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D(4) dopamine receptor
A D(4) dopamine receptor that is encoded in the genome of rat. [OMA:P30729, PRO:DNx]
Synonyms
D(2C) dopamine receptor;
Dopamine D4 receptor
Research
Bioassay Publications (41)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 24 (58.54) | 18.7374 |
| 1990's | 5 (12.20) | 18.2507 |
| 2000's | 6 (14.63) | 29.6817 |
| 2010's | 6 (14.63) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (64)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| octoclothepine | Rattus norvegicus (Norway rat) | IC50 | 0.0030 | 1 | 3 |
| bmy 7378 | Rattus norvegicus (Norway rat) | IC50 | 0.0910 | 1 | 2 |
| buspirone | Rattus norvegicus (Norway rat) | IC50 | 0.1200 | 1 | 2 |
| chlorpromazine | Rattus norvegicus (Norway rat) | IC50 | 0.0416 | 7 | 12 |
| chlorpromazine | Rattus norvegicus (Norway rat) | Ki | 0.0140 | 1 | 1 |
| clonidine | Rattus norvegicus (Norway rat) | Ki | 4.0000 | 1 | 2 |
| cyproheptadine | Rattus norvegicus (Norway rat) | Ki | 0.0630 | 1 | 1 |
| adtn | Rattus norvegicus (Norway rat) | IC50 | 0.0024 | 2 | 2 |
| granisetron | Rattus norvegicus (Norway rat) | Ki | 0.0091 | 1 | 2 |
| haloperidol | Rattus norvegicus (Norway rat) | IC50 | 0.0067 | 4 | 5 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 0.0060 | 2 | 2 |
| imipramine | Rattus norvegicus (Norway rat) | IC50 | 0.8100 | 1 | 1 |
| jl 18 | Rattus norvegicus (Norway rat) | Ki | 0.0210 | 1 | 1 |
| metoclopramide | Rattus norvegicus (Norway rat) | Ki | 0.2291 | 1 | 2 |
| nomifensine | Rattus norvegicus (Norway rat) | IC50 | 2.7240 | 2 | 2 |
| ondansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| phenoxybenzamine | Rattus norvegicus (Norway rat) | Ki | 0.1200 | 1 | 2 |
| promazine | Rattus norvegicus (Norway rat) | IC50 | 1.0400 | 1 | 2 |
| quipazine | Rattus norvegicus (Norway rat) | Ki | 0.0010 | 1 | 2 |
| spiperone | Rattus norvegicus (Norway rat) | Ki | 0.0020 | 1 | 1 |
| sulpiride | Rattus norvegicus (Norway rat) | Ki | 1.6000 | 1 | 1 |
| thioridazine | Rattus norvegicus (Norway rat) | IC50 | 0.0850 | 1 | 2 |
| apomorphine | Rattus norvegicus (Norway rat) | IC50 | 0.1432 | 7 | 7 |
| yohimbine | Rattus norvegicus (Norway rat) | Ki | 2.0000 | 1 | 2 |
| apomorphine hydrochloride, anhydrous | Rattus norvegicus (Norway rat) | Ki | 0.0037 | 1 | 1 |
| apocodeine | Rattus norvegicus (Norway rat) | IC50 | 6.2000 | 2 | 2 |
| 2-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Rattus norvegicus (Norway rat) | IC50 | 0.7580 | 1 | 1 |
| pimozide | Rattus norvegicus (Norway rat) | IC50 | 0.0004 | 1 | 4 |
| bromocriptine | Rattus norvegicus (Norway rat) | IC50 | 0.0279 | 2 | 3 |
| penfluridol | Rattus norvegicus (Norway rat) | IC50 | 0.0620 | 1 | 2 |
| butaclamol | Rattus norvegicus (Norway rat) | IC50 | 0.0053 | 2 | 3 |
| butaclamol | Rattus norvegicus (Norway rat) | IC50 | 0.0020 | 1 | 2 |
| butaclamol | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 1 | 1 |
| pergolide | Rattus norvegicus (Norway rat) | IC50 | 0.0031 | 2 | 3 |
| flutroline | Rattus norvegicus (Norway rat) | IC50 | 0.0120 | 1 | 2 |
| gepirone | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 2 |
| aripiprazole | Rattus norvegicus (Norway rat) | Ki | 0.5100 | 1 | 1 |
| sertraline hydrochloride | Rattus norvegicus (Norway rat) | IC50 | 0.0700 | 1 | 1 |
| lerisetron | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 1 | 1 |
| sertraline | Rattus norvegicus (Norway rat) | IC50 | 0.2600 | 1 | 2 |
| mezilamine | Rattus norvegicus (Norway rat) | Ki | 0.0400 | 2 | 3 |
| 2-(n,n-dipropyl)amino-5,6-dihydroxytetralin | Rattus norvegicus (Norway rat) | IC50 | 0.1355 | 2 | 3 |
| sonepiprazole | Rattus norvegicus (Norway rat) | Ki | 0.0072 | 1 | 1 |
| sk&f-38393 | Rattus norvegicus (Norway rat) | IC50 | 34.4300 | 1 | 1 |
| dexmethylphenidate hydrochloride | Rattus norvegicus (Norway rat) | IC50 | 0.1235 | 2 | 2 |
| chloroethylnorapomorphine | Rattus norvegicus (Norway rat) | IC50 | 5.1970 | 2 | 2 |
| n-n-propylnorapomorphine | Rattus norvegicus (Norway rat) | IC50 | 0.2394 | 2 | 4 |
| preclamol | Rattus norvegicus (Norway rat) | IC50 | 0.9300 | 1 | 1 |
| tropisetron | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 1 | 2 |
| n-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 1 | 1 |
| flupenthixol | Rattus norvegicus (Norway rat) | IC50 | 0.0030 | 1 | 3 |
| l 745870 | Rattus norvegicus (Norway rat) | Ki | 0.0021 | 2 | 2 |
| fluvoxamine | Rattus norvegicus (Norway rat) | IC50 | 0.5400 | 1 | 1 |
| zimeldine | Rattus norvegicus (Norway rat) | IC50 | 4.5000 | 1 | 1 |
| morphine chloride | Rattus norvegicus (Norway rat) | IC50 | 0.0340 | 2 | 4 |
| (8R)-7-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,13,14-triol | Rattus norvegicus (Norway rat) | IC50 | 2.2050 | 2 | 2 |
| (8R)-7-propyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,13,14-triol | Rattus norvegicus (Norway rat) | IC50 | 0.3125 | 2 | 2 |
| dihydrexidine | Rattus norvegicus (Norway rat) | Ki | 0.0130 | 1 | 1 |
| cilansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| vilazodone | Rattus norvegicus (Norway rat) | IC50 | 3.4000 | 1 | 1 |
| pnu 96415e | Rattus norvegicus (Norway rat) | Ki | 0.0030 | 1 | 1 |
| 11-hydroxy-n-(n-propyl)noraporphine hydrochloride, (r)-isomer | Rattus norvegicus (Norway rat) | IC50 | 0.3680 | 2 | 2 |
| 11-hydroxy-n-(n-propyl)noraporphine hydrochloride, (r)-isomer | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 1 | 1 |
| fauc 113 | Rattus norvegicus (Norway rat) | Ki | 0.0028 | 2 | 2 |
| clozapine | Rattus norvegicus (Norway rat) | IC50 | 0.9312 | 5 | 7 |
| clozapine | Rattus norvegicus (Norway rat) | Ki | 0.0975 | 4 | 4 |
| olanzapine | Rattus norvegicus (Norway rat) | Ki | 0.0500 | 1 | 1 |
| flumezapine | Rattus norvegicus (Norway rat) | IC50 | 0.0200 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| apomorphine | Rattus norvegicus (Norway rat) | EC50 | 0.0042 | 3 | 3 |
| abt724 | Rattus norvegicus (Norway rat) | EC50 | 0.0171 | 3 | 3 |
Azaphenothiazines - promising phenothiazine derivatives. An insight into nomenclature, synthesis, structure elucidation and biological properties.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Neuroleptics from the 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 3. Carboxamidoalkyl derivatives.Journal of medicinal chemistry, , Volume: 29, Issue:10, 1986
Design, synthesis, and X-ray data of novel potential antipsychotic agents. Substituted 7-phenylquinolizidines: stereospecific, neuroleptic, and antinociceptive properties.Journal of medicinal chemistry, , Volume: 27, Issue:2, 1984
Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans.Journal of medicinal chemistry, , Volume: 26, Issue:7, 1983
Preparation of some 10-[3-(dimethylamino)-1-propyl]-10H-pyrazino[2,3-b][1,4] benzothiazines as potential neuroleptics.Journal of medicinal chemistry, , Volume: 26, Issue:4, 1983
2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
Conformationally restricted phenothiazine neuroleptics. 1. 3-(Dimethylamino)-1,2,3,4-tetrahydroazepino[3,2,1-kl]phenothiazine.Journal of medicinal chemistry, , Volume: 23, Issue:8, 1980
Further evaluation of the tropane analogs of haloperidol.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.Journal of medicinal chemistry, , Volume: 29, Issue:1, 1986
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.Journal of medicinal chemistry, , Volume: 28, Issue:12, 1985
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.Journal of medicinal chemistry, , Volume: 26, Issue:2, 1983
2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.Journal of medicinal chemistry, , Volume: 25, Issue:10, 1982
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
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines.Journal of medicinal chemistry, , Volume: 31, Issue:8, 1988
Dopamine autoreceptor agonists: resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analogue of apomorphine.Journal of medicinal chemistry, , Volume: 30, Issue:3, 1987
Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists.Journal of medicinal chemistry, , Volume: 27, Issue:12, 1984
Synthesis and dopaminergic properties of some exo- and endo-2-aminobenzonorbornenes designed as rigid analogue of dopamine.Journal of medicinal chemistry, , Volume: 25, Issue:4, 1982
Aporphines, 36. Dopamine receptor interactions of trihydroxyaporphines. Synthesis, radioreceptor binding, and striatal adenylate cyclase stimulation of 2,10,11-trihydroxyaporphines in comparison with other hydroxylated aporphines.Journal of medicinal chemistry, , Volume: 24, Issue:12, 1981
Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists.Journal of medicinal chemistry, , Volume: 27, Issue:12, 1984
Synthesis of (7R)-7H-indolo[3,4-gh][1,4]benzoxazines, a new class of D-heteroergolines with dopamine agonist activity.Journal of medicinal chemistry, , Volume: 26, Issue:3, 1983
Neuroleptics from the 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 3. Carboxamidoalkyl derivatives.Journal of medicinal chemistry, , Volume: 29, Issue:10, 1986
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.Journal of medicinal chemistry, , Volume: 26, Issue:2, 1983
Design, synthesis, and X-ray data of novel potential antipsychotic agents. Substituted 7-phenylquinolizidines: stereospecific, neuroleptic, and antinociceptive properties.Journal of medicinal chemistry, , Volume: 27, Issue:2, 1984
Synthesis and receptor binding studies relevant to the neuroleptic activities of some 1-methyl-4-piperidylidene-9-substituted-pyrrolo[2,1-b][3]benzazepine derivatives.Journal of medicinal chemistry, , Volume: 26, Issue:7, 1983
Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists.Journal of medicinal chemistry, , Volume: 27, Issue:12, 1984
Synthesis of (7R)-7H-indolo[3,4-gh][1,4]benzoxazines, a new class of D-heteroergolines with dopamine agonist activity.Journal of medicinal chemistry, , Volume: 26, Issue:3, 1983
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
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
Identification of a new selective dopamine D4 receptor ligand.Bioorganic & medicinal chemistry, , Jun-15, Volume: 22, Issue:12, 2014
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine.Journal of medicinal chemistry, , Volume: 31, Issue:7, 1988
Aporphines, 36. Dopamine receptor interactions of trihydroxyaporphines. Synthesis, radioreceptor binding, and striatal adenylate cyclase stimulation of 2,10,11-trihydroxyaporphines in comparison with other hydroxylated aporphines.Journal of medicinal chemistry, , Volume: 24, Issue:12, 1981
Identification of a new selective dopamine D4 receptor ligand.Bioorganic & medicinal chemistry, , Jun-15, Volume: 22, Issue:12, 2014
Evaluation of 18F-labeled benzodioxine piperazine-based dopamine D4 receptor ligands: lipophilicity as a determinate of nonspecific binding.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.Journal of medicinal chemistry, , Volume: 28, Issue:12, 1985
1-[3-(Diarylamino)propyl]piperidines and related compounds, potential antipsychotic agents with low cataleptogenic profiles.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.Journal of medicinal chemistry, , Volume: 26, Issue:2, 1983
2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding.Journal of medicinal chemistry, , Volume: 25, Issue:12, 1982
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.Journal of medicinal chemistry, , Volume: 25, Issue:10, 1982
Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.Journal of medicinal chemistry, , Volume: 24, Issue:9, 1981