title: [Characterization of cholecystokinin receptors in gastric chief cells--effect of CCK analogs and CCK receptor antagonists on chief cells].
abstract: In isolated guinea pig gastric chief cells, gastrin-I and cholecystokinin-hexapeptide (CCK-4) stimulated pepsinogen release. However, the efficacies of these two peptide were 51% of that observed with CCK-octapeptide (CCK8). CR1409 and L-364718, both of which are new CCK receptor antagonists in pancreatic acinar cells, also inhibited 10(-8) M CCK8-stimulated pepsinogen release with a half-maximal inhibitory concentration (IC50) observed at 3 x 10(-9) M, respectively. The dose response curve to CCK8 for pepsinogen release shifted to the right in the presence of CR1409 or L-364718. The IC50 of these two antagonists for the CCK8-stimulated increase in cytosolic Ca2+ concentration monitored by Fura-2 were equal to those for CCK8-stimulated pepsinogen release. By contrast, the IC50 of dibutyryl cyclic GMP, a well-known CCK receptor antagonist, for CCK8-stimulated pepsinogen release was less than that for CCK8-stimulated increase in cytosolic Ca2+ concentration. Results suggested that CCK receptors in gastric chief cells are unique and may be different from CCK receptors in other tissues previously reported.
authors: T
authors: T
authors: Matozaki
authors: C
authors: C
authors: Sakamoto
authors: M
authors: M
authors: Nagao
authors: H
authors: H
authors: Nishizaki
authors: Y
authors: Y
authors: Konda
authors: O
authors: O
authors: Nakano
authors: S
authors: S
authors: Baba
mesh_terms: D000818:Animals; D002118:Calcium / Q000378:metabolism; D002478:Cells, Cultured; D002766:Cholecystokinin / Q000031:analogs & derivatives / Q000494:pharmacology*; D003995:Dibutyryl Cyclic GMP / Q000494:pharmacology; D005753:Gastric Mucosa / Q000378:metabolism; D006168:Guinea Pigs; D010435:Pepsinogens / Q000378:metabolism; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013270:Stomach / Q000166:cytology*
chemical_list: D010435:Pepsinogens; D011949:Receptors, Cholecystokinin; D003995:Dibutyryl Cyclic GMP; D002766:Cholecystokinin; D002118:Calcium