Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMZ51UJ)

• Drug Name: A-123189 Drug Info
• Synonyms: A-123189; CHEMBL13856; GTPL491; SCHEMBL7834335; BDBM50099325; A123189; A 123189; 3-{2-[4-(2-Methoxy-phenyl)-piperazin-1-yl]-ethyl}-5-m-tolyl-1H-thieno[2,3-d]pyrimidine-2,4-dione; 3-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-5-(3-methylphenyl)-1H-thieno[3,2-e]pyrimidine-2,4-dione

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 9891167
  TTD Drug ID: DMZ51UJ

Molecule-Related Drug Atlas

Drug(s) Targeting Adrenergic receptor alpha-1B (ADRA1B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methamphetamine	DMPM4SK	Anxiety		Approved	[4]
Propericiazine	DME9JNL	Psychiatric disorder	6E8Z	Approved	[5]
Methoxamine	DMF5XQH	Hypertension	BA00-BA04	Approved	[6]
Phendimetrazine	DM6TS1N	Obesity	5B81	Approved	[7]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[8]
TIOSPIRONE	DME5QDP	N. A.	N. A.	Discontinued in Phase 3	[9]
Sunepitron	DM6M8ZX	N. A.	N. A.	Discontinued in Phase 3	[10]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[11]
SOU-001	DMPAEK5	Urinary incontinence	MF50.2	Discontinued in Phase 2	[12]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[13]

Drug(s) Targeting Adrenergic receptor alpha-1A (ADRA1A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SILODOSIN	DMJSBT6	Benign prostatic hyperplasia	GA90	Approved	[2]
NAFTOPIDIL	DMQ8R4E	Hypertension	BA00-BA04	Approved	[2]
Tamsulosin	DM5QF9V	Benign prostatic hyperplasia	GA90	Approved	[14]
Xatral	DMLHOA0	Benign prostatic hyperplasia	GA90	Approved	[15]
Dutasteride + tamsulosin	DM6P8HU	Benign prostatic hyperplasia	GA90	Phase 3	[16]
Besipirdine	DMLVNTA	Cognitive impairment	6D71	Phase 3	[17]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[8]
PMID30124346-Compound-LDT8	DM5MUNG	Benign prostatic hyperplasia	GA90	Patented	[18]
PMID30124346-Compound-LDT66	DMJMTNL	Benign prostatic hyperplasia	GA90	Patented	[18]
TIOSPIRONE	DME5QDP	N. A.	N. A.	Discontinued in Phase 3	[9]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adrenergic receptor alpha-1A (ADRA1A)	TTNGILX	ADA1A_HUMAN	Inhibitor	[2]
Adrenergic receptor alpha-1B (ADRA1B)	TTBRKXS	ADA1B_HUMAN	Inhibitor	[3]

References

• [1] 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: 491).
• [2] Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64.
• [3] Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien. Bioorg Med Chem Lett. 2001 May 7;11(9):1119-21.
• [4] Mirtazapine treatment after conditioning with methamphetamine alters subsequent expression of place preference. Drug Alcohol Depend. 2009 Jan 1;99(1-3):231-9.
• [5] Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91.
• [6] Activation of alpha1-adrenoceptors inhibits growth hormone secretion in humans. Exp Clin Endocrinol Diabetes. 2009 Oct;117(9):460-2.
• [7] Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
• [8] A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33.
• [9] 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.
• [10] An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35.
• [11] 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.
• [12] Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83.
• [13] Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716.
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [15] Pharma & Vaccines. Product Development Pipeline. April 29 2009.
• [16] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [17] Alpha-Adrenergic activity and cardiovascular effects of besipirdine HCl (HP 749) and metabolite P7480 in vitro and in the conscious rat and dog. J Pharmacol Exp Ther. 1997 Apr;281(1):337-46.
• [18] 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.