[Effect of cholecystokinin and its antagonists lorglumide, devazepide, and L-365,260 on gastrointestinal motility in rats].
Cholecystokinin (CCK) plays an important role in gallbladder contraction and gut motility. Sincalide (CCK-8) evoked guinea pig isolated ileum contraction at 10(-5)-10(-1) mumol.L-1 in a concentration-dependent manner, EC50 being 207 pmol.L-1. It delayed the gastric emptying as well. The rate of inhibition of gastric emptying was 71 +/- 12% at 100 micrograms.kg-1 by ip. Sincalide antagonists: lorglumide, devazepide, and L-365,260 antagonized the ileal smooth muscle response to sincalide in a concentration-dependent manner. Their pA2 were 7.30, 10.02, and 7.77, respectively. Lorglumide, devazepide, and L-365,260 inhibited the delaying of gastric emptying evoked by sincalide. The IC50 were 0.11, 0.0064, and 0.66 mg.kg-1, respectively.
Wang
S X
SX
Department of Pharmacology, National Institute of Pharmaceutical Research and Development, Beijing, China.
D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology*; D020109:Devazepide; D005746:Gastric Emptying / Q000187:drug effects; D005769:Gastrointestinal Motility / Q000187:drug effects*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D010671:Phenylurea Compounds; D011377:Proglumide / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors; D012844:Sincalide / Q000037:antagonists & inhibitors*
D001570:Benzodiazepinones; D010671:Phenylurea Compounds; D011949:Receptors, Cholecystokinin; C058121:L 365260; D011377:Proglumide; D020109:Devazepide; C048181:lorglumide; D012844:Sincalide