General Information of Drug (ID: DM682UV)

Drug Name
PD-158771 Drug Info
Synonyms PD 158771; N-[4-[2-(4-phenylpiperazin-1-yl)ethyl]cyclohexyl]pyrimidin-2-amine; Trans-N-(4-(2-(4-Phenyl-1-piperazinyl)ethyl)cyclohexyl)-2-pyrimidinamine
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Preclinical [1]
Cross-matching ID
PubChem CID
3075615
CAS Number
CAS 189152-50-9
TTD Drug ID
DM682UV

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting Dopamine D3 receptor (D3R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cariprazine DMJYDVK Bipolar disorder 6A60 Approved [2]
Pramipexole DMNMW9R Parkinson disease 8A00.0 Approved [3]
Ropinirole DMA6S1D Parkinson disease 8A00.0 Approved [3]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [4]
P2B-001 DM9PVHX Parkinson disease 8A00.0 Phase 3 [5]
RP5063 DMKUE8O Schizophrenia 6A20 Phase 2 [6]
ONC201 DMM5SCF Endometrial cancer 2C76 Phase 2 [7]
TAK-906 DMBQD9H Diabetic gastroparesis DA41.00 Phase 2 [8]
GSK598809 DMGU05N Drug abuse 6C4G.1Z Phase 2 [9]
GSK618334 DMJPXZ4 Drug abuse 6C4G.1Z Phase 1 [9]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [10]
Haloperidol DM96SE0 Delirium Approved [11]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [12]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [13]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [14]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [15]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [16]
Pimozide DMW83TP Schizophrenia 6A20 Approved [17]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [18]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [19]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 1A receptor (HTR1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trazodone DMK1GBJ Depression 6A70-6A7Z Approved [3]
Buspirone DMBS632 Anxiety disorder 6B00-6B0Z Approved [20]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [21]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [22]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [2]
Gepirone DMGX5Q0 Major depressive disorder 6A70.3 Approved [23]
TERTATOLOL DM2L3D5 Hypertension BA00-BA04 Approved [24]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [25]
Treximet DMU54QB Migraine 8A80 Approved [9]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [4]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Antagonist [1]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Antagonist [1]
Dopamine D3 receptor (D3R) TT4C8EA DRD3_HUMAN Antagonist [1]

References

1 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
2 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
5 Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51.
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 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
10 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
11 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
12 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
13 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
14 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
15 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: 3639).
16 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
17 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
18 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
19 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
20 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
21 Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.
22 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
23 Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
24 Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile, Bioorg. Med. Chem. Lett. 3(10):2035-2038 (1993).
25 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.