PMID: 8968365Dec 1, 1996Paper

Pharmacological profile of a new serine derivative cholecystokinin receptor antagonist TP-680 on pancreatic, biliary and gastric function

The Journal of Pharmacology and Experimental Therapeutics
I TachibanaM Otsuki

Abstract

The in vivo pharmacological effects of the newly developed serine derivative [(R)-1-[3-(3-carboxypyridine-2-yl)thio-2-(indol-2-yl) carbonylamino]propionyl-4-diphenyl-methyl-piperazine] (TP-680), a cholecystokinin type-A (CCK-A) receptor antagonist, on pancreatic, biliary and gastric function were examined in rats and mice. The i.v. infusion of TP-680 in rats caused a parallel rightward shift of the entire dose-response curve for cholecystokinin octapeptide (CCK-8)-stimulated pancreatic exocrine secretion without altering the maximal response (ID50 = 480 nmol/kg). TP-680 also antagonized CCK-8-stimulated pancreatic secretion in mice (ID50 = 600 nmol/kg). Secretion of pancreatic juice and protein elicited by intraduodenal infusion of casein was also antagonized by TP-680. The CCK antagonism produced by i.v. TP-680 persisted for 16 h. Specificity for CCK was demonstrated by the inability of TP-680 (1000 nmol/kg) to antagonize either secretin- or bombesin-stimulated pancreatic secretion in rats. Moreover, specificity for CCK-A receptor was also demonstrated by the inability of TP-680 to antagonize pentagastrin-stimulated gastric acid secretion. Administered i.v., TP-680 was highly potent in antagonizing CCK-8-induced inhibition of ...Continue Reading

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