Page last updated: 2024-08-07 16:11:11
D(4) dopamine receptor
A D(4) dopamine receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P21917]
Synonyms
D(2C) dopamine receptor;
Dopamine D4 receptor
Research
Bioassay Publications (195)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 4 (2.05) | 18.7374 |
| 1990's | 33 (16.92) | 18.2507 |
| 2000's | 91 (46.67) | 29.6817 |
| 2010's | 56 (28.72) | 24.3611 |
| 2020's | 11 (5.64) | 2.80 |
Compounds (146)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 2-(n-phenethyl-n-propyl)amino-5-hydroxytetralin | Homo sapiens (human) | Ki | 0.0540 | 1 | 1 |
| 3-[(4-chlorophenyl)-phenylmethoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| amiodarone | Homo sapiens (human) | IC50 | 17.7200 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 6.2130 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.0340 | 1 | 1 |
| astemizole | Homo sapiens (human) | IC50 | 6.0870 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 2.1340 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 1.3650 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.1414 | 3 | 3 |
| clebopride | Homo sapiens (human) | Ki | 0.0032 | 1 | 1 |
| clotrimazole | Homo sapiens (human) | IC50 | 19.9190 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 6.9850 | 1 | 0 |
| disulfiram | Homo sapiens (human) | IC50 | 3.1500 | 1 | 0 |
| disulfiram | Homo sapiens (human) | Ki | 1.1050 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 1.2996 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 0.4557 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 9.3280 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 3.2710 | 1 | 0 |
| fentanyl | Homo sapiens (human) | Ki | 0.5540 | 1 | 1 |
| fluphenazine | Homo sapiens (human) | IC50 | 5.8770 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 2.0610 | 1 | 0 |
| haloperidol | Homo sapiens (human) | IC50 | 0.0978 | 6 | 5 |
| haloperidol | Homo sapiens (human) | Ki | 0.0135 | 41 | 41 |
| isoproterenol | Homo sapiens (human) | Ki | 2.9000 | 1 | 1 |
| jl 18 | Homo sapiens (human) | Ki | 0.0360 | 1 | 1 |
| ketanserin | Homo sapiens (human) | Ki | 0.0035 | 1 | 1 |
| loperamide | Homo sapiens (human) | Ki | 1.8500 | 1 | 1 |
| loxapine | Homo sapiens (human) | IC50 | 0.0140 | 1 | 1 |
| loxapine | Homo sapiens (human) | Ki | 0.0063 | 3 | 3 |
| methadone | Homo sapiens (human) | Ki | 26.2000 | 1 | 1 |
| mianserin | Homo sapiens (human) | IC50 | 3.3113 | 2 | 2 |
| miconazole | Homo sapiens (human) | IC50 | 15.2700 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 5.3540 | 1 | 0 |
| mirtazapine | Homo sapiens (human) | Ki | 0.0250 | 1 | 1 |
| modafinil | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| mosapramine | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| nemonapride | Homo sapiens (human) | IC50 | 0.0982 | 1 | 1 |
| nemonapride | Homo sapiens (human) | Ki | 0.0008 | 2 | 2 |
| prazosin | Homo sapiens (human) | Ki | 8.3000 | 1 | 1 |
| prochlorperazine | Homo sapiens (human) | IC50 | 2.3110 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.8100 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 1.6000 | 4 | 4 |
| rbi 257 | Homo sapiens (human) | Ki | 0.0003 | 2 | 2 |
| risperidone | Homo sapiens (human) | Ki | 0.0106 | 6 | 6 |
| 3-(3-cyanophenyl)-n-n-propylpiperidine | Homo sapiens (human) | Ki | 0.9330 | 1 | 1 |
| spiperone | Homo sapiens (human) | IC50 | 0.0005 | 1 | 1 |
| spiperone | Homo sapiens (human) | Ki | 0.0006 | 5 | 5 |
| sulpiride | Homo sapiens (human) | Ki | 2.1000 | 1 | 1 |
| thioridazine | Homo sapiens (human) | IC50 | 1.4680 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.5150 | 1 | 0 |
| n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
| zotepine | Homo sapiens (human) | Ki | 0.0390 | 2 | 2 |
| lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.0560 | 1 | 1 |
| apomorphine | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| apomorphine | Homo sapiens (human) | Ki | 0.0089 | 1 | 1 |
| phenyltoloxamine | Homo sapiens (human) | Ki | 2.7650 | 1 | 1 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| normethadone | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| azaperone | Homo sapiens (human) | Ki | 0.0065 | 2 | 4 |
| 11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Homo sapiens (human) | Ki | 0.4200 | 1 | 1 |
| 2-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
| 2-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
| benperidol | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| canadine, (s)-isomer | Homo sapiens (human) | Ki | 0.4860 | 1 | 1 |
| 1-(3-chloro-5-benzo[b][1]benzoxepinyl)-4-methylpiperazine | Homo sapiens (human) | Ki | 0.0005 | 2 | 2 |
| penfluridol | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| butaclamol | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
| haloperidol decanoate | Homo sapiens (human) | Ki | 0.0058 | 1 | 1 |
| remoxipride | Homo sapiens (human) | IC50 | 3.8720 | 1 | 1 |
| remoxipride | Homo sapiens (human) | Ki | 3.8720 | 1 | 1 |
| quinpirole | Homo sapiens (human) | Ki | 0.0180 | 12 | 12 |
| preclamol | Homo sapiens (human) | Ki | 0.5650 | 1 | 2 |
| ipsapirone | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
| eticlopride | Homo sapiens (human) | Ki | 0.0704 | 1 | 1 |
| n 0437, (-)-isomer | Homo sapiens (human) | Ki | 0.0550 | 1 | 1 |
| sertindole | Homo sapiens (human) | Ki | 0.0160 | 2 | 2 |
| fananserin | Homo sapiens (human) | Ki | 0.0029 | 2 | 2 |
| aripiprazole | Homo sapiens (human) | Ki | 0.1576 | 11 | 12 |
| ziprasidone | Homo sapiens (human) | Ki | 0.0400 | 4 | 4 |
| dopamine hydrochloride | Homo sapiens (human) | Ki | 0.0204 | 1 | 2 |
| mezilamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| tetrahydropalmatine | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| tandospirone | Homo sapiens (human) | Ki | 0.0072 | 1 | 1 |
| way 100635 | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
| gr 127935 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| ecopipam | Homo sapiens (human) | Ki | 5.5175 | 2 | 2 |
| 3-iodo-2-hydroxy-6-methoxy-n-((1-ethyl-2-pyrrolidinyl)methyl)benzamide | Homo sapiens (human) | Ki | 0.5700 | 1 | 1 |
| pramipexole | Homo sapiens (human) | Ki | 0.0457 | 8 | 10 |
| aj 76 | Homo sapiens (human) | Ki | 0.1170 | 1 | 1 |
| 1,2,3,6-tetrahydro-4-phenyl-1-((3-phenyl-3-cyclohexen-1-yl)methyl)pyridine | Homo sapiens (human) | Ki | 0.0909 | 2 | 2 |
| n 0734 | Homo sapiens (human) | Ki | 0.0720 | 1 | 1 |
| l 741742 | Homo sapiens (human) | Ki | 0.0033 | 5 | 5 |
| sonepiprazole | Homo sapiens (human) | Ki | 0.0052 | 2 | 2 |
| l 741626 | Homo sapiens (human) | Ki | 0.9619 | 5 | 5 |
| chloroethylnorapomorphine | Homo sapiens (human) | IC50 | 8.0000 | 1 | 1 |
| harmalan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| corydalmine | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 0.2620 | 1 | 1 |
| ngd 94-1 | Homo sapiens (human) | Ki | 0.0037 | 2 | 2 |
| roxindole | Homo sapiens (human) | Ki | 0.0240 | 1 | 1 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| tetrahydrocolumbamine | Homo sapiens (human) | Ki | 0.0774 | 1 | 1 |
| sb 243213 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| levosulpiride | Homo sapiens (human) | Ki | 2.1000 | 2 | 2 |
| tamoxifen | Homo sapiens (human) | IC50 | 11.1610 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 3.9130 | 1 | 0 |
| raclopride | Homo sapiens (human) | Ki | 3.1000 | 1 | 1 |
| bp 897 | Homo sapiens (human) | Ki | 0.1055 | 4 | 4 |
| n-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| n-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide | Homo sapiens (human) | Ki | 0.0000 | 2 | 2 |
| pd 168,077 | Homo sapiens (human) | Ki | 0.0091 | 5 | 5 |
| le 300 | Homo sapiens (human) | Ki | 0.1080 | 1 | 1 |
| abt724 | Homo sapiens (human) | Ki | 0.0837 | 4 | 1 |
| quercetin | Homo sapiens (human) | Ki | 7.8460 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| preclamol | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
| l 745870 | Homo sapiens (human) | IC50 | 0.4785 | 5 | 5 |
| l 745870 | Homo sapiens (human) | Ki | 0.0008 | 17 | 17 |
| pd 128907 | Homo sapiens (human) | Ki | 0.0978 | 2 | 2 |
| sb 271046 | Homo sapiens (human) | Ki | 0.1300 | 1 | 1 |
| jl 13 compound | Homo sapiens (human) | Ki | 0.1090 | 1 | 1 |
| 7-hydroxy-2-n,n-dipropylaminotetralin, (r)-isomer | Homo sapiens (human) | Ki | 0.1100 | 1 | 1 |
| l 750667 | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| uh 232 | Homo sapiens (human) | Ki | 0.0480 | 1 | 1 |
| stepholidine | Homo sapiens (human) | Ki | 3.7480 | 1 | 1 |
| sarizotan | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| ms-245 | Homo sapiens (human) | Ki | 3.2000 | 1 | 1 |
| armodafinil | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| n-demethylloperamide | Homo sapiens (human) | Ki | 0.0011 | 1 | 1 |
| cp 293019 | Homo sapiens (human) | Ki | 0.0034 | 1 | 1 |
| f 13640 | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| slv 313 | Homo sapiens (human) | Ki | 0.0100 | 1 | 1 |
| fauc 346 | Homo sapiens (human) | Ki | 0.0898 | 4 | 4 |
| ngb 2904 | Homo sapiens (human) | Ki | 4.5567 | 3 | 3 |
| 4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 0.1017 | 3 | 5 |
| pnu 109291 | Homo sapiens (human) | Ki | 3.7040 | 2 | 2 |
| pnu 96415e | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 0.0110 | 1 | 1 |
| n-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide | Homo sapiens (human) | Ki | 1.3000 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | IC50 | 0.0618 | 2 | 2 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 0.0010 | 2 | 2 |
| fauc 365 | Homo sapiens (human) | Ki | 0.7979 | 10 | 10 |
| fauc 213 | Homo sapiens (human) | Ki | 0.0029 | 8 | 8 |
| way-208466 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| fauc 113 | Homo sapiens (human) | Ki | 0.0030 | 7 | 7 |
| desmethoxyfallypride | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| 2-(3',4',5',6'-tetrahydro-2'h-(2,4') bipyridinyl-1'-yl)-n-m-tolyl-acetamide | Homo sapiens (human) | IC50 | 0.1297 | 2 | 2 |
| 2-(3',4',5',6'-tetrahydro-2'h-(2,4') bipyridinyl-1'-yl)-n-m-tolyl-acetamide | Homo sapiens (human) | Ki | 0.0220 | 3 | 3 |
| cariprazine | Homo sapiens (human) | Ki | 0.3070 | 3 | 4 |
| 5-hydroxy-2-n,n-dipropylaminotetralin, (s)-isomer | Homo sapiens (human) | Ki | 0.0470 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| pg 01037 | Homo sapiens (human) | Ki | 0.4100 | 5 | 5 |
| le 404 | Homo sapiens (human) | Ki | 0.0113 | 1 | 1 |
| lassbio-579 | Homo sapiens (human) | Ki | 0.1750 | 2 | 2 |
| gsk598809 | Homo sapiens (human) | Ki | 35.6000 | 1 | 1 |
| octoclothepine, (s)-isomer | Homo sapiens (human) | Ki | 0.0015 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| clozapine | Homo sapiens (human) | IC50 | 0.0796 | 12 | 12 |
| clozapine | Homo sapiens (human) | Ki | 0.2028 | 51 | 51 |
| olanzapine | Homo sapiens (human) | IC50 | 0.1730 | 1 | 1 |
| olanzapine | Homo sapiens (human) | Ki | 0.0305 | 6 | 6 |
Drugs with Activation Measurements
Drugs with Other Measurements
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists.Journal of medicinal chemistry, , Volume: 24, Issue:6, 1981
[no title available],
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DJournal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Development of a bivalent dopamine D₂ receptor agonist.Journal of medicinal chemistry, , Nov-24, Volume: 54, Issue:22, 2011
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.European journal of medicinal chemistry, , Volume: 42, Issue:7, 2007
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 13, Issue:17, 2003
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.Bioorganic & medicinal chemistry letters, , May-20, Volume: 12, Issue:10, 2002
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).Journal of medicinal chemistry, , Dec-31, Volume: 41, Issue:27, 1998
2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors.Journal of medicinal chemistry, , Jan-03, Volume: 40, Issue:1, 1997
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.Journal of medicinal chemistry, , Oct-15, Volume: 36, Issue:21, 1993
Aporphines. 58. N-(2-chloroethyl) [8,9-2H]norapomorphine, an irreversible ligand for dopamine receptors: synthesis and application.Journal of medicinal chemistry, , Volume: 27, Issue:6, 1984
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists.Journal of medicinal chemistry, , Volume: 24, Issue:6, 1981
[no title available],
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.Journal of medicinal chemistry, , Aug-19, Volume: 37, Issue:17, 1994
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[no title available]Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
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[no title available]Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
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Functionally selective dopamine D₂, D₃ receptor partial agonists.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
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Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
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Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
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Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
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[no title available]Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
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[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
[no title available]Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
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Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
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Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
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Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
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Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine DJournal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Discovery of highly potent and selective D4 ligands by interactive SAR study.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 23, Issue:18, 2013
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.Bioorganic & medicinal chemistry letters, , Jan-04, Volume: 9, Issue:1, 1999
Dopamine DJournal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DJournal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Development of molecular tools based on the dopamine DBioorganic & medicinal chemistry, , 07-01, Volume: 25, Issue:13, 2017
Functionally selective dopamine D₂, D₃ receptor partial agonists.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.Journal of medicinal chemistry, , May-26, Volume: 54, Issue:10, 2011
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.European journal of medicinal chemistry, , Volume: 62, 2013
Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.European journal of medicinal chemistry, , Volume: 66, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.Bioorganic & medicinal chemistry letters, , Sep-04, Volume: 10, Issue:17, 2000
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.Journal of medicinal chemistry, , Jul-15, Volume: 42, Issue:14, 1999
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 9, Issue:21, 1999
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.Bioorganic & medicinal chemistry letters, , Jan-04, Volume: 9, Issue:1, 1999
2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.Bioorganic & medicinal chemistry letters, , Jul-19, Volume: 9, Issue:14, 1999
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).Journal of medicinal chemistry, , Dec-31, Volume: 41, Issue:27, 1998
2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors.Journal of medicinal chemistry, , Jan-03, Volume: 40, Issue:1, 1997
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.Journal of medicinal chemistry, , Aug-19, Volume: 37, Issue:17, 1994
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists.Journal of medicinal chemistry, , Volume: 24, Issue:6, 1981
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Enables
This protein enables 13 target(s):
| Target | Category | Definition |
|---|
| dopamine neurotransmitter receptor activity, coupled via Gi/Go | molecular function | Combining with the neurotransmitter dopamine and activating adenylate cyclase via coupling to Gi/Go to initiate a change in cell activity. [GOC:mah, ISBN:0953351033, IUPHAR_RECEPTOR:2254, IUPHAR_RECEPTOR:2256, IUPHAR_RECEPTOR:2258] |
| dopamine neurotransmitter receptor activity | molecular function | Combining with the neurotransmitter dopamine to initiate a change in cell activity. [GOC:PARL, IUPHAR_GPCR:1282, PMID:21711983] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| potassium channel regulator activity | molecular function | Binds to and modulates the activity of a potassium channel. [GOC:dos, GOC:mah] |
| SH3 domain binding | molecular function | Binding to a SH3 domain (Src homology 3) of a protein, small protein modules containing approximately 50 amino acid residues found in a great variety of intracellular or membrane-associated proteins. [GOC:go_curators, Pfam:PF00018] |
| dopamine binding | molecular function | Binding to dopamine, a catecholamine neurotransmitter formed by aromatic-L-amino-acid decarboxylase from 3,4-dihydroxy-L-phenylalanine. [ISBN:0198506732] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| epinephrine binding | molecular function | Binding to epinephrine, a hormone produced by the medulla of the adrenal glands that increases heart activity, improves the power and prolongs the action of muscles, and increases the rate and depth of breathing. It is synthesized by the methylation of norepinephrine. [GOC:ai] |
| norepinephrine binding | molecular function | Binding to norepinephrine, (3,4-dihydroxyphenyl-2-aminoethanol), a hormone secreted by the adrenal medulla and a neurotransmitter in the sympathetic peripheral nervous system and in some tracts of the CNS. It is also the biosynthetic precursor of epinephrine. [GOC:ai] |
| G protein-coupled serotonin receptor activity | molecular function | Combining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai] |
| neurotransmitter receptor activity | molecular function | Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
| serotonin binding | molecular function | Binding to serotonin (5-hydroxytryptamine), a monoamine neurotransmitter occurring in the peripheral and central nervous systems, also having hormonal properties. [GOC:ai] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| postsynapse | cellular component | The part of a synapse that is part of the post-synaptic cell. [GOC:dos] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
Involved In
This protein is involved in 28 target(s):
| Target | Category | Definition |
|---|
| behavioral fear response | biological process | An acute behavioral change resulting from a perceived external threat. [GOC:dph, PMID:9920659] |
| synaptic transmission, dopaminergic | biological process | The vesicular release of dopamine. from a presynapse, across a chemical synapse, the subsequent activation of dopamine receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos, GOC:dph] |
| response to amphetamine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an amphetamine stimulus. Amphetamines consist of a group of compounds related to alpha-methylphenethylamine. [GOC:dph, GOC:ef] |
| intracellular calcium ion homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah] |
| adenylate cyclase-inhibiting dopamine receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by dopamine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| dopamine receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a dopamine receptor binding to one of its physiological ligands. [GOC:mah, PMID:21711983] |
| adult locomotory behavior | biological process | Locomotory behavior in a fully developed and mature organism. [GOC:ai] |
| positive regulation of sodium:proton antiporter activity | biological process | Any process that activates or increases the activity of a sodium:hydrogen antiporter, which catalyzes the reaction: Na+(out) + H+(in) = Na+(in) + H+(out). [GOC:mah] |
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |
| response to histamine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a histamine stimulus. Histamine, the biogenic amine 2-(1H-imidazol-4-yl)ethanamine, is involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter. [GOC:BHF, GOC:mah, GOC:vk] |
| social behavior | biological process | Behavior directed towards society, or taking place between members of the same species. Occurs predominantly, or only, in individuals that are part of a group. [GOC:jh2, PMID:12848939, Wikipedia:Social_behavior] |
| regulation of dopamine metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways involving dopamine. [GOC:go_curators] |
| dopamine metabolic process | biological process | The chemical reactions and pathways involving dopamine, a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:jl, ISBN:0198506732] |
| fear response | biological process | The response of an organism to a perceived external threat. [GOC:go_curators] |
| regulation of circadian rhythm | biological process | Any process that modulates the frequency, rate or extent of a circadian rhythm. A circadian rhythm is a biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:dph, GOC:jl, GOC:tb] |
| positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
| behavioral response to cocaine | biological process | Any process that results in a change in the behavior of an organism as a result of a cocaine stimulus. [GOC:jid] |
| behavioral response to ethanol | biological process | Any process that results in a change in the behavior of an organism as a result of an ethanol stimulus. [GOC:jid] |
| rhythmic process | biological process | Any process pertinent to the generation and maintenance of rhythms in the physiology of an organism. [GOC:jid] |
| arachidonic acid secretion | biological process | The controlled release of arachidonic acid from a cell or a tissue. [GOC:ai] |
| negative regulation of protein secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the controlled release of a protein from a cell. [GOC:ai] |
| positive regulation of dopamine uptake involved in synaptic transmission | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of dopamine into a cell. [GOC:ai] |
| inhibitory postsynaptic potential | biological process | A process that causes a temporary decrease in postsynaptic membrane potential due to the flow of negatively charged ions into the postsynaptic cell. The flow of ions that causes an IPSP is an inhibitory postsynaptic current (IPSC) and makes it more difficult for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
| regulation of postsynaptic neurotransmitter receptor internalization | biological process | Any process that modulates the frequency, rate or extent of endocytosis of neurotransmitter receptor at the postsynapse. [GOC:ai] |
| negative regulation of voltage-gated calcium channel activity | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of voltage-gated calcium channel activity. [GOC:BHF, GOC:TermGenie] |
| adenylate cyclase-inhibiting serotonin receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by serotonin binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |