Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00011

Target Information
NameDopamine D1 receptor    
Type of targetSuccessful target    
SynonymsD(1) dopamine receptor    
D(1A) dopamine receptor    
DiseaseParkinson's disease    [1]
MethylergonovineApprovedExcessive bleeding[3]
PergolideApprovedParkinson's disease[4]
D1 agonist D2 antagonistPreclinicalSchizophrenia[5]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Gap junction
Neuroactive ligand-receptor interaction
UniProt IDP21728
PDB Structure1OZ5.    
FunctionThis is one of the five types (D1 to D5) of receptors for dopamine, and the activity of this receptor is mediated by g proteins which activate adenylyl cyclase.    
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+)-[6]
(R,S)-homoaromaline hydrochloride[6]
(S,S)-oxandrine hydrochloride[6]
1,2-Bis-[R- (-)-apomorphine-2'-oxy]ethane[15]
1- (4-[16]
1-Aminomethyl-isochroman-5,6-diol,   hydrobromide[18]
1-Benzyl-4- (2-ethynyl-pyrrol-1-yl)-piperidine[19]
1-Benzyl-4- (2-iodo-pyrrol-1-yl)-piperidine[19]
1-Benzyl-4- (2-oxazol-5-yl-pyrrol-1-yl)-piperidine[19]
1-[2- (2-Benzyl-phenoxy)-ethyl]-piperidine[21]
1-[2- (2-Benzyl-phenoxy)-ethyl]-pyrrolidine[21]
1-[3- (2-Benzyl-phenoxy)-propyl]-pyrrolidine[21]
2-{[R- (-)-Apomorphine-2'-oxy]ethoxy}-ethanol[15]
3- (1-Propyl-piperidin-3-yl)-phenol[25]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[26]
4-[2- (2-Benzyl-phenoxy)-ethyl]-morpholine[21]
5- (2-Amino-ethyl)-2-chloro-phenol,   hydrobromide[27]
6- (2-Amino-ethyl)-biphenyl-2,3,4'-triol[28]
6- (2-Amino-ethyl)-biphenyl-2,3-diol[28]
6- (2-Dipropylamino-ethyl)-biphenyl-2,3,4'-triol[28]
6- (2-Dipropylamino-ethyl)-biphenyl-2,3-diol[28]
LE 300[39]
N- (4-Dipropylaminobutyl)-4-biphenylcarboxamide[41]
N- (4-Propylaminobutyl)-4-biphenylcarboxamide[41]
SK&F-38393,   SK&F-383933,   SK-38393,   SK-383933[18]
SK&F-89626,   SK-89626[47]
TEPA (possesses cytotoxic activity)[48]
[R- (-)-Apomorphine-2-yl]-[15]
AgonistD1 agonist D2 antagonist[5]
SKF 38393[50][51]
MultitargetD1 agonist D2 antagonist[5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Locomotor behavior of dopamine D1 receptor transgenic/D2 receptor deficient hybrid mice. Brain Res. 2001 Jun 29;905(1-2):142-51. To Reference
Ref 2Etiology of iodinated radiocontrast nephrotoxicity and its attenuation by beraprost. Yakugaku Zasshi. 2008 Jul;128(7):1023-9. To Reference
Ref 3Reinforcement in an in vitro analog of appetitive classical conditioning of feeding behavior in Aplysia: blockade by a dopamine antagonist. Learn Mem. 2005 May-Jun;12(3):216-20. To Reference
Ref 4Dopamine and cognitive functioning in de novo subjects with Parkinson's disease: effects of pramipexole and pergolide on working memory. Neuropsychologia. 2009 Apr;47(5):1374-81. Epub 2009 Feb 7. To Reference
Ref 5The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 6J. Nat. Prod. 55(9):1281-1286 (1992) To Reference
Ref 7J Med Chem. 2000 May 18;43(10):2079-81.7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists. To Reference
Ref 8Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. To Reference
Ref 9J Nat Prod. 1998 Jun 26;61(6):709-12.Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine. To Reference
Ref 10Bioorg Med Chem Lett. 2007 Aug 1;17(15):4128-30. Epub 2007 May 23.R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands. To Reference
Ref 11J Med Chem. 2008 Feb 28;51(4):983-7. Epub 2008 Feb 6.Synthesis and dopamine receptor affinities of N-alkyl-11-hydroxy-2-methoxynoraporphines: N-alkyl substituents determine D1 versus D2 receptor selectivity. To Reference
Ref 12Bioorg Med Chem. 2008 Jul 15;16(14):6675-81. Epub 2008 Jun 5.Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines. To Reference
Ref 13J Med Chem. 2007 Jan 25;50(2):171-81.Advances in development of dopaminergic aporphinoids. To Reference
Ref 14J Med Chem. 1990 Jun;33(6):1800-5.Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogues. To Reference
Ref 15Bioorg Med Chem. 2008 Apr 15;16(8):4563-8. Epub 2008 Feb 15.Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines. To Reference
Ref 16Bioorg Med Chem Lett. 2006 Jun 1;16(11):2955-9. Epub 2006 Mar 24.Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. To Reference
Ref 17J Med Chem. 1991 Oct;34(10):2946-53.Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands. To Reference
Ref 18J Med Chem. 1990 Nov;33(11):2948-50.(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist. To Reference
Ref 19Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. To Reference
Ref 20J Med Chem. 1982 Jul;25(7):855-8.Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. To Reference
Ref 21J Med Chem. 2004 Aug 12;47(17):4155-8.Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity. To Reference
Ref 22Bioorg Med Chem. 2008 Sep 15;16(18):8335-8. Epub 2008 Aug 28.N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands. To Reference
Ref 23J Med Chem. 1981 Sep;24(9):1107-10.Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists. To Reference
Ref 24J Nat Prod. 2000 Apr;63(4):480-4.Halogenated boldine derivatives with enhanced monoamine receptor selectivity. To Reference
Ref 25J Med Chem. 1988 Aug;31(8):1621-5.Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. To Reference
Ref 26J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 27J Med Chem. 1992 Nov 13;35(23):4408-14.Synthesis and pharmacological characterization of 2-(4-chloro-3-hydroxyphenyl)ethylamine and N,N-dialkyl derivatives as dopamine receptor ligands. To Reference
Ref 28J Med Chem. 1986 Oct;29(10):1904-12.Synthesis and dopaminergic binding of 2-aryldopamine analogues: phenethylamines, 3-benzazepines, and 9-(aminomethyl)fluorenes. To Reference
Ref 29Bioorg Med Chem Lett. 2004 Dec 6;14(23):5813-6.Design, synthesis, and evaluation of hexahydrobenz[f]isoquinolines as a novel class of dopamine 3 receptor ligands. To Reference
Ref 30Bioorg Med Chem. 2009 Oct 1;17(19):6898-907. Epub 2009 Aug 20.Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities? To Reference
Ref 31J Med Chem. 1989 Aug;32(8):1913-21.Synthesis and receptor affinities of some conformationally restricted analogues of the dopamine D1 selective ligand (5R)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl- 1H-3-benzazepin-7-ol. To Reference
Ref 32Bioorg Med Chem. 2008 Mar 15;16(6):3218-23. Epub 2007 Dec 31.Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors. To Reference
Ref 33J Med Chem. 1982 Oct;25(10):1133-40.Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. To Reference
Ref 34J Med Chem. 1980 Jun;23(6):635-43.Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. To Reference
Ref 35Bioorg Med Chem. 2007 Nov 1;15(21):6819-29. Epub 2007 Aug 19.In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors. To Reference
Ref 36J Med Chem. 1997 Dec 5;40(25):4146-53.Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. To Reference
Ref 37J Med Chem. 1981 Sep;24(9):1021-6.Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. To Reference
Ref 38Bioorg Med Chem. 2009 Jul 1;17(13):4448-58. Epub 2009 May 12.Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. To Reference
Ref 39Bioorg Med Chem Lett. 2007 Mar 1;17(5):1399-402. Epub 2006 Dec 3.Dopamine/serotonin receptor ligands. Part 15: Oxygenation of the benz-indolo-azecine LE 300 leads to novel subnanomolar dopamine D1/D5 antagonists. To Reference
Ref 40Bioorg Med Chem Lett. 2009 Jan 1;19(1):51-3. Epub 2008 Nov 13.Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines. To Reference
Ref 41J Med Chem. 2008 Nov 13;51(21):6829-38. Epub 2008 Oct 4.Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. To Reference
Ref 42J Med Chem. 2005 Sep 8;48(18):5771-9.Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. To Reference
Ref 43J Med Chem. 1995 Jan 20;38(2):318-27.Evaluation of cis- and trans-9- and 11-hydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridines as structurally rigid, selective D1 dopamine receptor ligands. To Reference
Ref 44Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. Epub 2007 Nov 17.Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. To Reference
Ref 45J Med Chem. 1998 Nov 5;41(23):4486-91.Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes. To Reference
Ref 46J Med Chem. 1988 Oct;31(10):1941-6.Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as dopamine receptor ligands. To Reference
Ref 47J Med Chem. 1990 Jun;33(6):1756-64.trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist. To Reference
Ref 48J Med Chem. 1998 Oct 8;41(21):4165-70.N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies. To Reference
Ref 49J Med Chem. 2006 Nov 16;49(23):6848-57.trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist. To Reference
Ref 50Involvement of dopamine receptors of different types in formation of latent inhibition of passive avoidance reaction in Wistar rats. Zh Vyssh Nerv Deiat Im I P Pavlova. 2009 Mar-Apr;59(2):185-91. To Reference
Ref 51Effect of dopamine receptor agonists on sensory nerve activity: possible therapeutic targets for the treatment of asthma and COPD. Br J Pharmacol. 2002 Jun;136(4):620-8. To Reference
Ref 52Dopamine modulates effort-based decision making in rats. Behav Neurosci. 2009 Apr;123(2):242-51. To Reference


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