Target Validation Information
Target ID T02551
Target Name D(3) dopamine receptor
Target Type
Successful
Drug Potency against Target Ropinirole Drug Info Ki = 4.37 nM [552855]
(R)-2-(Benzylamino-methyl)-chroman-7-ol Drug Info Ki = 2.4 nM [526840]
BP-897 Drug Info Ki = 20.2 nM [531051]
SB-271046 Drug Info Ki = 1330 nM [529191]
STEPHOLIDINE Drug Info Ki = 30 nM [530374]
ISOLOXAPINE Drug Info IC50 = 2480 nM [533577]
Etoloxamine Drug Info Ki = 4667 nM [527160]
1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine Drug Info Ki = 2923 nM [527160]
(+)-3-(1-Propyl-piperidin-3-yl)-phenol Drug Info Ki = 132 nM [533938]
(-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile Drug Info Ki = 249 nM [533938]
D-315 Drug Info Ki = 1.77 nM [531014]
L-741626 Drug Info Ki = 104 nM
Azaperone Drug Info Ki = 53 nM [533796]
QUINPIROLE Drug Info Ki = 49 nM [530429]
(R)-(-)-2-Phenyl-apomorphine hydrochloride Drug Info Ki = 7.7 nM [529328]
MAZAPERTINE Drug Info Ki = 1.8 nM [533800]
(+/-)-7-hydroxy-2-(N,N-di-n-propylamino)tetralin Drug Info Ki = 6.19 nM [529836]
Pramipexole Drug Info Ki = 0.5 nM [537564]
FLUMEZAPINE Drug Info IC50 = 20 nM [533515]
BP4.879a Drug Info IC50 = 5 nM [552656]
D-189 Drug Info Ki = 46.7 nM [529420]
(4-Phenylethynyl-cyclohex-3-enyl)-dipropyl-amine Drug Info Ki = 3500 nM [525701]
A-690344 Drug Info Ki = 1.3 nM [527867]
A-437203 Drug Info Ki = 2.9 nM [527867]
D-264 Drug Info Ki = 0.92 nM [530117]
(2-Benzyl-phenyl)-(2-pyrrolidin-1-yl-ethyl)-amine Drug Info Ki = 4654 nM [527160]
3-(1-Propyl-pyrrolidin-3-yl)-phenol Drug Info Ki = 52 nM
(-)-5-hydroxy-2-(dipropylamino)tetralin Drug Info Ki = 1.36 nM [530606]
(R)-(-)-2-Methyl-apomorphine hydrochloride Drug Info Ki = 40.1 nM [529328]
PD-158771 Drug Info Ki = 13.7 nM [553267]
BTS-79018 Drug Info Ki = 1.6 nM [552197]
UH-232 Drug Info Ki = 4.2 nM
R-226161 Drug Info Ki = 375 nM [528772]
SPIPERONE Drug Info Ki = 0.25 nM [527420]
Sarizotan Drug Info IC50 = 0.1 nM [552854]
1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine Drug Info Ki = 770 nM [525629]
FLUTROLINE Drug Info IC50 = 14 nM [533512]
GR-218231 Drug Info Ki = 1.3 nM [529862]
PG-01037 Drug Info IC50 = 3 nM [528974]
D-220 Drug Info Ki = 7.1 nM [529420]
4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole Drug Info Ki = 95.3 nM [534802]
Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine Drug Info Ki = 8.8 nM [525599]
L-741742 Drug Info Ki = 770 nM [534132]
3-(4-Benzyl-piperazin-1-yl)-phenol Drug Info Ki = 28.9 nM [534802]
2-(4-Dipropylamino-cyclohexylidene)-malononitrile Drug Info Ki = 1600 nM [525701]
Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine Drug Info Ki = 19.5 nM [525599]
ISOCLOZAPINE Drug Info IC50 = 758 nM [533570]
3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole Drug Info Ki = 6700 nM [534131]
1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine Drug Info Ki = 7900 nM [525629]
3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole Drug Info Ki = 95 nM [534131]
N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide Drug Info Ki = 950 nM [529734]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info Ki = 35 nM
1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine Drug Info Ki = 1818 nM [527160]
4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one Drug Info Ki = 2.8 nM [525599]
(4-Dipropylamino-cyclohexylidene)-acetonitrile Drug Info Ki = 13000 nM [525701]
3-(2-Benzylamino-ethoxy)-phenol Drug Info Ki = 11 nM [525599]
4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole Drug Info Ki = 56 nM [534802]
4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole Drug Info Ki = 870.5 nM [534802]
1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine Drug Info Ki = 2100 nM [528099]
1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine Drug Info Ki = 6800 nM [525629]
D-210 Drug Info Ki = 5.09 nM [529420]
D-218 Drug Info Ki = 34.8 nM [529420]
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine Drug Info IC50 = 1500 nM [533570]
1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine Drug Info Ki = 7804 nM [527160]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
(+/-)-nantenine Drug Info Ki = 309 nM [530558]
D-192 Drug Info Ki = 254 nM [529420]
D-190 Drug Info Ki = 40.7 nM [529420]
D-219 Drug Info Ki = 1.82 nM [529420]
D-193 Drug Info Ki = 155 nM [529420]
D-203 Drug Info Ki = 12.4 nM [529420]
L-Carnitine Drug Info Ki = 8.72 nM [529027]
1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one Drug Info Ki = 195 nM [528904]
NLX-101 Drug Info Ki = 10000 nM [531174]
Sumanirole Drug Info Ki = 2333 nM [534334]
1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine Drug Info Ki = 2600 nM [525629]
4-(4-Benzyl-piperazin-1-yl)-1H-indole Drug Info Ki = 35.4 nM [534802]
D-366 Drug Info Ki = 0.57 nM [530606]
3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole Drug Info Ki = 280 nM [534131]
(4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine Drug Info Ki = 190 nM [529734]
N-(4-Propylaminobutyl)-4-biphenylcarboxamide Drug Info Ki = 11000 nM [529734]
[2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine Drug Info Ki = 67.2 nM [525599]
4-Dipropylamino-cyclohex-1-enecarbonitrile Drug Info Ki = 13000 nM [525701]
1-Benzyl-4-pyrrol-1-yl-piperidine Drug Info Ki = 15000 nM [525629]
(+)-BUTACLAMOL Drug Info IC50 = 6.6 nM [529789]
A-706149 Drug Info Ki = 0.8 nM [527843]
Action against Disease Model Pramipexole EC50 in terminally differentiated neuroblastoma SH-SY5Y: 64300nM [552462] Drug Info
References
Ref 552462Involvement of dopamine D(2)/D(3) receptors and BDNF in the neuroprotective effects of S32504 and pramipexole against 1-methyl-4-phenylpyridinium in terminally differentiated SH-SY5Y cells. Exp Neurol. 2004 Nov;190(1):157-70.
Ref 552855Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67.
Ref 526840J Med Chem. 2003 Oct 9;46(21):4377-92.Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.
Ref 531051Bioorg Med Chem Lett. 2010 Sep 1;20(17):5199-202. Epub 2010 Jul 6.Synthesis and in vitro binding studies of piperazine-alkyl-naphthamides: impact of homology and sulphonamide/carboxamide bioisosteric replacement on the affinity for 5-HT1A, alpha2A, D4.2, D3 and D2L receptors.
Ref 529191Bioorg 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.
Ref 530374Bioorg 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?.
Ref 533577J Med Chem. 1981 Sep;24(9):1021-6.Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.
Ref 527160J 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.
Ref 527160J 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.
Ref 533938J Med Chem. 1993 Oct 15;36(21):3188-96.Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
Ref 533938J Med Chem. 1993 Oct 15;36(21):3188-96.Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
Ref 531014Bioorg Med Chem. 2010 Aug 1;18(15):5661-74. Epub 2010 Jun 12.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 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol.
Ref 533796J Med Chem. 1993 Nov 26;36(24):3929-36.Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
Ref 530429J Med Chem. 2009 Nov 12;52(21):6860-70.1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands.
Ref 529328Bioorg Med Chem. 2008 Apr 1;16(7):3773-9. Epub 2008 Feb 5.Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines.
Ref 533800J Med Chem. 1994 Apr 15;37(8):1060-2.A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
Ref 529836J Med Chem. 2008 Dec 25;51(24):7806-19.Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: binding characterization at D2/D3 receptors and elucidation of a pharmacophore model.
Ref 537564Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
Ref 533515J Med Chem. 1982 Oct;25(10):1133-40.Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
Ref 5526565-HT3 receptors. Curr Pharm Des. 2006;12(28):3615-30.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 525701J Med Chem. 2000 Feb 24;43(4):756-62.Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.
Ref 527867Bioorg Med Chem Lett. 2006 Feb;16(3):490-4. Epub 2005 Nov 11.Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives.
Ref 527867Bioorg Med Chem Lett. 2006 Feb;16(3):490-4. Epub 2005 Nov 11.Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives.
Ref 530117Bioorg Med Chem. 2009 Jun 1;17(11):3923-33. Epub 2009 Apr 19.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-naphthalen-2-ol: effect on affinity and selectivity for dopamine D3 receptor.
Ref 527160J 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.
Ref 530606J Med Chem. 2010 Feb 11;53(3):1023-37.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 D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.
Ref 529328Bioorg Med Chem. 2008 Apr 1;16(7):3773-9. Epub 2008 Feb 5.Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines.
Ref 553267Aminopyrimidines with high affinity for both serotonin and dopamine receptors. J Med Chem. 1998 Feb 26;41(5):760-71.
Ref 552197N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. J Med Chem. 1999 Aug 26;42(17):3342-55.
Ref 528772Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Ref 527420J Med Chem. 2005 Feb 10;48(3):694-709.Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
Ref 5528545-HT1A receptor, an old target for new therapeutic agents. Curr Top Med Chem. 2008;8(12):1024-34.
Ref 525629Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.
Ref 533512J Med Chem. 1980 Jun;23(6):635-43.Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines.
Ref 529862Bioorg Med Chem. 2009 Jan 15;17(2):758-66. Epub 2008 Nov 24.Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.
Ref 528974J Med Chem. 2007 Aug 23;50(17):4135-46. Epub 2007 Aug 2.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.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 534802Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80.New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.
Ref 525599Bioorg Med Chem Lett. 1999 Sep 6;9(17):2593-8.New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.
Ref 534132J Med Chem. 1996 May 10;39(10):1943-5.5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
Ref 534802Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80.New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.
Ref 525701J Med Chem. 2000 Feb 24;43(4):756-62.Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.
Ref 525599Bioorg Med Chem Lett. 1999 Sep 6;9(17):2593-8.New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.
Ref 533570J 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.
Ref 534131J Med Chem. 1996 May 10;39(10):1941-2.3-((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.
Ref 525629Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.
Ref 534131J Med Chem. 1996 May 10;39(10):1941-2.3-((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.
Ref 529734J 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.
Ref 527160J 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.
Ref 525599Bioorg Med Chem Lett. 1999 Sep 6;9(17):2593-8.New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.
Ref 525701J Med Chem. 2000 Feb 24;43(4):756-62.Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.
Ref 525599Bioorg Med Chem Lett. 1999 Sep 6;9(17):2593-8.New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.
Ref 534802Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80.New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.
Ref 534802Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80.New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.
Ref 528099Bioorg 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.
Ref 525629Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 533570J 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.
Ref 527160J 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.
Ref 531079J 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.
Ref 530558Bioorg 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.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 529027Bioorg Med Chem. 2007 Dec 1;15(23):7258-73. Epub 2007 Aug 25.Hybrid approach for the design of highly affine and selective dopamine D(3) receptor ligands using privileged scaffolds of biogenic amineGPCR ligands.
Ref 528904Bioorg Med Chem. 2007 Sep 1;15(17):5811-8. Epub 2007 Jun 7.Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand.
Ref 531174J Med Chem. 2010 Oct 14;53(19):7167-79.Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
Ref 534334J Med Chem. 1997 Feb 28;40(5):639-46.Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.
Ref 525629Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.
Ref 534802Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80.New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.
Ref 530606J Med Chem. 2010 Feb 11;53(3):1023-37.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 D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.
Ref 534131J Med Chem. 1996 May 10;39(10):1941-2.3-((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.
Ref 529734J 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.
Ref 529734J 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.
Ref 525599Bioorg Med Chem Lett. 1999 Sep 6;9(17):2593-8.New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.
Ref 525701J Med Chem. 2000 Feb 24;43(4):756-62.Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.
Ref 525629Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.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.
Ref 527843Bioorg Med Chem Lett. 2006 Feb;16(3):658-62. Epub 2005 Nov 2.Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com.

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