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Inhibitory effect of CR-1409, a competitive inhibitor of cholecystokinin, on pancreatic exocrine secretion in the conscious rat.

1988; Tohoku University; Volume: 155; Issue: 2 Linguagem: Inglês

10.1620/tjem.155.165

1349-3329

Kyoko Miyasaka, Rieko Nakamura, Akihiro Funakoshi, Kenichi Kitani,

Peptidase Inhibition and Analysis

MIYASAKA, K., NAKAMURA, R., FUNAKOSHI, A. and KITANI, K. Inhibitory Effect of CR-1409, a Competitive Inhibitor of Cholecystokinin, on Pancreatic Exocrine Secretion in the Conscious Rat. Tohoku J. exp. Med., 1988, 155 (2), 165-172 - The inhibitory effect of CR-1409, a new glutaramic acid derivative and a competitive inhibitor for cholecystokinin (CCK), on the basal and CCK-stimulated pancreatic secretion was examined in the conscious rat in vivo. Rats were prepared with cannulae draining pure bile and pancreatic juice separately and with a duodenal cannula and right and left jugular vein cannulae. Plasma CCK level increased to 3.65±0.79 and 19.9±4.47pM (mean±S.E.) by a 2-hr infusion of 100 and 300pmole/kg/hr of CCK-octapeptide (CCK-8), respectively. Simultaneous infusion of 170nmole/kg/hr of CR-1409 completely abolished pancreatic responses to 100pmole/kg/hr of CCK-8. Infusion of CR-1409 at rate of 57nmole/ kg/hr slightly but significantly inhibited CCK-8 (100pmole/kg/hr)-stimulated secretion. Pancreatic responses to 300pmole/kg/hr of CCK-8 were partially inhibited but not completely abolished by the 170nmole/kg/hr of CR-1409. Neither the basal pancreatic secretion nor the bile secretion was affected by CR-1409. We conclude that CR-1409 inhibited CCK-stimulated pancreatic secretion in vivo.