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

General Information of Drug (ID: DMZ4HMP)

Drug Name

A-71378 Drug Info

Synonyms

A 71378; Desamino-tyr(SO3H)-nle-gly-trp-nle-(N-methyl)asp-phe-NH2; (3S)-4-[[(2R)-1-[2-[[(2S)-2-[[1H-indol-3-ylmethyl-[2-[[(2S)-2-[3-(4-sulfooxyphenyl)propanoylamino]hexanoyl]amino]acetyl]carbamoyl]amino]hexanoyl]carbamoyl]phenyl]propan-2-yl]amino]-3-(methylamino)-4-oxobutanoic acid; (3S)-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-[[(2S)-2-[3-(4-sulfooxyphenyl)propanoylamino]hexanoyl]amino]acetyl]amino]propanoyl]amino]hexanoyl]-methylamino]-4-oxobutanoic acid

Indication

Disease Entry	ICD 11	Status	REF
Obesity	5B81	Preclinical	[1]

Cross-matching ID

PubChem CID: 5489450
CAS Number: CAS 127902-33-4
TTD Drug ID: DMZ4HMP

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Discontinued Drug(s)

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Drug(s) Targeting Cholecystokinin receptor type A (CCKAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dexloxiglumide	DM52HUD	Pancreatic malfunction	DC30-DC3Z	Phase 2	[3]
proglumide	DM4MF9V	Influenza virus infection	1E30-1E32	Phase 2	[4]
Lintitript	DMS5X94	Obesity	5B81	Discontinued in Phase 2	[5]
Tarazepide	DMX6ZYE	Gastrointestinal disease	DE2Z	Discontinued in Phase 2	[6]
GI 181771	DMIUFS4	Obesity	5B81	Discontinued in Phase 2	[7]
Pranazepide	DMP43IR	Pancreatic malfunction	DC30-DC3Z	Discontinued in Phase 2	[8]
CE-326597	DMXO49B	Obesity	5B81	Discontinued in Phase 2	[9]
UCL-2000; butabindide	DML51D0	Obesity	5B81	Discontinued in Phase 1	[2]
SSR-125180	DMSOBW2	Obesity	5B81	Discontinued in Phase 1	[10]
T-0632	DML4M5K	Pancreatic malfunction	DC30-DC3Z	Discontinued in Phase 1	[11]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cholecystokinin receptor type A (CCKAR)	TTCG0AL	CCKAR_HUMAN	Agonist	[2]

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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: 894).
2	Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
3	Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. J Med Chem. 1989 Feb;32(2):445-9.
4	Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8.
5	A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15.
6	Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80.
7	Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506.
8	Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines, Bioorg. Med. Chem. Lett. 7(2):169-174 (1997).
9	Obesity Pharmacotherapy: Current Perspectives and Future Directions. Curr Cardiol Rev. 2013 February; 9(1): 33-54.
10	US patent application no. 8,748,419, Antagonists.
11	Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12.