title: Pharmacological studies on CCKB receptors in guinea pig synaptoneurosomes.
abstract: Preliminary studies on CCK receptors in the central nervous system were carried out on guinea pig cerebral cortical synaptoneurosome preparations. In binding assays, the range of affinity of CCK-8, Boc-[Nle28,Nle31]CCK-7, a potent CCK analog, Boc-[Leu31]CCK-4 and of the two benzodiazepine CCK receptor antagonists L-365,260 and MK-329, is in agreement with the presence of CCKB receptors on this model. The effects of Boc-[Nle28,Nle31]CCK-7 on inositol phosphates, cAMP accumulation and 45Ca2+ efflux were investigated. Neither inositol phosphate nor cAMP accumulations could be observed. On the other hand, evidence of Boc-[Nle28,Nle31]CCK-7-, CCK-8- and Boc-[Leu31]CCK-4-induced 45Ca2+ efflux was found in a dose-dependent manner. The CCKB-selective receptor antagonist L-365,260 and, with a weaker efficiency, the CCKA-selective receptor antagonist MK-329, are able to block a maximal effect of Boc-[Nle28,Nle31]CCK-7-induced 45Ca2+ efflux, suggesting that CCKB receptors may regulate calcium ion mobilization.
authors.affiliation: Centre CNRS-INSERM de Pharmacologie-Endocrinologie, Faculté de Pharmacie, Montpellier, France.
authors.forename: M C
authors.initials: MC
authors.lastname: Galas
authors.forename: N
authors.initials: N
authors.lastname: Bernad
authors.forename: J
authors.initials: J
authors.lastname: Martinez
mesh_terms: D000818:Animals; D001570:Benzodiazepinones / Q000378:metabolism / Q000494:pharmacology; D001665:Binding Sites; D002118:Calcium / Q000378:metabolism*; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D002766:Cholecystokinin / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D020109:Devazepide; D006168:Guinea Pigs; D007295:Inositol Phosphates / Q000378:metabolism; D008297:Male; D010446:Peptide Fragments / Q000378:metabolism / Q000494:pharmacology; D010671:Phenylurea Compounds; D011949:Receptors, Cholecystokinin / Q000378:metabolism*; D012844:Sincalide / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D013574:Synaptosomes / Q000187:drug effects* / Q000378:metabolism; D013758:Tetragastrin / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology
chemical_list: D001570:Benzodiazepinones; D007295:Inositol Phosphates; D010446:Peptide Fragments; D010671:Phenylurea Compounds; D011949:Receptors, Cholecystokinin; D013758:Tetragastrin; C060807:butyloxycarbonyl-tryptophyl-leucyl-aspartyl-phenylalaninamide; C058121:L 365260; D002766:Cholecystokinin; C047716:cholecystokinin (27-33), tert-butyloxycarbonyl-Nle(28,31)-; D000242:Cyclic AMP; D020109:Devazepide; D012844:Sincalide; D002118:Calcium