vitro inhibition of [3H]citalopram binding to serotonin transporter on rat striatal membranes.
|
None
|
82.0
nM
|
|
|
Sigma receptor binding was determined by labeling with radioligand [3H](+)-pentazocine on frozen membranes obtained from frozen guinea pig brain
|
Cavia porcellus
|
43.0
nM
|
|
|
Affinity at rat serotonin transporter using [125I]RTI-55 displacement.
|
None
|
126.0
nM
|
|
|
Binding affinity against Serotonin transporter (SERT) labelled with [125I]RTI-55 in rat.
|
None
|
126.0
nM
|
|
|
Binding affinity against serotonin transporter using [125]RTI-55
|
None
|
130.0
nM
|
|
|
Binding affinity against serotonin transporter by displacement of [3H]citalopram in rat brain
|
Rattus norvegicus
|
105.0
nM
|
|
|
Binding affinity at Serotonin transporter using [3H]citalopram as radioligand from rat brain
|
None
|
105.0
nM
|
|
|
Binding affinity towards rat serotonin transporter (SERT)
|
None
|
126.0
nM
|
|
|
Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand
|
Cavia porcellus
|
318.0
nM
|
|
|
In vitro binding affinity towards serotonin transporter in rat cerebral cortical homogenates by [3H]paroxetine displacement.
|
None
|
52.8
nM
|
|
|
Inhibition of [3H]5-HT uptake at the rat serotonin transporter.
|
None
|
73.0
nM
|
|
|
Binding affinity against Serotonin transporter in male Sprague-Dawley rats using [3H]paroxetine ligand
|
None
|
24.1
nM
|
|
|
The inhibition of reuptake against Serotonin transporter (5-HT)
|
None
|
73.0
nM
|
|
|
Binding affinity for serotonin transporter (SERT) using [125I]RTI-55
|
None
|
126.0
nM
|
|
|
Inhibition of dopamine reuptake ([3H]DA uptake) in rat cytosol
|
Rattus norvegicus
|
6.63
nM
|
|
|
Inhibition of rat brain dopamine transporter as accumulation of [3H]DA
|
Rattus norvegicus
|
10.6
nM
|
|
|
Inhibition of rat brain Serotonin transporter as accumulation of [3H]5-HT
|
Rattus norvegicus
|
91.1
nM
|
|
|
Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]-NE
|
Rattus norvegicus
|
102.0
nM
|
|
|
Inhibition of rat brain Dopamine transporter uptake as [3H]DA accumulation
|
Rattus norvegicus
|
14.2
nM
|
|
|
Inhibition of rat brain Serotonin transporter uptake as [3H]5-HT accumulation
|
Rattus norvegicus
|
101.4
nM
|
|
|
Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]NE
|
Rattus norvegicus
|
114.0
nM
|
|
|
Inhibition of [3H]WIN-35428 binding to rat brain dopamine transporter
|
Rattus norvegicus
|
10.6
nM
|
|
|
Displacement of [125I]RTI-55 dopamine transporter binding in rat striatal membrane
|
Rattus norvegicus
|
0.43
nM
|
|
|
Inhibition of [3H]WIN-35428 binding to rat striatum DAT
|
Rattus norvegicus
|
8.56
nM
|
|
|
Inhibition of DAT-mediated [3H]DA uptake in rat striatum
|
Rattus norvegicus
|
10.6
nM
|
|
|
Inhibition of SERT-mediated [3H]5-HT uptake in rat cerebral cortex
|
Rattus norvegicus
|
91.1
nM
|
|
|
Inhibition of NET-mediated [3H]NE uptake in rat cerebral cortex
|
Rattus norvegicus
|
102.0
nM
|
|
|
Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat striatum
|
Rattus norvegicus
|
21.1
nM
|
|
|
Displacement of [125I]RTI55 from DAT in rat brain synaptosomes
|
Rattus norvegicus
|
3.7
nM
|
|
|
Displacement of [125I]RTI55 from SERT in rat brain synaptosomes
|
Rattus norvegicus
|
126.0
nM
|
|
|
Displacement of [3H]WIN-from DAT in rat striatum
|
Rattus norvegicus
|
10.2
nM
|
|
|
Inhibition of [3H]dopamine uptake in DAT in rat striatum
|
Rattus norvegicus
|
10.6
nM
|
|
|
Inhibition of [3H]5HT uptake in SERT in rat cerebral cortex
|
Rattus norvegicus
|
91.1
nM
|
|
|
Inhibition of [3H]NE uptake in NET in rat cerebral cortex
|
Rattus norvegicus
|
102.0
nM
|
|
|
Inhibition of human DAT
|
Homo sapiens
|
27.0
nM
|
|
|
Displacement of [3H]WIN-35428 from DAT in rat striatum membrane
|
Rattus norvegicus
|
1.77
nM
|
|
|
Displacement of [3H]citalopram from SERT in rat brain stem membrane
|
Rattus norvegicus
|
104.0
nM
|
|
|
Displacement of [3H]nisoxetine from NET in rat frontal cortex membrane
|
Rattus norvegicus
|
497.0
nM
|
|
|
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane
|
Cavia porcellus
|
50.8
nM
|
|
|
Displacement of [125I]RTI55 from DAT
|
None
|
3.7
nM
|
|
|
Displacement of [125I]RTI55 from SERT
|
None
|
130.0
nM
|
|
|
Inhibition of [3H]dopamine reuptake at dopamine transporter
|
None
|
5.07
nM
|
|
|
Inhibition of [3H]DA uptake at DAT in rat brain striatal synaptosomes by liquid scintillation spectrophotometry
|
Rattus norvegicus
|
18.0
nM
|
|
|
Inhibition of human dopamine transporter
|
Homo sapiens
|
7.2
nM
|
|
|
Displacement of [3H]-WIN 35,428 from DAT in rabbit striatal membrane
|
Oryctolagus cuniculus
|
1.5
nM
|
|
|
Displacement of [3H]WIN35428 from DAT after 1.5 hrs by scintillation counting
|
None
|
22.0
nM
|
|
|
Inhibition of human SERT expressed in HEK293 cells at 0.1 uM incubated for 15 mins by neurotransmitter reuptake assay
|
Homo sapiens
|
2.0
%
|
|
|
Inhibition of human NET expressed in HEK293 cells at 0.1 uM incubated for 15 mins by neurotransmitter reuptake assay
|
Homo sapiens
|
-6.0
%
|
|
|
Inhibition of human DAT expressed in HEK293 cells at 0.1 uM incubated for 15 mins by neurotransmitter reuptake assay
|
Homo sapiens
|
29.0
%
|
|
|
Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
|
Homo sapiens
|
190.0
nM
|
|
|
Displacement of [3H]paroxetine from mouse SERT in whole brain membrane
|
Mus musculus
|
24.1
nM
|
|
|
Displacement of [3H]RTI-121 from mouse DAT in striatal membranes
|
Mus musculus
|
12.0
nM
|
|
|
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
|
Cavia porcellus
|
320.0
nM
|
|
|
Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method
|
Homo sapiens
|
110.0
nM
|
|
|
Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by microbeta liquid scintillation counting method
|
Homo sapiens
|
43.0
nM
|
|
|
Inhibition of re-uptake of [3H]-NE at human NET expressed in HEK293 cells by liquid scintillation counting
|
Homo sapiens
|
110.0
nM
|
|
|
Inhibition of re-uptake of [3H]-DA at human DAT expressed in HEK293 cells by liquid scintillation counting
|
Homo sapiens
|
40.0
nM
|
|
|
Displacement of [125I]RTI-55 from recombinant human DAT expressed in CHOK1 cells after 3 hrs by scintillation counting method
|
Homo sapiens
|
0.71
nM
|
|
|
Displacement of [3H]-WIN35428 from human DAT expressed in HEK293 cells measured after 30 mins
|
Homo sapiens
|
8.8
nM
|
|
|
Displacement of [3H]-WIN35428 from human DAT expressed in HEK293 cells at 10 uM measured after 30 mins
|
Homo sapiens
|
50.0
%
|
|
|
Displacement of [3H]-WIN35428 from human DAT expressed in HEK cell membrane assessed as inhibition constant by radioligand binding assay
|
Homo sapiens
|
4.7
nM
|
|
