Target Information

Target General Information

Top

Target ID

T02551 (Former ID: TTDS00013)

Target Name

Dopamine D3 receptor (D3R)

Synonyms

D(3) dopamine receptor

Gene Name

DRD3

Target Type

Successful target

[1]

Disease

[+] 2 Target-related Diseases

Bipolar disorder [ICD-11: 6A60]

Parkinsonism [ICD-11: 8A00]

Function

Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.

Click to Show/Hide

BioChemical Class

GPCR rhodopsin

UniProt ID

DRD3_HUMAN

Sequence

MASLSQLSSHLNYTCGAENSTGASQARPHAYYALSYCALILAIVFGNGLVCMAVLKERAL
QTTTNYLVVSLAVADLLVATLVMPWVVYLEVTGGVWNFSRICCDVFVTLDVMMCTASILN
LCAISIDRYTAVVMPVHYQHGTGQSSCRRVALMITAVWVLAFAVSCPLLFGFNTTGDPTV
CSISNPDFVIYSSVVSFYLPFGVTVLVYARIYVVLKQRRRKRILTRQNSQCNSVRPGFPQ
QTLSPDPAHLELKRYYSICQDTALGGPGFQERGGELKREEKTRNSLSPTIAPKLSLEVRK
LSNGRLSTSLKLGPLQPRGVPLREKKATQMVAIVLGAFIVCWLPFFLTHVLNTHCQTCHV
SPELYSATTWLGYVNSALNPVIYTTFNIEFRKAFLKILSC

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

ADReCS ID

BADD_A04234

HIT2.0 ID

T43Y5O

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 3 Approved Drugs

Cariprazine

Drug Info

Approved

Bipolar disorder

[1], [2]

Pramipexole

Drug Info

Approved

Parkinson disease

[3], [4]

Ropinirole

Drug Info

Approved

Parkinson disease

[5], [6]

Clinical Trial Drug(s)

[+] 8 Clinical Trial Drugs

CM-2395

Drug Info

Phase 3

Schizophrenia

[7]

P2B-001

Drug Info

Phase 3

Parkinson disease

[8]

GSK598809

Drug Info

Phase 2

Drug abuse

[9]

ONC201

Drug Info

Phase 2

Glioma

[8], [10]

RP5063

Drug Info

Phase 2

Schizophrenia

[11]

TAK-906

Drug Info

Phase 2

Diabetic gastroparesis

[12]

GSK618334

Drug Info

Phase 1

Drug abuse

[13]

Pfizer 10

Drug Info

Phase 1

Female sexual arousal dysfunction

[14]

Discontinued Drug(s)

[+] 15 Discontinued Drugs

Quinelorane

Drug Info

Discontinued in Phase 3

Male sexual disorder

[15], [16]

A-437203

Drug Info

Discontinued in Phase 2

Psychotic disorder

[17]

BP-897

Drug Info

Discontinued in Phase 2

Cocaine addiction

[18], [19]

AVE-5997EF

Drug Info

Discontinued in Phase 1

Psychotic disorder

[20]

S-33138

Drug Info

Discontinued in Phase 1

Psychotic disorder

[21]

AS-8112

Drug Info

Terminated

Vomiting

[27]

BP4.879a

Drug Info

Terminated

Schizophrenia

[23]

BTS-79018

Drug Info

Terminated

Schizophrenia

[23]

Dianicline+rimonabant

Drug Info

Terminated

Tobacco dependence

[28]

E-2040

Drug Info

Terminated

Schizophrenia

[29]

PNU-177864

Drug Info

Terminated

Schizophrenia

[23]

PNU-96391A

Drug Info

Terminated

Substance use disorder

[30]

RGH-1756

Drug Info

Terminated

Schizophrenia

[23]

SB-277011

Drug Info

Terminated

Schizophrenia

[23], [31]

YM-43611

Drug Info

Terminated

Psychotic disorder

[32]

Preclinical Drug(s)

[+] 7 Preclinical Drugs

F-15063

Drug Info

Preclinical

Schizophrenia

[22]

PD-157533

Drug Info

Preclinical

Schizophrenia

[23]

PD-157695

Drug Info

Preclinical

Schizophrenia

[23]

PD-158771

Drug Info

Preclinical

Schizophrenia

[23]

S-33084

Drug Info

Preclinical

Psychotic disorder

[24], [25]

S32504

Drug Info

Preclinical

Parkinson disease

[26]

U-99194A

Drug Info

Preclinical

Schizophrenia

[23]

Mode of Action

[+] 8 Modes of Action

Modulator

[+] 13 Modulator drugs

Cariprazine

Drug Info

[1]

Pramipexole

Drug Info

[33]

Ropinirole

Drug Info

[33]

Quinelorane

Drug Info

[40]

A-437203

Drug Info

[41]

BP-897

Drug Info

[42]

F-15063

Drug Info

[46]

S-33084

Drug Info

[47]

S32504

Drug Info

[26]

E-2040

Drug Info

[50]

PNU-96391A

Drug Info

[30]

YM-43611

Drug Info

[52]

PD-152255

Drug Info

[91]

Agonist

[+] 8 Agonist drugs

CM-2395

Drug Info

[34]

Pfizer 10

Drug Info

[14]

7-trans-OH-PIPAT

Drug Info

[73]

N-propylnorapomorphine

Drug Info

[86]

PD 128907

Drug Info

[89], [90]

PF-592379

Drug Info

[92]

piribedil

Drug Info

[94]

[3H]7-OH-DPAT

Drug Info

[78], [101], [102]

Inhibitor

[+] 76 Inhibitor drugs

P2B-001

Drug Info

[35]

TAK-906

Drug Info

[38]

MAZAPERTINE

Drug Info

[43]

GR-218231

Drug Info

[51]

(+)-BUTACLAMOL

Drug Info

[54]

(+/-)-nantenine

Drug Info

[56]

(-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile

Drug Info

[57]

(2-Benzyl-phenyl)-(2-pyrrolidin-1-yl-ethyl)-amine

Drug Info

[58]

(4-Dipropylamino-cyclohexylidene)-acetonitrile

Drug Info

[59]

(4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine

Drug Info

[60]

(4-Phenylethynyl-cyclohex-3-enyl)-dipropyl-amine

Drug Info

[59]

(R)-(-)-2-Methyl-apomorphine hydrochloride

Drug Info

[61]

(R)-(-)-2-Phenyl-apomorphine hydrochloride

Drug Info

[61]

(R)-2-(Benzylamino-methyl)-chroman-7-ol

Drug Info

[62]

1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine

Drug Info

[63]

1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one

Drug Info

[64]

1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine

Drug Info

[65]

1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine

Drug Info

[65]

1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine

Drug Info

[65]

1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine

Drug Info

[65]

1-Benzyl-4-pyrrol-1-yl-piperidine

Drug Info

[65]

1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine

Drug Info

[66]

1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine

Drug Info

[67]

1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine

Drug Info

[58]

1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine

Drug Info

[58]

1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine

Drug Info

[58]

2-(4-Dipropylamino-cyclohexylidene)-malononitrile

Drug Info

[59]

3-(1-Propyl-pyrrolidin-3-yl)-phenol

Drug Info

[67]

3-(2-Benzylamino-ethoxy)-phenol

Drug Info

[68]

3-(4-Benzyl-piperazin-1-yl)-phenol

Drug Info

[69]

3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole

Drug Info

[70]

3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole

Drug Info

[70]

3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole

Drug Info

[70]

4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one

Drug Info

[68]

4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole

Drug Info

[69]

4-(4-Benzyl-piperazin-1-yl)-1H-indole

Drug Info

[69]

4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole

Drug Info

[69]

4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole

Drug Info

[69]

4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one

Drug Info

[71]

4-Dipropylamino-cyclohex-1-enecarbonitrile

Drug Info

[59]

5-OH-DPAT

Drug Info

[72]

A-690344

Drug Info

[74]

A-706149

Drug Info

[75]

A-987306

Drug Info

[54]

Azaperone

Drug Info

[76]

Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine

Drug Info

[68]

Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine

Drug Info

[68]

D-189

Drug Info

[77]

D-190

Drug Info

[77]

D-192

Drug Info

[77]

D-193

Drug Info

[77]

D-203

Drug Info

[77]

D-210

Drug Info

[77]

D-218

Drug Info

[77]

D-219

Drug Info

[77]

D-220

Drug Info

[77]

D-237

Drug Info

[78]

D-264

Drug Info

[79]

D-315

Drug Info

[80]

D-366

Drug Info

[72]

Etoloxamine

Drug Info

[58]

FLUMEZAPINE

Drug Info

[81]

FLUTROLINE

Drug Info

[82]

ISOCLOZAPINE

Drug Info

[66]

ISOLOXAPINE

Drug Info

[83]

L-741626

Drug Info

[84]

L-741742

Drug Info

[85]

N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide

Drug Info

[60]

N-(4-Propylaminobutyl)-4-biphenylcarboxamide

Drug Info

[60]

PG-01037

Drug Info

[93]

QUINPIROLE

Drug Info

[95]

R-226161

Drug Info

[96]

SB-271046

Drug Info

[97]

STEPHOLIDINE

Drug Info

[99]

UH-232

Drug Info

[100]

[2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine

Drug Info

[68]

Antagonist

[+] 20 Antagonist drugs

GSK598809

Drug Info

[36]

ONC201

Drug Info

[10]

GSK618334

Drug Info

[36]

AVE-5997EF

Drug Info

[23]

S-33138

Drug Info

[44], [45]

PD-157533

Drug Info

[23]

PD-157695

Drug Info

[23]

PD-158771

Drug Info

[23]

AS-8112

Drug Info

[48]

BP4.879a

Drug Info

[23]

Dianicline+rimonabant

Drug Info

[49]

PNU-177864

Drug Info

[23]

RGH-1756

Drug Info

[23]

SB-277011

Drug Info

[23]

(+)-AJ76

Drug Info

[53]

(+)-S-14297

Drug Info

[55]

AS-9705

Drug Info

[48]

nafadotride

Drug Info

[87]

NGB 2904

Drug Info

[88]

[3H]spiperone

Drug Info

[103], [104]

Partial agonist

[+] 1 Partial agonist drugs

RP5063

Drug Info

[37]

Ligand

[+] 2 Ligand drugs

Aryl piperazine derivative 1

Drug Info

[39]

Aryl piperazine derivative 6

Drug Info

[39]

Binder

[+] 2 Binder drugs

U-99194A

Drug Info

[23]

BTS-79018

Drug Info

[23]

Modulator (allosteric modulator)

[+] 1 Modulator (allosteric modulator) drugs

SB269652

Drug Info

[98]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 2 KEGG Pathways

Neuroactive ligand-receptor interaction

Dopaminergic synapse

Reactome

[+] 2 Reactome Pathways

Dopamine receptors

G alpha (i) signalling events

WikiPathways

[+] 6 WikiPathways

Monoamine GPCRs

GPCRs, Class A Rhodopsin-like

GPCR ligand binding

GPCR downstream signaling

Nicotine Activity on Dopaminergic Neurons

GPCRs, Other

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.

REF 2

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7671).

REF 3

REF 4

Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.

REF 5

REF 6

Update on ropinirole in the treatment of Parkinson's disease. Neuropsychiatr Dis Treat. 2009;5:33-6.

REF 7

Pharmaceutical Research Companies Are Developing More Than 300 Medicines to Treat Mental Illnesses. Pharmaceutical Research and Manufacturers of America report.2010.

REF 8

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 9

ClinicalTrials.gov (NCT01188967) Effectiveness of GSK598809, a Selective D3 Antagonist, Added to Cognitive Behavioral Therapy and Nicotine Replacement Therapy for Smoking Cessation and Prevention of Very Early Relapse to Smoking. U.S. National Institutes of Health.

REF 10

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 11

ClinicalTrials.gov (NCT01490086) RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder. U.S. National Institutes of Health.

REF 12

ClinicalTrials.gov (NCT03544229) A Study to Evaluate the Efficacy and Safety of TAK-906 in Adult Participants With Symptomatic Idiopathic or Diabetic Gastroparesis. U.S. National Institutes of Health.

REF 13

ClinicalTrials.gov (NCT00513279) To Investigate If Single Doses Of GSK618334 Are Safe And To Investigate Blood Levels Of GSK618334. U.S. National Institutes of Health.

REF 14

Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66.

REF 15

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001472)

REF 17

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012940)

REF 18

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Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012397)

REF 20

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018413)

REF 21

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014544)

REF 22

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026348)

REF 23

The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.

REF 24

REF 25

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013394)

REF 26

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.

REF 27

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009088)

REF 28

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027143)

REF 29

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126)

REF 30

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.

REF 31

REF 32

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005975)

REF 33

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 34

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)

REF 35

Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51.

REF 36

Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).

REF 37

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 38

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.

REF 39

5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.

REF 40

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.

REF 41

Association of dopamine-related genetic loci to dopamine D3 receptor antagonist ABT-925 clinical response.Transl Psychiatry.2013 Apr 9;3:e245.

REF 42

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.

REF 43

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.

REF 44

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.

REF 45

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 46

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.

REF 47

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.

REF 48

Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.

REF 49

Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole. J Neurochem. 2003 Nov;87(3):631-41.

REF 50

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126)

REF 51

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.

REF 52

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.

REF 53

Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature. 1990 Sep 13;347(6289):146-51.

REF 54

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.

REF 55

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.

REF 56

Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.

REF 57

Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. J Med Chem. 1993 Oct 15;36(21):3188-96.

REF 58

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.

REF 59

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.

REF 60

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.

REF 61

Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines. Bioorg Med Chem. 2008 Apr 1;16(7):3773-9.

REF 62

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.

REF 63

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.

REF 64

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.

REF 65

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.

REF 66

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.

REF 67

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).

REF 68

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.

REF 69

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.

REF 70

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.

REF 71

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.

REF 72

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