Detailed Information (TTD) -- BIDD

TTD Target ID: TTDS00011

Target Information
Name	Dopamine D1 receptor
Type of target	Successful target
Synonyms	D(1) dopamine receptor
	D(1A) dopamine receptor
Disease	Parkinson's disease [1]
Drug(s)	Fenoldopam		Approved	Hypertension	[2]
	Methylergonovine		Approved	Excessive bleeding	[3]
	Pergolide		Approved	Parkinson's disease	[4]
	BSF-78438		Preclinical	Schizophrenia	[5]
	D1 agonist D2 antagonist		Preclinical	Schizophrenia	[5]
BioChemical Class	G-protein coupled receptor (rhodopsin family)
Pathway	Calcium signaling pathway
	Gap junction
	Neuroactive ligand-receptor interaction
UniProt ID	P21728
PDB Structure	1OZ5.
Function	This 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.
Sequence	MRTLNTSAMDGTGLVVERDFSVRILTACFLSLLILSTLLGNTLVCAAVIRFRHLRSKVTN FFVISLAVSDLLVAVLVMPWKAVAEIAGFWPFGSFCNIWVAFDIMCSTASILNLCVISVD RYWAISSPFRYERKMTPKAAFILISVAWTLSVLISFIPVQLSWHKAKPTSPSDGNATSLA ETIDNCDSSLSRTYAISSSVISFYIPVAIMIVTYTRIYRIAQKQIRRIAALERAAVHAKN CQTTTGNGKPVECSQPESSFKMSFKRETKVLKTLSVIMGVFVCCWLPFFILNCILPFCGS GETQPFCIDSNTFDVFVWFGWANSSLNPIIYAFNADFRKAFSTLLGCYRLCPATNNAIET VSINNNGAAMFSSHHEPRGSISKECNLVYLIPHAVGSSEDLKKEEAAGIARPLEKLSPAL SVILDYDTDVSLEKIQPITQNGQHPT
Target Validation	Click to Find Target Validation Information.
Inhibitor	(+)-		[6]
	(+)-		[6]
	(+)-BUTACLAMOL		[7]
	(+/-)-nantenine		[8]
	(-)-		[6]
	(R)-		[9]
	(R)-		[10]
	(R)-		[11]
	(R)-		[11]
	(R)-		[11]
	(R)-		[11]
	(R)-		[11]
	(R)-11-Amino-2-methoxyaporphine		[12]
	(R)-2,11-Diaminoaporphine		[12]
	(R,S)-homoaromaline hydrochloride		[6]
	(S)-BULBOCAPNINE		[13]
	(S)APOMORPHINE		[14]
	(S,S)-oxandrine hydrochloride		[6]
	1,2,3,7,12,12a-hexahydro-1-aza-pleiaden-5-ol		[13]
	1,2,3,7,12,12a-hexahydro-1-aza-pleiadene-5,6-diol		[13]
	1,2-Bis-[R- (-)-apomorphine-2'-oxy]ethane		[15]
	1- (4-		[16]
	1-Aminomethyl-3-cyclohexyl-isochroman-5,6-diol		[17]
	1-Aminomethyl-3-phenyl-isochroman-5,6-diol		[18]
	1-Aminomethyl-isochroman-5,6-diol		[18]
	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-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine		[20]
	1-[2- (2-Benzyl-phenoxy)-ethyl]-piperidine		[21]
	1-[2- (2-Benzyl-phenoxy)-ethyl]-pyrrolidine		[21]
	1-[3- (2-Benzyl-phenoxy)-propyl]-pyrrolidine		[21]
	11-Butyryloxy-N-n-propylnoraporphine		[22]
	11-Heptanoyloxy-N-n-propylnoraporphine		[22]
	11-Hexanoyloxy-N-n-propylnoraporphine		[22]
	11-Propionyloxy-N-n-propylnoraporphine		[22]
	11-valeryloxynoraporphine		[22]
	2-Methyl-8-phenyl-1,2,3,4-tetrahydro-isoquinoline		[23]
	2-methoxyapomorphine		[15]
	2-{[R- (-)-Apomorphine-2'-oxy]ethoxy}-ethanol		[15]
	3,8-dibromoboldine		[24]
	3- (1-Propyl-piperidin-3-yl)-phenol		[25]
	3-Chloroboldine		[24]
	3-Iodoboldine		[24]
	3-bromoboldine		[24]
	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]
	9-Aminomethyl-9H-fluorene-2,5,6-triol		[28]
	9-Aminomethyl-9H-fluorene-3,4-diol		[28]
	A-70108		[18]
	BOLDINE		[24]
	BP-897		[29]
	DIHYDREXIDINE		[30]
	Ecopipam		[31]
	Etoloxamine		[21]
	FALCARINDIOL		[32]
	FLUMEZAPINE		[33]
	FLUTROLINE		[34]
GLAUCINE		[13]
IBZM		[35]
ISOCLOZAPINE		[36]
ISOLOXAPINE		[37]
L-745870		[38]
LE 300		[39]
MCL-516		[40]
MELOSMINE		[13]
N- (4-Dipropylaminobutyl)-4-biphenylcarboxamide		[41]
N- (4-Propylaminobutyl)-4-biphenylcarboxamide		[41]
NORSTEPHALAGINE		[13]
PREDICENTRINE		[13]
PUKATEINE		[13]
Phenyltoloxamine		[21]
QUINPIROLE		[42]
R-N-PROPYLNORAPOMORPHINE		[11]
Ro-21-7767		[43]
SB-271046		[44]
SCH-12679		[45]
SCH-24518		[46]
SK&F-38393, SK&F-383933, SK-38393, SK-383933		[18]
SK&F-89626, SK-89626		[47]
STEPHOLIDINE		[30]
TEPA (possesses cytotoxic activity)		[48]
[R- (-)-Apomorphine-2-yl]-		[15]
dihydrexidine		[49]
Agonist	D1 agonist D2 antagonist		[5]
	Fenoldopam		[2]
	Pergolide		[4]
	SKF 38393		[50][51]
Antagonist	Methylergonovine		[3]
	SCH-23390		[52]
Binder	BSF-78438		[5]
Multitarget	D1 agonist D2 antagonist		[5]
	Pergolide		[4]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
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Ref 2	Etiology of iodinated radiocontrast nephrotoxicity and its attenuation by beraprost. Yakugaku Zasshi. 2008 Jul;128(7):1023-9. To Reference
Ref 3	Reinforcement 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 4	Dopamine 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 5	The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
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Ref 8	Bioorg 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 9	J Nat Prod. 1998 Jun 26;61(6):709-12.Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine. To Reference
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Ref 11	J 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
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Ref 14	J 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 15	Bioorg Med Chem. 2008 Apr 15;16(8):4563-8. Epub 2008 Feb 15.Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines. To Reference
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Ref 17	J 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 18	J 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
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Ref 20	J 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
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Ref 27	J 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 28	J 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 29	Bioorg 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
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Ref 31	J 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 32	Bioorg 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 33	J 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 34	J Med Chem. 1980 Jun;23(6):635-43.Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. To Reference
Ref 35	Bioorg 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 36	J 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 37	J 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 38	Bioorg 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 39	Bioorg 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
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Ref 41	J 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 42	J 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 43	J 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
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