Pharmacological studies on CCKB receptors in guinea pig synaptoneurosomes. |
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Authors: | M C Galas N Bernad J Martinez |
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Institution: | Centre CNRS-INSERM de Pharmacologie-Endocrinologie, Faculté de Pharmacie, Montpellier, France. |
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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. |
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