Peripheral benzodiazepine binding sites on striated muscles of the rat: properties and effect of denervation.
In order to test the hypothesis that peripheral benzodiazepine binding sites mediate some direct effects of benzodiazepines on striated muscles, the properties of specific 3H-Ro 5-4864 binding to rat biceps and rat diaphragm homogenates were investigated. In both tissues a single population of sites was found with a KD value of 3 nmol/l. The density of these sites in both muscles was higher than the density in rat brain, but was considerably lower than in rat kidney. Competition experiments indicate a substrate specificity of specific 3H-Ro 5-4864 binding similar to the properties already demonstrated for the specific binding of this ligand to peripheral benzodiazepine binding sites in many other tissues. The properties of these sites in the rat diaphragm are not changed after motoric denervation by phrenicectomy. It is concluded that peripheral benzodiazepine binding sites are not involved in direct effects of benzodiazepines on striated muscles.
D000818:Animals; D001569:Benzodiazepines / Q000378:metabolism* / Q000494:pharmacology; D001570:Benzodiazepinones / Q000378:metabolism; D001665:Binding Sites; D066298:In Vitro Techniques; D008297:Male; D009121:Muscle Denervation; D009132:Muscles / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains
D001570:Benzodiazepinones; D001569:Benzodiazepines; C028513:4'-chlorodiazepam