CR-1409 at concentrations between 0.3 and 30 microM inhibited cholecystokinin-stimulated amylase release in a dose-dependent manner without appreciable effect on the basal amylase secretion. Biphasic dose-response curves to cholecystokinin for amylase release shifted to the right with an increase in the concentration of the drug.

Lorglumide (CR-1409) is a drug which inhibits gastrointestinal motility and reduces gastric secretions, acting as a cholecystokinin antagonist, [1] with fairly high selectivity for the CCK A subtype. [2] .

1987年1月1日 · Behavioral and receptor binding techniques were employed to evaluate the potency of CR 1409, a new analog of proglumide, as a cholecystokinin antagonist. CR 1409, at doses of 1 mg/kg i.p. in mice, effectively blocked the inhibition of feeding and exploratory behaviors induced by cholecystokinin.

CR 1409 caused a rightward and parallel shift in the dose-response curve of CCK-8-stimulated pancreatic protein secretion in anesthetized rats, demonstrating a competitive mechanism of inhibition. The mean pA2 value, showing the 50% inhibitory dose of CR 1409, was 6.4.

The inhibitory effects of CR-1409, a new glutaramic acid derivative developed as a cholecystokinin (CCK) receptor antagonist, on caerulein-stimulated amylase secretion and on intracellular Ca2+ ([Ca2+]i) mobilization were studied in isolated rat pancreatic acini. Pancreatic acini were prepared by co …

Lorglumide sodium salt (CR-1409 sodium salt) 是一种有效的胆囊收缩素（CCK）受体拮抗剂。 MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

1986年11月1日 · CR 1409, a glutaramic acid derivative with competitive cholecystokinin-antagonistic activity, was administered IP and evaluated in comparison with proglumide (the model CCK-receptor antagonist), gabexate (protease inhibitor) and PGE 2 (cytoprotective) on two different models of experimental pancreatitis. Acute pancreatitis was induced in mice ...

The potency and selectivity of D,L-4-(3,4-dichloro-benzoyl-amino)-5-(dipentyl-amino)-5-oxo-pen tan oic acid (CR 1409) as a cholecystokinin (CCK) antagonist was investigated on motor responses of the longitudinal and circular muscles of the guinea-pig isolated ileum.

The effects of proglumide-related cholecystokinin (CCK) receptor antagonists CR 1409 and CR 1392 on CCK-octapeptide (CCK-8)-stimulated immunoreactive insulin (IRI) release and exocrine secretion were examined simultaneously in the isolated perfused rat pancreas. The CR 1409, at concentrations of 10- …

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