General Information of Drug (ID: DMKI2GJ)

Drug Name
Azaperone Drug Info
Synonyms
Azaperone; 1649-18-9; Azaperon; Stresnil; Fluoperidol; Suicalm; Eucalmyl; Azeperone; Sedaperone vet; Azaperona; Azaperonum; R-1929; NSC 170976; Azaperonum [INN-Latin]; Azaperona [INN-Spanish]; 1-Butanone, 1-(4-fluorophenyl)-4-[4-(2-pyridinyl)-1-piperazinyl]-; UNII-19BV78AK7W; 1-(3-(4-Fluorobenzoyl)propyl)-4-(2-pyridyl)piperazine; CCRIS 1586; C19H22FN3O; 1-(4-Fluorophenyl)-4-[4-(2-pyridinyl)-1-piperazinyl]-1-butanone; 4'-Fluoro-4-(4-(2-pyridyl)-1-piperazinyl)butyrophenone; EINECS 216-715-8; R 1929; BRN 0565491; MLS003106751
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
15443
ChEBI ID
CHEBI:88301
CAS Number
CAS 1649-18-9
TTD Drug ID
DMKI2GJ

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
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 [3]
Pramipexole DMNMW9R Parkinson disease 8A00.0 Approved [4]
Ropinirole DMA6S1D Parkinson disease 8A00.0 Approved [4]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [5]
P2B-001 DM9PVHX Parkinson disease 8A00.0 Phase 3 [6]
RP5063 DMKUE8O Schizophrenia 6A20 Phase 2 [7]
ONC201 DMM5SCF Endometrial cancer 2C76 Phase 2 [8]
TAK-906 DMBQD9H Diabetic gastroparesis DA41.00 Phase 2 [9]
GSK598809 DMGU05N Drug abuse 6C4G.1Z Phase 2 [10]
GSK618334 DMJPXZ4 Drug abuse 6C4G.1Z Phase 1 [10]
⏷ 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 [11]
Haloperidol DM96SE0 Delirium Approved [12]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [13]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [14]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [15]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [16]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [17]
Pimozide DMW83TP Schizophrenia 6A20 Approved [18]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [19]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [21]
Quinidine DMLPICK N. A. N. A. Approved [22]
Verapamil DMA7PEW Angina pectoris BA40 Approved [23]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [24]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [24]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [25]
Propranolol DM79NTF Angina pectoris BA40 Approved [26]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [27]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [28]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [24]
⏷ 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
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Inhibitor [1]
Dopamine D3 receptor (D3R) TT4C8EA DRD3_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [2]

References

1 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.
2 Why are most phospholipidosis inducers also hERG blockers?. Arch Toxicol. 2017 Dec;91(12):3885-3895. doi: 10.1007/s00204-017-1995-9. Epub 2017 May 27.
3 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
6 Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51.
7 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9 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.
10 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
11 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.
12 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
13 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
14 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.
15 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
16 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).
17 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
18 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
19 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.
20 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
21 Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
22 Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
23 Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
24 Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
25 Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
26 Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
27 Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
28 Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.