General Information of Drug (ID: DMKANOH)

Drug Name
Bis(31/31')[[Cys(31), Nva(34)]NPY(27-36)-NH(2)] Drug Info
Synonyms
Loxiglumide; LOXIGLUMIDE; 107097-80-3; Loxiglumide [INN]; Loxiglumidum [Latin]; Loxiglumida [Spanish]; CR 1505; CR-1505; CHEMBL206025; (+-)-4-(3,4-Dichlorobenzamido)-N-(3-methoxypropyl)-N-pentylglutaramic acid; 4-(3,4-dichlorobenzamido)-5-((3-methoxypropyl)(pentyl)amino)-5-oxopentanoic acid; (+-)-4-((3,4-Dichlorobenzoyl)amino)-5-((3-methoxypropyl)pentylamino)-5-oxopentanoic acid; D,L-4-(3,4-Dichlorobenzoylamino)-5-(N-3-methoxypropylpentylamino)-5-oxo-pentanoic acid; Loxiglumidum; Loxiglumida; Pentanoic
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
60182
ChEBI ID
CHEBI:31785
CAS Number
CAS 107097-80-3
TTD Drug ID
DMKANOH

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Discontinued Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
CGP71683A DMRYC08 Obesity 5B81 Discontinued in Phase 3 [5]
Velneperit DMROSHN Obesity 5B81 Discontinued in Phase 2 [6]
S-234462 DM80P4U Obesity 5B81 Discontinued in Phase 1 [6]
Axovan-3 DM1JN6A Eating disorder 6B82 Discontinued in Phase 1 [7]
FR-79620 DMXR287 Diabetic complication 5A2Y Preclinical [8]
GW-594884A DMHUD27 Obesity 5B81 Preclinical [8]
NPY5RA-972 DMXUCSN Obesity 5B81 Preclinical [8]
RWJ-49815 DMUGZMO Fungal infection 1F29-1F2F Terminated [7]
AR-129330 DMUSYKG Discovery agent N.A. Investigative [9]
S-25585 DMBUD1M Eating disorder 6B82 Investigative [7]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexloxiglumide DM52HUD Pancreatic malfunction DC30-DC3Z Phase 2 [10]
proglumide DM4MF9V Influenza virus infection 1E30-1E32 Phase 2 [11]
Lintitript DMS5X94 Obesity 5B81 Discontinued in Phase 2 [12]
Tarazepide DMX6ZYE Gastrointestinal disease DE2Z Discontinued in Phase 2 [13]
GI 181771 DMIUFS4 Obesity 5B81 Discontinued in Phase 2 [14]
Pranazepide DMP43IR Pancreatic malfunction DC30-DC3Z Discontinued in Phase 2 [15]
CE-326597 DMXO49B Obesity 5B81 Discontinued in Phase 2 [16]
UCL-2000; butabindide DML51D0 Obesity 5B81 Discontinued in Phase 1 [8]
SSR-125180 DMSOBW2 Obesity 5B81 Discontinued in Phase 1 [17]
T-0632 DML4M5K Pancreatic malfunction DC30-DC3Z Discontinued in Phase 1 [18]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
A-68552 DM1BDHY Obesity 5B81 Terminated [19]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cholecystokinin receptor (CCKR) TTKAPQ1 NOUNIPROTAC Antagonist [2]
Cholecystokinin receptor type A (CCKAR) TTCG0AL CCKAR_HUMAN Antagonist [3]
Neuropeptide Y receptor type 5 (NPY5R) TTY6EWA NPY5R_HUMAN Agonist [4]

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: 892).
2 Cholecystokinin receptor antagonist, loxiglumide, inhibits invasiveness of human pancreatic cancer cell lines. FEBS Lett. 1996 Apr 1;383(3):241-4.
3 Role of CCK(A) receptors in postprandial lower esophageal sphincter function in morbidly obese subjects. Dig Dis Sci. 2002 Nov;47(11):2531-7.
4 Bis(31/31')[[Cys(31), Nva(34)]NPY(27-36)-NH(2)]: a neuropeptide Y (NPY) Y(5) receptor selective agonist with a latent stimulatory effect on food intake in rats. Peptides. 2002 Aug;23(8):1485-90.
5 Neuropeptide Y-induced enhancement of the evoked release of newly synthesized dopamine in rat striatum: mediation by Y2 receptors. Neuropharmacology. 2007 May;52(6):1396-402.
6 Clinical pipeline report, company report or official report of Shionogi (2011).
7 Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36.
8 Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
9 Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3853-6.
10 Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. J Med Chem. 1989 Feb;32(2):445-9.
11 Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8.
12 A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15.
13 Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80.
14 Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506.
15 Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines, Bioorg. Med. Chem. Lett. 7(2):169-174 (1997).
16 Obesity Pharmacotherapy: Current Perspectives and Future Directions. Curr Cardiol Rev. 2013 February; 9(1): 33-54.
17 US patent application no. 8,748,419, Antagonists.
18 Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12.
19 CN patent application no. 102481276, Chemosensory receptor ligand-based therapies.