(+/-)-4-([3,4-Dichlorobenzoyl]amino)-5-(dipentylamino)-5-oxopentanoic acid sodium

Lorglumide sodium salt has been used as a cck-a (cholecystokinin A) receptor antagonist for peptide determination in rat islet cells. It has been used as a CCK1 inhibitor to check the effect of cck1 (cck-a) and cck2 (cck-b) receptors on cerulein-induced upregulation of egr-1 (early growth response 1) expression in rat pancreatic acinar cells.

lorglumide (sodium salt) is the first nonpeptidic, selective and potent inhibitor of the cck-a receptor [1][2][3][4] .cholecystokinin (cck) is a peptide hormone that plays important roles in the physiological regulation of pancreatic enzyme secretion, induction of pancreatic growth, smooth muscle contraction in the gall bladder and stomach, and modulation of feeding and behavior [1][2][3].lorglumide (cr1409) is the first nonpeptidic, selective and potent inhibitor of the cck-a receptor. lorglumide inhibited cck a receptor and cck b receptor with ic50 values of 50 nm and 3 μm, respectively [4]. in the guinea-pig isolated ileum, lorglumide (0.06-2.1 μm) antagonized longitudinal muscle responses to ceruletide (a cck-related decapeptide) and cck-octapeptide (cck-8) in a concentration dependent and competitive manner. lorglumide (0.2-0.4 μm) also blocked contractions of the circular muscle induced by ceruletide [2].in mice, cr1409 completely abolished the trophic effects of exogenous cck and significantly inhibited the effects of chronic camostate feeding. cr1409 reduced pancreatic weight, dna and protein content [3].

Potent and selective non-peptide cholecystokinin (CCKA) receptor antagonist; orally active.

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[4]. scarpignato c, varga g, dobronyi i, et al. effect of a new potent cck antagonist, lorglumide, on caerulein- and bombesin-induced pancreatic secretion and growth in the rat. br j pharmacol. 1989 mar;96(3):661-9.