|
Compound was evaluated for the binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in cloned CHO cells
|
None
|
673.0
nM
|
|
|
Ability to bind at 5-hydroxytryptamine 1A receptor of rat hippocampus by displacing [3H]8-OH-DPAT
|
None
|
372.0
nM
|
|
|
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus
|
None
|
179.0
nM
|
|
|
Binding affinity against serotonin 5-hydroxytryptamine 2 receptor
|
None
|
3.311
nM
|
|
|
Ability to bind at 5-hydroxytryptamine 2 receptor of rat hippocampus by displacing [3H]spiperone
|
None
|
8.8
nM
|
|
|
In vitro binding affinity against rat 5-hydroxytryptamine 2 receptor.
|
None
|
3.3
nM
|
|
|
Binding affinity determined in radioreceptor binding assay by using [3H]ketanserin radioligand against 5-hydroxytryptamine 2 receptor
|
None
|
0.7
nM
|
|
|
Binding affinity towards human 5-hydroxytryptamine 6 receptor
|
None
|
4.0
nM
|
|
|
Binding affinity towards rat 5-hydroxytryptamine 7 receptor
|
None
|
21.0
nM
|
|
|
Inhibitory activity against Dopamine sensitive adenylate cyclase in rats
|
None
|
118.0
nM
|
|
|
The compound was tested for its binding affinity towards alpha-1 adrenergic receptor by displacing [3H]WB-4101 radioligand in rat cerebral cortexc
|
None
|
5.5
nM
|
|
|
Ability to bind at Alpha-1 adrenergic receptor by displacing [3H]WB-4101
|
None
|
31.0
nM
|
|
|
In vitro affinity for cortical alpha-1 adrenergic receptor labelled with [3H]WB-4101
|
None
|
31.0
nM
|
|
|
Compound was evaluated for the inhibition of [3H]haloperidol binding in calf brain homogenates
|
Bos taurus
|
10.0
nM
|
|
|
Inhibition of apomorphine induced emesis in dogs at 2 mg/kg of dose.
|
Canis lupus familiaris
|
22.2
%
|
|
|
Binding affinity against dopamine D2 receptor
|
None
|
1.995
nM
|
|
|
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
|
Rattus norvegicus
|
2.15
nM
|
|
|
Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone
|
None
|
40.0
nM
|
|
|
Ability to bind at dopamine receptor D2 of rat corpus striatum by displacing [3H]spiperone
|
None
|
40.0
nM
|
|
|
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
|
Rattus norvegicus
|
50.0
nM
|
|
|
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
|
None
|
35.0
nM
|
|
|
Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes.
|
None
|
80.0
nM
|
|
|
Compound was tested for inhibition of [3H]spiperone binding in membrane preparations obtained from calf caudate.
|
None
|
25.0
nM
|
|
|
Inhibition of binding of 1.6 nM [3H]haloperidol to dopamine receptor by 50%
|
Bos taurus
|
34.0
nM
|
|
|
Inhibition of [3H]haloperidol binding to Dopamine receptor in calf caudate nuclei.
|
None
|
34.0
nM
|
|
|
compound was tested for its ability to displace [3H]- spiroperidol from dopamine receptor.
|
None
|
25.0
nM
|
|
|
Ability to inhibit the binding of [3H]spiroperidol in rat striatal tissue
|
None
|
77.0
nM
|
|
|
Compound was tested for inhibition of [3H]spiperone binding in membrane preparations obtained from rat corpus striatum.
|
None
|
112.0
nM
|
|
|
Affinity for Dopamine receptors in the rat striatum using [3H]spiroperidol displacement.
|
None
|
51.0
nM
|
|
|
Ability to displace [3H]spiroperidol from labeled Dopamine receptor of corpus striatum
|
None
|
51.0
nM
|
|
|
Concentration inhibiting the specific binding of [3H]spiroperidol by 50%
|
None
|
31.0
nM
|
|
|
Concentration of compound for 50% displacement of [3H]spiperone from Dopamine receptor in rat brain
|
None
|
111.0
nM
|
|
|
Tested for displacement of rat caudate dopamine receptors by using [3H]apomorphine as radioligand
|
None
|
38.9
nM
|
|
|
Tested for displacement of rat caudate dopamine receptors by using [3H]spiperone as radioligand
|
None
|
9.88
nM
|
|
|
Displacement of [3H]spiroperidol from dopamine receptor of rat corpus striatum homogenate
|
Rattus norvegicus
|
51.0
nM
|
|
|
In vitro ability to displace [3H]spiroperidol from rat dopamine receptor
|
None
|
14.0
nM
|
|
|
Binding affinity against dopamine receptor D1
|
None
|
35.48
nM
|
|
|
In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue.
|
None
|
2.01
nM
|
|
|
Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells
|
Homo sapiens
|
3.0
nM
|
|
|
Inhibition of [3H]spiperone binding to Dopamine receptor D2 at 0.02 nM
|
Rattus norvegicus
|
4.97
nM
|
|
|
Compound was evaluated for binding affinity towards Dopamine receptor D2 in striatal membranes, using [3H]- spiperone as radioligand in the absence of sodium chloride
|
None
|
1.77
nM
|
|
|
Compound was evaluated for binding affinity towards Dopamine receptor D2 in striatal membranes, using [3H]- spiperone as radioligand in the presence of sodium chloride
|
None
|
2.19
nM
|
|
|
Compound was evaluated for the binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells
|
None
|
3.0
nM
|
|
|
Compound was tested for inhibitory activity against the binding of [3H]spiperone to Dopamine receptor D2 in rat striatal membranes
|
None
|
1.2
nM
|
|
|
In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone
|
None
|
10.0
nM
|
|
|
Inhibition of dopamine-stimulated adenylate cyclase obtained from rat corpus striatum was determined by the conversion of [32P]ATP to [32P]-cAMP
|
None
|
79.0
nM
|
|
|
Tested for Competitive binding inhibition of [3H]spiperone to Dopamine receptor D2 in rat striatal membrane.
|
None
|
50.0
nM
|
|
|
Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum
|
None
|
7.8
nM
|
|
|
In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 100 (uM) of Cell-free parasite Plasmodium yoelii
|
Plasmodium yoelii
|
100.0
%
|
|
|
In Vitro inhibition of Heme Oxygenase in Cell-free parasite Plasmodium yoelii at concentration 50 uM
|
Plasmodium yoelii
|
85.0
%
|
|
|
3,4 -Dihydroxy phenylacetic acid (DOPAC) levels in mouse brain at 10 mg/kg dose.
|
Mus musculus
|
232.0
%
|
|
|
The homovanillic acid (HVA)levels in mouse brain at 10 mg/kg of dose.
|
Mus musculus
|
203.0
%
|
|
|
The homovanillic acid (HVA)levels in mouse brain at 50 mg/kg of dose.
|
Mus musculus
|
304.0
%
|
|
|
3,4 -Dihydroxy phenylacetic acid (DOPAC) levels in mouse brain at 50 mg/kg dose.
|
Mus musculus
|
303.0
%
|
|
|
Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 15 mg/kg
|
Mus musculus
|
0.0
%
|
|
|
Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 50 mg/kg
|
Mus musculus
|
30.0
%
|
|
|
Antiexploratory activity (EXPL) of mice determined by an antimex activity meter, 10 mg/kg of dose was administered perorally
|
Mus musculus
|
46.3
%
|
|
|
Antiexploratory activity (EXPL) of mice determined by an antimex activity meter, 50 mg/kg of dose was administered perorally
|
Mus musculus
|
90.1
%
|
|
|
Inhibitory activity against tremorine-induced tremors, after 1 hour of peroral administration in mouse at dose 7.5 mg/kg
|
Mus musculus
|
0.0
%
|
|
|
Inhibitory activity against tremorine-induced tremors, after 5 hour of peroral administration in mouse at dose 7.5 mg/kg
|
Mus musculus
|
15.0
%
|
|
|
In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain.
|
None
|
60.7
nM
|
|
|
Binding affinity against muscarinic (M) receptor
|
None
|
60.26
nM
|
|
|
Binding affinity against PCP binding site associated with N-methyl-D-aspartate glutamate receptor from rat synaptic plasma membrane(SPM) determined using [3H]TCP as radioligand.
|
None
|
25.0
%
|
|
|
Inhibition of [3H]1 binding to dextromethorpin binding site of guinea pig microsomal pellet P3 N-methyl-D-aspartate glutamate receptor
|
Cavia porcellus
|
600.0
nM
|
|
|
High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model
|
None
|
600.0
nM
|
|
|
Tested for displacement of [3H]prazosin from Prazosin receptor site of calf cerebral cortex
|
Bos taurus
|
12.0
nM
|
|
|
Binding affinity against rat striatal membranes using [3H]spiroperidol as the radioligand after 2 hours of conditioned feeding
|
Rattus norvegicus
|
180.0
nM
|
|
|
Inhibition of [3H]spiroperidol binding to rat striatal membrane using 0.5 nM ligand.
|
Rattus norvegicus
|
51.0
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 10 uM
|
Cavia porcellus
|
72.2
%
|
|
|
Ability to displace [3H]haloperidol from rat striatal membranes, in order to measure its intrinsic affinity for the dopamine (DA) receptor
|
None
|
12.0
nM
|
|
|
Binding affinity for human 5-hydroxytryptamine 6 receptor
|
Homo sapiens
|
50.0
nM
|
|
|
Displacement of [3H]spiperone from dopamine D2-like receptor in porcine striata homogenate
|
Sus scrofa
|
8.0
nM
|
|
|
Antagonist activity at rat TRPV1 receptor expressed in CHO cells by Ca2+ uptake assay
|
Rattus norvegicus
|
520.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells
|
Homo sapiens
|
10.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells
|
Homo sapiens
|
1.585
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
|
Homo sapiens
|
25.12
nM
|
|
|
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells
|
Homo sapiens
|
6.31
nM
|
|
|
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
|
Homo sapiens
|
39.81
nM
|
|
|
Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells
|
Homo sapiens
|
39.81
nM
|
|
|
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
|
Homo sapiens
|
50.12
nM
|
|
|
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
|
Homo sapiens
|
31.62
nM
|
|
|
Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells
|
Homo sapiens
|
63.1
nM
|
|
|
Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells
|
Homo sapiens
|
125.89
nM
|
|
|
Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells
|
Homo sapiens
|
158.49
nM
|
|
|
Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex
|
Rattus norvegicus
|
1.585
nM
|
|
|
Displacement of [3H]RX 821002 from adrenergic alpha-2 receptor in rat cerebral cortex
|
Rattus norvegicus
|
501.19
nM
|
|
|
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
|
Cavia porcellus
|
50.12
nM
|
|
|
Inhibition of NorA pump-mediated ethidium bromide efflux in Staphylococcus aureus K1199B at 50 uM by fluorimetric analysis
|
Staphylococcus aureus
|
81.0
%
|
|
|
Inhibition of Trypanosoma cruzi recombinant trypanothione reductase at 12.2 uM
|
Trypanosoma cruzi
|
70.0
%
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
85.1
%
|
|
|
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
|
Homo sapiens
|
4.25
nM
|
|
|
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
|
Homo sapiens
|
96.0
nM
|
|
|
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
|
Homo sapiens
|
172.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells
|
Homo sapiens
|
4.06
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells
|
Homo sapiens
|
6.9
nM
|
|
|
Spasmolytic activity in guinea pig ileum assessed as inhibition of spontaneous contraction
|
Cavia porcellus
|
180.0
nM
|
|
|
Displacement of [3H]spiperone from D2 like receptor in pig striatal tissue by topcount scintillation counting
|
Sus scrofa
|
3.2
nM
|
|
|
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
|
Homo sapiens
|
52.0
nM
|
|
|
Inhibition of human aldehyde oxidase
|
Homo sapiens
|
570.0
nM
|
|
|
Inhibition of guinea pig aldehyde oxidase
|
Cavia porcellus
|
860.0
nM
|
|
|
Inhibition of NorA in Staphylococcus aureus 1199B assessed as reduction in ethidium bromide efflux at 50 uM by fluorimetry after 5 mins
|
Staphylococcus aureus
|
76.0
%
|
|
|
Displacement of [3H]spiperone from dopamine D2 like receptor in porcine striatal membranes after 30 mins by scintillation counting
|
Sus scrofa
|
8.0
nM
|
|
|
Displacement of [3H]-N-methylspiperone from dopamine D2-like receptor in pig striatal tissue homogenates after 30 mins by scintillation counting
|
Sus scrofa
|
2.67
nM
|
|
|
Displacement of [3H]mesulergine from 5-HT2C receptor after 1.5 hrs by scintillation counting
|
None
|
27.0
nM
|
|
|
Displacement of [3H]LSD from 5-HT7 receptor after 1.5 hrs by scintillation counting
|
None
|
27.0
nM
|
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
83.0
nM
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
20.0
nM
|
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
652.0
nM
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
232.0
nM
|
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
206.0
nM
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
44.0
nM
|
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
149.0
nM
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
21.0
nM
|
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
25.0
nM
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
18.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
3.851
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
1.1
nM
|
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
8.538
nM
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
3.456
nM
|
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
8.966
nM
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
4.963
nM
|
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
3.991
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
1.962
nM
|
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
352.0
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
132.0
nM
|
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
26.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
12.0
nM
|
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
374.0
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
54.0
nM
|
|
|
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
|
None
|
19.0
nM
|
|
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
|
None
|
19.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
126.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
80.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
5.235
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
2.742
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
57.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
26.0
nM
|
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
39.0
nM
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
21.0
nM
|
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
451.0
nM
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
189.0
nM
|
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
225.0
nM
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
112.0
nM
|
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
54.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
18.0
nM
|
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
12.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
4.205
nM
|
|
|
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
|
None
|
479.0
nM
|
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
None
|
17.0
nM
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
None
|
1.957
nM
|
|
|
Displacement of [3H]spiperone from dopamine D2-like receptor in porcine striatal homogenates after 30 mins by scintillation counting
|
Sus scrofa
|
7.6
nM
|
|
|
Binding affinity to human mBBr-labeled CaM M124C mutant by fluorescence spectroscopy
|
Homo sapiens
|
640.0
nM
|
|
|
Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 30 mins by scintillation counting
|
Homo sapiens
|
3.8
nM
|
|
|
Displacement of [3H]-N-methylspiperone from human dopamine D2long receptor expressed in HEK293 cells after 30 mins by scintillation counting
|
Homo sapiens
|
1.2
nM
|
|
|
Displacement of [3H]-N-methylspiperone from dopamine D2 like receptor in pig striatal homogenates after 30 mins by scintillation counting
|
Sus scrofa
|
4.1
nM
|
|
|
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
|
27.1
%
|
|
|
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
|
22.8
%
|
|
|
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
|
4.3
%
|
|
|
Displacement of [3H]alpha-BGT from nAChR in Torpedo nobiliana electric organs membranes at 1000 uM by scintillation counting method
|
Torpedo nobiliana
|
7.15
%
|
|
|
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
|
Homo sapiens
|
11.0
nM
|
|
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
|
Homo sapiens
|
10.72
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
99.49
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
97.66
%
|
|
|
Binding affinity to SERT (unknown origin) by radioligand binding assay
|
Homo sapiens
|
120.0
nM
|
|
|
Binding affinity to 5HT2A receptor (unknown origin) by radioligand binding assay
|
Homo sapiens
|
3.4
nM
|
|
|
Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay
|
Homo sapiens
|
12.0
nM
|
|
|
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
|
Homo sapiens
|
12.0
nM
|
|
|
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
|
Homo sapiens
|
31.62
nM
|
|
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
|
Homo sapiens
|
30.0
nM
|
|
|
Displacement of [3H]N-Methylspiperone from dopamine D3 receptor (unknown origin)
|
Homo sapiens
|
3.311
nM
|
|
Displacement of [3H]N-Methylspiperone from dopamine D3 receptor (unknown origin)
|
Homo sapiens
|
3.3
nM
|
|
|
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
|
Homo sapiens
|
60.26
nM
|
|
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
|
Homo sapiens
|
60.0
nM
|
|
|
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
|
Homo sapiens
|
120.23
nM
|
|
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
|
Homo sapiens
|
119.0
nM
|
|
|
Displacement of [3H]Mesulergine from 5-HT2C receptor (unknown origin)
|
Homo sapiens
|
30.2
nM
|
|
Displacement of [3H]Mesulergine from 5-HT2C receptor (unknown origin)
|
Homo sapiens
|
30.0
nM
|
|
|
Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin)
|
Homo sapiens
|
5.888
nM
|
|
Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin)
|
Homo sapiens
|
5.9
nM
|
|
|
Neuroleptic activity in STD-ddy mouse assessed as inhibition of locomotion at 100 mg/kg, po measured for 3 mins
|
Mus musculus
|
97.4
%
|
|
|
Neuroleptic activity in STD-ddy mouse assessed as inhibition of locomotion at 10 mg/kg, po measured for 3 mins
|
Mus musculus
|
67.6
%
|
|
|
Neuroleptic activity in Wistar HLA rat assessed as inhibition of methamphetamine-induced stereotyped behavior at 10 mg/kg, ip administered 20 mins before methamphetamine challenge measured every 30 mins for 3 hrs followed by every 1 hr for further 3 hrs
|
Rattus norvegicus
|
75.0
%
|
|
|
Displacement of [3H]-HALO from dopamine receptor in calf caudate membranes after 10 mins by liquid scintillation counting analysis
|
Bos taurus
|
34.0
nM
|
|
|
Neuroleptic activity in squirrel monkey assessed as inhibition of Sidman avoidance at 2.5 mg/kg, po measured for 4 hrs
|
Saimiri sciureus
|
11.0
%
|
|
|
Neuroleptic activity in squirrel monkey assessed as inhibition of Sidman avoidance at 5 mg/kg, po measured for 4 hrs
|
Saimiri sciureus
|
54.0
%
|
|
|
Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells
|
Homo sapiens
|
6.1
nM
|
|
|
Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method
|
Homo sapiens
|
1.0
nM
|
|
|
Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
|
Homo sapiens
|
1.0
nM
|
|
|
Competitive inhibition of human liver cytosolic aldehyde oxidase using DACA as substrate assessed as free enzyme by Lineweaver-Burk plot analysis
|
Homo sapiens
|
620.0
nM
|
|
|
Binding affinity to Wistar rat brain lipid by TRANSIL assay
|
Rattus norvegicus
|
184.0
nM
|
|
|
Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by PDSP assay
|
Homo sapiens
|
11.0
nM
|
|
|
Displacement of [3H]apomorphine from rat caudate dopamine receptor
|
Rattus norvegicus
|
67.3
nM
|
|
|
Antagonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as decrease in apomorphine-induced calcium mobilization preincubated for 30 mins followed by apomorphine challenge measured for 30 secs by aequorin-derived luminescence assay
|
Homo sapiens
|
3.0
nM
|
|
|
Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293T cell membranes by radioligand binding assay
|
Homo sapiens
|
7.6
nM
|
|
Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293T cell membranes by radioligand binding assay
|
Homo sapiens
|
14.79
nM
|
|
|
Displacement of [3H]-raclopride from human D2 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
|
Homo sapiens
|
1.8
nM
|
|
|
Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
|
Homo sapiens
|
1.8
nM
|
|
|
Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay
|
Chlorocebus sabaeus
|
26.52
ug.mL-1
|
|
|
Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
|
Homo sapiens
|
12.02
nM
|
|
|
Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
|
Homo sapiens
|
2.344
nM
|
|
