title: Cholecystokinin antagonistic activities of loxiglumide.
abstract: Cholecystokinin (CCK) antagonistic activities of loxiglumide ((+/-)-4-(3,4-dichlorobenzamido)-N-(3-methoxypropyl)-N-pentylgl utaramic acid, CR1505, CAS 107097-80-3) were investigated in the gastrointestine and gallbladder in vivo. Intravenous administration of loxiglumide antagonized the CCK-induced reduction of gastric emptying in rats, acceleration of intestinal transport in mice, increase in ileal motility in rabbits, gallbladder contraction in guinea pigs and acceleration of gallbladder emptying in mice. Orally administered loxiglumide also antagonized the CCK-induced gallbladder emptying in mice. Furthermore, egg yolk-stimulated gallbladder emptying in mice was also inhibited by loxiglumide, indicating that this agent antagonizes not only exogenous but also endogenous CCK. These results demonstrate that loxiglumide is an intravenously and orally effective, potent CCK antagonist.
authors.affiliation: Pharmacological Research Laboratory, Tokyo Tanabe Co., Ltd., Japan.
authors.forename: K
authors.initials: K
authors.lastname: Wakatsuki
authors.forename: T
authors.initials: T
authors.lastname: Saito
authors.forename: M
authors.initials: M
authors.lastname: Saeki
authors.forename: K
authors.initials: K
authors.lastname: Ninomiya
authors.forename: H
authors.initials: H
authors.lastname: Kasai
authors.forename: K
authors.initials: K
authors.lastname: Kimura
authors.forename: M
authors.initials: M
authors.lastname: Fujii
mesh_terms: D000818:Animals; D002766:Cholecystokinin / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D005704:Gallbladder / Q000187:drug effects; D016473:Gallbladder Emptying / Q000187:drug effects; D005746:Gastric Emptying / Q000187:drug effects; D005769:Gastrointestinal Motility / Q000187:drug effects; D005772:Gastrointestinal Transit / Q000187:drug effects; D006168:Guinea Pigs; D006727:Hormone Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D066298:In Vitro Techniques; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D011377:Proglumide / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D006727:Hormone Antagonists; C053737:loxiglumide; D002766:Cholecystokinin; D011377:Proglumide