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

General Information of Drug (ID: DM1GLIN)

• Drug Name: A-81988 Drug Info
• Synonyms: 2-[Propyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridine-3-carboxylic acid; 141887-34-5; A81988; A 81988; CHEMBL416477; Abbott-81988; 2-[propyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]pyridine-3-carboxylic acid; 3-Pyridinecarboxylicacid, 2-[propyl[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]amino]-; ACMC-20n0yv; [3H]A81988; [3H]-A81988; AC1L30WD; 2-(N-Propyl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)amino)pyridine-3-carboxylic acid; Oprea1_714523; SCHEMBL7048946; GTPL3938; CTK0H8555; DTXSID40161846; BDBM50003154; HY-U00188; CS-7281; L007227; Abbott-81988

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Terminated	[1]

• Cross-matching ID:
  PubChem CID: 132387
  CAS Number: CAS 141887-34-5
  TTD Drug ID: DM1GLIN

Molecule-Related Drug Atlas

Drug(s) Targeting Angiotensin II receptor type-1 (AGTR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Losartan	DM72JXH	Diabetic kidney disease	GB61.Z	Approved	[3]
Olmesartan medoxomil	DMWBHRY	High blood pressure	BA00	Approved	[4]
Irbesartan	DMTP1DC	Diabetic kidney disease	GB61.Z	Approved	[3]
Valsartan	DMREUQ6	Chronic heart failure	BD1Z	Approved	[3]
Candesartan	DMRK8OT	Chronic heart failure	BD1Z	Approved	[5]
Telmisartan	DMS3GX2	Hypertension	BA00-BA04	Approved	[6]
ANGIOTENSIN II	DMLWQ27	Increase blood pressure	BA04	Approved	[7]
SARALASIN	DMKS1DV	Hypertension	BA00-BA04	Approved	[8]
Tasosartan	DMM13DI	Hypertension	BA00-BA04	Approved	[9]
Eprosartan	DM07K2I	Hypertension	BA00-BA04	Approved	[10]

Drug(s) Targeting Angiotensin II receptor (AGTR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CYT-006-AngQb	DMIRSWE	Hypertension	BA00-BA04	Phase 2	[11]
DA-727	DM9KS1A	Hypertension	BA00-BA04	Phase 1	[12]
BIBR-363	DMGWFZJ	Hypertension	BA00-BA04	Discontinued in Phase 2	[13]
FK-739	DM7TLF6	Hypertension	BA00-BA04	Discontinued in Phase 2	[14]
ETRX-101	DMRB23N	Anemia	3A00-3A9Z	Discontinued in Phase 2	[15]
Elisartan potassium	DM0XF8J	Hypertension	BA00-BA04	Discontinued in Phase 2	[16]
ICI-D-8731	DM3R8TX	Hypertension	BA00-BA04	Discontinued in Phase 2	[17]
E-4177	DM2G7IP	Hypertension	BA00-BA04	Discontinued in Phase 2	[18]
CGP-48369	DMY8KO4	Hypertension	BA00-BA04	Discontinued in Phase 1	[19]
ICI-D-6888	DMZYA9E	Hypertension	BA00-BA04	Discontinued in Phase 1	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiotensin II receptor (AGTR)	TTGN1ZA	NOUNIPROTAC	Modulator	[2]
Angiotensin II receptor type-1 (AGTR1)	TT8DBY3	AGTR1_HUMAN	Antagonist	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002509)
• [2] [3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors. Eur J Pharmacol. 1994 Mar 15;267(1):49-54.
• [3] Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41.
• [4] Mechanism of diastolic stiffening of the failing myocardium and its prevention by angiotensin receptor and calcium channel blockers. J Cardiovasc Pharmacol. 2009 Jul;54(1):47-56.
• [5] Candesartan: widening indications for this angiotensin II receptor blocker Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007.
• [6] Deletion of angiotensin II type I receptor reduces hepatic steatosis. J Hepatol. 2009 Jun;50(6):1226-35.
• [7] The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1. J Med Chem. 2010 Mar 11;53(5):2063-75.
• [8] Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
• [9] Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54.
• [10] Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7.
• [11] CYT-006-AngQb, a vaccine against angiotensin II for the potential treatment of hypertension. Curr Opin Investig Drugs. 2009 Mar;10(3):269-75.
• [12] WO patent application no. 2009,0880,06, Combined pharmaceutical agent.
• [13] Evaluation of the angiotensin challenge methodology for assessing the pharmacodynamic profile of antihypertensive drugs acting on the renin-angiotensin system. Br J Clin Pharmacol. 1999 October; 48(4): 594-604.
• [14] The pharmacological characterization of FK 739, a new angiotensin II-receptor antagonist. Jpn J Pharmacol. 1993 Nov;63(3):335-43.
• [15] WO patent application no. 2010,0332,07, Polymer conjugates of therapeutic peptides.
• [16] Safety and tolerability of losartan potassium, an angiotensin II receptor antagonist, compared with hydrochlorothiazide, atenolol, felodipine ER, and angiotensin-converting enzyme inhibitors for the treatment of systemic hypertension. Am J Cardiol. 1995 Apr 15;75(12):793-5.
• [17] Vasomotor responses in cyclosporin A-treated rats after chronic angiotensin blockade. Hypertension. 1994 Jun;23(6 Pt 2):832-7.
• [18] Prevention of renal damage by angiotensin II blockade, accompanied by increased renal hepatocyte growth factor in experimental hypertensive rats. Hypertension. 1999 Aug;34(2):279-84.
• [19] Antihypertensive therapy augments endothelium-dependent relaxations in coronary arteries of spontaneously hypertensive rats. Circulation. 1994 May;89(5):2212-8.
• [20] WO patent application no. 1995,0216,09, Treatment of normotensive glaucoma with angiotensin ii antagonists.