Quantitative assessment of central beta 1- and beta 2-adrenoceptor regulation using CGP 20712 A.
The use of 100 nM CGP 20712 A (1-[2-((3-carbamoyl-4-hydroxy)phenoxy)ethylamino]-3-[4-(1-methyl-4- trifluoromethyl-2-imidazolyl)phenoxy]-2-propanol methanesulfonate), a specific beta 1-adrenoceptor antagonist, in an in vitro [3H]dihydroalprenolol binding assay simplified the detection of drug-induced alterations in central beta 1- and beta 2-adrenoceptor density. Injection of rats with DSP-4 (N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine hydrochloride), a selective noradrenergic neurotoxin, caused an increase in neocortical and hippocampal beta 1-adrenoceptor density. Subchronic infusion of desipramine, a noradrenaline uptake inhibitor, effected a decrease in neocortical and hippocampal beta 1-adrenoceptor density. Subchronic infusion of clenbuterol, a centrally acting beta-adrenoceptor agonist, appeared to decrease striatal beta 2-adrenoceptor density. The results are discussed in terms of the quantitation and regulation of central beta-adrenoceptors.
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects; D004082:Dihydroalprenolol; D007093:Imidazoles / Q000494:pharmacology*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*
D000319:Adrenergic beta-Antagonists; D007093:Imidazoles; D011943:Receptors, Adrenergic, beta; D004082:Dihydroalprenolol; C049763:CGP 20712A