Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT4C8EA)

• DTT Name: Dopamine D3 receptor (D3R)
• Synonyms: D(3) dopamine receptor
• Gene Name: DRD3
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: DRD3_HUMAN
• TTD ID: T02551
• Sequence:
  MASLSQLSSHLNYTCGAENSTGASQARPHAYYALSYCALILAIVFGNGLVCMAVLKERAL
  QTTTNYLVVSLAVADLLVATLVMPWVVYLEVTGGVWNFSRICCDVFVTLDVMMCTASILN
  LCAISIDRYTAVVMPVHYQHGTGQSSCRRVALMITAVWVLAFAVSCPLLFGFNTTGDPTV
  CSISNPDFVIYSSVVSFYLPFGVTVLVYARIYVVLKQRRRKRILTRQNSQCNSVRPGFPQ
  QTLSPDPAHLELKRYYSICQDTALGGPGFQERGGELKREEKTRNSLSPTIAPKLSLEVRK
  LSNGRLSTSLKLGPLQPRGVPLREKKATQMVAIVLGAFIVCWLPFFLTHVLNTHCQTCHV
  SPELYSATTWLGYVNSALNPVIYTTFNIEFRKAFLKILSC
• Function: Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Dopaminergic synapse (hsa04728)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Dopamine receptors (R-HSA-390651)

Molecular Interaction Atlas (MIA) of This DTT

3 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cariprazine	DMJYDVK	Bipolar disorder	6A60	Approved	[1]
Pramipexole	DMNMW9R	Parkinson disease	8A00.0	Approved	[2]
Ropinirole	DMA6S1D	Parkinson disease	8A00.0	Approved	[2]

8 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CM-2395	DMASPWR	Schizophrenia	6A20	Phase 3	[3]
P2B-001	DM9PVHX	Parkinson disease	8A00.0	Phase 3	[4]
GSK598809	DMGU05N	Drug abuse	6C4G.1Z	Phase 2	[5]
ONC201	DMM5SCF	Endometrial cancer	2C76	Phase 2	[6]
RP5063	DMKUE8O	Schizophrenia	6A20	Phase 2	[7]
TAK-906	DMBQD9H	Diabetic gastroparesis	DA41.00	Phase 2	[8]
GSK618334	DMJPXZ4	Drug abuse	6C4G.1Z	Phase 1	[5]
Pfizer 10	DM6ER9L	Female sexual arousal dysfunction	HA01.1	Phase 1	[9]

2 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aryl piperazine derivative 1	DM9DJGU	N. A.	N. A.	Patented	[10]
Aryl piperazine derivative 6	DMZ3DS5	N. A.	N. A.	Patented	[10]

16 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Quinelorane	DMO9XTJ	Male sexual disorder	HA02.0	Discontinued in Phase 3	[11]
A-437203	DMEG240	Psychotic disorder	6A20-6A25	Discontinued in Phase 2	[12]
BP-897	DMAQ6DS	Cocaine addiction	6C45.2	Discontinued in Phase 2	[13]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[14]
AVE-5997EF	DM5FDX2	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[15]
S-33138	DM1R8Z7	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[16]
AS-8112	DMIFDPL	Vomiting	MD90	Terminated	[20]
BP4.879a	DMN8FAG	Schizophrenia	6A20	Terminated	[15]
BTS-79018	DMAH3Z9	Schizophrenia	6A20	Terminated	[15]
E-2040	DMZWU8V	Schizophrenia	6A20	Terminated	[21]
GR-218231	DMIJCH1	N. A.	N. A.	Terminated	[22]
PNU-177864	DMRT69H	Schizophrenia	6A20	Terminated	[15]
PNU-96391A	DMLMISK	Substance use disorder	6C4Z	Terminated	[23]
RGH-1756	DM8RIA6	Schizophrenia	6A20	Terminated	[15]
SB-277011	DM3M16Q	Schizophrenia	6A20	Terminated	[15]
YM-43611	DMWI094	Psychotic disorder	6A20-6A25	Terminated	[24]

7 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
F-15063	DMUFP05	Schizophrenia	6A20	Preclinical	[17]
PD-157533	DMTG730	Schizophrenia	6A20	Preclinical	[15]
PD-157695	DMDSR1X	Schizophrenia	6A20	Preclinical	[15]
PD-158771	DM682UV	Schizophrenia	6A20	Preclinical	[15]
S-33084	DMWQ3TH	Psychotic disorder	6A20-6A25	Preclinical	[18]
S32504	DM4V8ZD	Parkinson disease	8A00.0	Preclinical	[19]
U-99194A	DMW87JR	Schizophrenia	6A20	Preclinical	[15]

86 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+)-AJ76	DMEDMC0	Discovery agent	N.A.	Investigative	[25]
(+)-BUTACLAMOL	DMX6UYN	Discovery agent	N.A.	Investigative	[26]
(+)-S-14297	DMX7ECD	Discovery agent	N.A.	Investigative	[27]
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[28]
(-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile	DME5TIR	Discovery agent	N.A.	Investigative	[29]
(2-Benzyl-phenyl)-(2-pyrrolidin-1-yl-ethyl)-amine	DMFRPGX	Discovery agent	N.A.	Investigative	[30]
(4-Dipropylamino-cyclohexylidene)-acetonitrile	DMRIWH2	Discovery agent	N.A.	Investigative	[31]
(4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine	DMHQCRU	Discovery agent	N.A.	Investigative	[32]
(4-Phenylethynyl-cyclohex-3-enyl)-dipropyl-amine	DMQM8O5	Discovery agent	N.A.	Investigative	[31]
(R)-(-)-2-Methyl-apomorphine hydrochloride	DMAYEJL	Discovery agent	N.A.	Investigative	[33]
(R)-(-)-2-Phenyl-apomorphine hydrochloride	DME62U0	Discovery agent	N.A.	Investigative	[33]
(R)-2-(Benzylamino-methyl)-chroman-7-ol	DMJVQN8	Discovery agent	N.A.	Investigative	[34]
1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine	DMUDVRM	Discovery agent	N.A.	Investigative	[35]
1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one	DMM18AQ	Discovery agent	N.A.	Investigative	[36]
1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine	DMF0GXD	Discovery agent	N.A.	Investigative	[37]
1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine	DMBRJ5S	Discovery agent	N.A.	Investigative	[37]
1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine	DMSBNY8	Discovery agent	N.A.	Investigative	[37]
1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine	DMCJZVA	Discovery agent	N.A.	Investigative	[37]
1-Benzyl-4-pyrrol-1-yl-piperidine	DMNWEC9	Discovery agent	N.A.	Investigative	[37]
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine	DMOL2Y0	Discovery agent	N.A.	Investigative	[38]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine	DMOCAUL	Discovery agent	N.A.	Investigative	[39]
1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine	DMTNRG7	Discovery agent	N.A.	Investigative	[30]
1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine	DMLSU30	Discovery agent	N.A.	Investigative	[30]
1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine	DMD2NXL	Discovery agent	N.A.	Investigative	[30]
2-(4-Dipropylamino-cyclohexylidene)-malononitrile	DMXH0FO	Discovery agent	N.A.	Investigative	[31]
3-(1-Propyl-pyrrolidin-3-yl)-phenol	DM4QRV9	Discovery agent	N.A.	Investigative	[39]
3-(2-Benzylamino-ethoxy)-phenol	DMZCTGF	Discovery agent	N.A.	Investigative	[40]
3-(4-Benzyl-piperazin-1-yl)-phenol	DMWPB0G	Discovery agent	N.A.	Investigative	[41]
3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole	DM0HYDZ	Discovery agent	N.A.	Investigative	[42]
3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole	DM17SNR	Discovery agent	N.A.	Investigative	[42]
3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole	DMM0WGI	Discovery agent	N.A.	Investigative	[42]
4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one	DMYVD2E	Discovery agent	N.A.	Investigative	[40]
4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole	DMXAEW9	Discovery agent	N.A.	Investigative	[41]
4-(4-Benzyl-piperazin-1-yl)-1H-indole	DMWR0AS	Discovery agent	N.A.	Investigative	[41]
4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole	DMZ4237	Discovery agent	N.A.	Investigative	[41]
4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole	DMVAB7U	Discovery agent	N.A.	Investigative	[41]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[43]
4-Dipropylamino-cyclohex-1-enecarbonitrile	DMKEHLD	Discovery agent	N.A.	Investigative	[31]
5-OH-DPAT	DMZT6JR	Discovery agent	N.A.	Investigative	[44]
7-trans-OH-PIPAT	DMOQMA0	Discovery agent	N.A.	Investigative	[45]
A-690344	DMT6A7G	Schizophrenia	6A20	Investigative	[46]
A-706149	DMXOPFU	Discovery agent	N.A.	Investigative	[47]
A-987306	DMU34BK	Discovery agent	N.A.	Investigative	[26]
AS-9705	DMR01O4	Gastric motility disorder	DA21	Investigative	[20]
Azaperone	DMKI2GJ	Discovery agent	N.A.	Investigative	[48]
Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine	DMTC4G0	Discovery agent	N.A.	Investigative	[40]
Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine	DMV6DY7	Discovery agent	N.A.	Investigative	[40]
D-189	DMU8BJH	Discovery agent	N.A.	Investigative	[49]
D-190	DMUMNSW	Discovery agent	N.A.	Investigative	[49]
D-192	DM8D26T	Discovery agent	N.A.	Investigative	[49]
D-193	DMU83T7	Discovery agent	N.A.	Investigative	[49]
D-203	DMKPIH0	Discovery agent	N.A.	Investigative	[49]
D-210	DMNLE4S	Discovery agent	N.A.	Investigative	[49]
D-218	DMQLT84	Discovery agent	N.A.	Investigative	[49]
D-219	DMQ2U4G	Discovery agent	N.A.	Investigative	[49]
D-220	DMTUJWN	Discovery agent	N.A.	Investigative	[49]
D-237	DMGA48T	Discovery agent	N.A.	Investigative	[50]
D-264	DMWLHBQ	Discovery agent	N.A.	Investigative	[51]
D-315	DMG1CD5	Discovery agent	N.A.	Investigative	[52]
D-366	DMZAM3G	Discovery agent	N.A.	Investigative	[44]
Etoloxamine	DMDOX1Z	Discovery agent	N.A.	Investigative	[30]
FLUMEZAPINE	DMW0HOG	Discovery agent	N.A.	Investigative	[53]
FLUTROLINE	DMUOHVL	Discovery agent	N.A.	Investigative	[54]
ISOCLOZAPINE	DM52CPU	Discovery agent	N.A.	Investigative	[38]
ISOLOXAPINE	DMH1BN4	Discovery agent	N.A.	Investigative	[55]
L-741626	DMCYQJF	Discovery agent	N.A.	Investigative	[56]
L-741742	DMP75YK	Discovery agent	N.A.	Investigative	[57]
N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide	DMU1ATH	Discovery agent	N.A.	Investigative	[32]
N-(4-Propylaminobutyl)-4-biphenylcarboxamide	DMG9D7A	Discovery agent	N.A.	Investigative	[32]
N-propylnorapomorphine	DMO7MTX	N. A.	N. A.	Investigative	[58]
nafadotride	DM79KLR	Discovery agent	N.A.	Investigative	[59]
NGB 2904	DMMC42Z	Discovery agent	N.A.	Investigative	[60]
PD 128907	DMYC51H	Discovery agent	N.A.	Investigative	[61]
PD-152255	DMV0EDM	Discovery agent	N.A.	Investigative	[62]
PF-592379	DMY93GJ	Discovery agent	N.A.	Investigative	[63]
PG-01037	DM2TP4Q	Discovery agent	N.A.	Investigative	[64]
piribedil	DMNP6QD	Discovery agent	N.A.	Investigative	[65]
QUINPIROLE	DMDNHEP	Discovery agent	N.A.	Investigative	[66]
R-226161	DM4BP7S	Discovery agent	N.A.	Investigative	[67]
SB-271046	DM5VJAF	Discovery agent	N.A.	Investigative	[68]
SB269652	DMEGNJK	Discovery agent	N.A.	Investigative	[69]
STEPHOLIDINE	DMGMXQC	Discovery agent	N.A.	Investigative	[70]
UH-232	DM5K6ZE	Discovery agent	N.A.	Investigative	[71]
[2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine	DMSPMHE	Discovery agent	N.A.	Investigative	[40]
[3H]7-OH-DPAT	DM2PW8T	Discovery agent	N.A.	Investigative	[72]
[3H]spiperone	DMWHEV8	Discovery agent	N.A.	Investigative	[73]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Parkinson's disease	8A00.0	Substantia nigra tissue	2.84E-03	0.13	2
Bipolar disorder	6A20	Pre-frontal cortex	1.88E-01	-0.03	-0.25
Schizophrenia	6A20	Pre-frontal cortex	5.74E-02	0.05	0.34
Schizophrenia	6A20	Superior temporal cortex	2.15E-01	-0.05	-0.46

References

• [1] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [3] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
• [4] Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51.
• [5] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK-906), a Novel Selective D 2 /D 3 Receptor Antagonist: A Phase 1 Randomized, Placebo-Controlled Single- and Multiple-Dose Escalation Study in Healthy Participants. Clin Pharmacol Drug Dev. 2021 Jan 18.
• [9] Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66.
• [10] 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
• [11] Quinelorane, a dopamine D3/D2 receptor agonist, reduces prepulse inhibition of startle and ventral pallidal GABA efflux: time course studies.Pharmacol Biochem Behav.2008 Oct;90(4):686-90.
• [12] Association of dopamine-related genetic loci to dopamine D3 receptor antagonist ABT-925 clinical response.Transl Psychiatry.2013 Apr 9;3:e245.
• [13] BP 897, a selective dopamine D3 receptor ligand with therapeutic potential for the treatment of cocaine-addiction.CNS Drug Rev.2003 Summer;9(2):141-58.
• [14] A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2.
• [15] The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
• [16] The dopamine D3 receptor antagonist, S33138, counters cognitive impairment in a range of rodent and primate procedures. Int J Neuropsychopharmacol. 2010 Sep;13(8):1035-51.
• [17] F15063, a potential antipsychotic with dopamine D(2)/D(3) antagonist, 5-HT(1A) agonist and D(4) partial agonist properties: (IV) duration of brain D2-like receptor occupancy and antipsychotic-like activity versus plasma concentration in mice.Naunyn Schmiedebergs Arch Pharmacol.2007 Jun;375(4):241-50.
• [18] S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: II. Functional and behavioral profile compared with GR218,231 and L741,626. J Pharmacol Exp Ther. 2000 Jun;293(3):1063-73.
• [19] S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: II. Actions in rodent, primate, and cellular models of antiparkinsonian activity ... J Pharmacol Exp Ther. 2004 Jun;309(3):921-35.
• [20] Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
• [21] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126)
• [22] Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of t... Bioorg Med Chem. 2009 Jan 15;17(2):758-66.
• [23] The dopamine stabilizer (-)-OSU6162 occupies a subpopulation of striatal dopamine D2/D3 receptors: an [(11)C]raclopride PET study in healthy human subjects. Neuropsychopharmacology. 2015 Jan;40(2):472-9.
• [24] Effects of YM-43611, a novel dopamine D2-like receptor antagonist, on immediate early gene expression in the rat forebrain. Neuropsychopharmacology. 1997 Jul;17(1):27-33.
• [25] Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature. 1990 Sep 13;347(6289):146-51.
• [26] 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... J Med Chem. 2008 Nov 27;51(22):7094-8.
• [27] S 14297, a novel selective ligand at cloned human dopamine D3 receptors, blocks 7-OH-DPAT-induced hypothermia in rats. Eur J Pharmacol. 1994 Aug 1;260(2-3):R3-5.
• [28] Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
• [29] Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. J Med Chem. 1993 Oct 15;36(21):3188-96.
• [30] Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8.
• [31] Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonis... J Med Chem. 2000 Feb 24;43(4):756-62.
• [32] Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. J Med Chem. 2008 Nov 13;51(21):6829-38.
• [33] Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines. Bioorg Med Chem. 2008 Apr 1;16(7):3773-9.
• [34] Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybri... J Med Chem. 2003 Oct 9;46(21):4377-92.
• [35] Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2955-9.
• [36] Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand. Bioorg Med Chem. 2007 Sep 1;15(17):5811-8.
• [37] Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.
• [38] Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1982 Jul;25(7):855-8.
• [39] Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity, Bioorg. Med. Chem. Lett. 7(3):241-246 (1997).
• [40] New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2593-8.
• [41] New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80.
• [42] 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... J Med Chem. 1996 May 10;39(10):1941-2.
• [43] 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
• [44] Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a... J Med Chem. 2010 Feb 11;53(3):1023-37.
• [45] Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors. J Med Chem. 1994 Nov 25;37(24):4245-50.
• [46] Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives. Bioorg Med Chem Lett. 2006 Feb;16(3):490-4.
• [47] Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.genes... Bioorg Med Chem Lett. 2006 Feb;16(3):658-62.
• [48] Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors. J Med Chem. 1993 Nov 26;36(24):3929-36.
• [49] Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly... J Med Chem. 2008 May 22;51(10):3005-19.
• [50] Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: binding character... J Med Chem. 2008 Dec 25;51(24):7806-19.
• [51] Investigation of various N-heterocyclic substituted piperazine versions of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-... Bioorg Med Chem. 2009 Jun 1;17(11):3923-33.
• [52] Further delineation of hydrophobic binding sites in dopamine D(2)/D(3) receptors for N-4 substituents on the piperazine ring of the hybrid template... Bioorg Med Chem. 2010 Aug 1;18(15):5661-74.
• [53] Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. J Med Chem. 1982 Oct;25(10):1133-40.
• [54] Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. J Med Chem. 1980 Jun;23(6):635-43.
• [55] Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1981 Sep;24(9):1021-6.
• [56] Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626. Bioorg Med Chem. 2010 Jul 15;18(14):5291-300.
• [57] 5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors. J Med Chem. 1996 May 10;39(10):1943-5.
• [58] A functional test identifies dopamine agonists selective for D3 versus D2 receptors. Neuroreport. 1995 Jan 26;6(2):329-32.
• [59] Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents. J Pharmacol Exp Ther. 1995 Dec;275(3):1239-46.
• [60] Pharmacological actions of NGB 2904, a selective dopamine D3 receptor antagonist, in animal models of drug addiction. CNS Drug Rev. 2007 Summer;13(2):240-59.
• [61] Neurochemical and functional characterization of the preferentially selective dopamine D3 agonist PD 128907. J Pharmacol Exp Ther. 1995 Dec;275(3):1355-66.
• [62] Pharmacological characterization of PD 152255, a novel dimeric benzimidazole dopamine D3 antagonist. Pharmacol Biochem Behav. 1998 Feb;59(2):487-93.
• [63] Lack of abuse potential in a highly selective dopamine D3 agonist, PF-592,379, in drug self-administration and drug discrimination in rats. Behav Pharmacol. 2012 Jun;23(3):280-91.
• [64] Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3... J Med Chem. 2007 Aug 23;50(17):4135-46.
• [65] Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804.
• [66] 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. J Med Chem. 2009 Nov 12;52(21):6860-70.
• [67] Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60.
• [68] Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43.
• [69] Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists. Eur Neuropsychopharmacol. 2015 Sep;25(9):1448-61.
• [70] Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities Bioorg Med Chem. 2009 Oct 1;17(19):6898-907.
• [71] (Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists, Bioorg. Med. Chem. Lett. 7(21):2759-2764 (1997).
• [72] Radioligand binding characterization of putative dopamine D3 receptor in human peripheral blood lymphocytes with [3H]7-OH-DPAT. J Neuroimmunol. 1995 May;58(2):139-44.
• [73] Regulation of human D(1), d(2(long)), d(2(short)), D(3) and D(4) dopamine receptors by amiloride and amiloride analogues. Br J Pharmacol. 2000 Jul;130(5):1045-59.