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

General Information of Drug (ID: DM625LN)

• Drug Name: AG-041R Drug Info
• Synonyms: AG-041R; LS-83786; 199800-49-2; GTPL901; MLS006010838; AG041R; CTK8E8139; DTXSID40430968; AG 041R; MolPort-009-019-290; ZINC3930890; NCGC00263225-01; SMR004701765; RT-011212; FT-0773348; J-012912

Indication

Disease Entry	ICD 11	Status	REF
Ulcerative colitis	DD71	Terminated	[1]

• Cross-matching ID:
  PubChem CID: 9807431
  CAS Number: CAS 159883-95-1
  TTD Drug ID: DM625LN

Molecule-Related Drug Atlas

Drug(s) Targeting Gastrin/cholecystokinin type B receptor (CCKBR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pentagastrin	DMRCLZB	Diagnostic imaging	N.A.	Approved	[3]
Ceruletide	DM2WE5K	Caerulein stimulated gastric and pancreatic secretion	5A4Y	Approved	[4]
GASTRAZOLE	DMO3ITF	Duodenal ulcer	DA63	Phase 3	[5]
Dexloxiglumide	DM52HUD	Pancreatic malfunction	DC30-DC3Z	Phase 2	[6]
Spiroglumide	DM7NJWY	Stomach disease	DA43-DA4Y	Phase 2	[7]
TT-223	DMCDMFP	Type-1 diabetes	5A10	Phase 2	[8]
Z 360	DM2M80G	Discovery agent	N.A.	Phase 2	[9]
S-0509	DM4KWEF	Ulcerative colitis	DD71	Phase 2	[10]
YF-476	DM54MAJ	Stomach ulcer	DA60.Z	Phase 2	[11]
Itriglumide	DM5UFRO	Anxiety disorder	6B00-6B0Z	Phase 2	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gastrin/cholecystokinin type B receptor (CCKBR)	TTVFO0U	GASR_HUMAN	Modulator	[2]

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: 901).
• [2] AG-041R, a gastrin/CCK-B antagonist, stimulates chondrocyte proliferation and metabolism in vitro. Biochem Biophys Res Commun. 2001 May 25;283(5):1118-23.
• [3] Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21.
• [4] Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.
• [5] Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 April 24; 94(8): 1107-1115.
• [6] Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecy... J Med Chem. 1997 Oct 10;40(21):3402-7.
• [7] Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9.
• [8] The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans. Int J Obes Relat Metab Disord. 2000 Mar;24(3):288-98.
• [9] Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gen... Biol Pharm Bull. 2010;33(2):216-22.
• [10] Selective action of a CCK-B/gastrin receptor antagonist, S-0509, on pentagastrin-, peptone meal- and beer-stimulated gastric acid secretion in dogs. Aliment Pharmacol Ther. 2000 Apr;14(4):479-88.
• [11] CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90.
• [12] Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases. Curr Top Med Chem. 2007; 7(12): 1211-1231.