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Differentiation of beta-adrenoceptors in right atrium, diaphragm and adipose tissue of the rat, using stereoisomers of propranolol, alprenolol, nifenalol and practolol.
Authors:H H Harms  J Zaagsma  J de Vente
Institution:1. Departments of Medicine U.C.L.A. School of Medicine, University of California Los Angeles, California 90024, USA;2. Pharmacology U.C.L.A. School of Medicine, University of California Los Angeles, California 90024, USA;3. Department of Chemistry University of Missouri - Kansas City Kansas City, Missouri 64110, USA
Abstract:2-Diazomorphine-bovine serum albumin (2-DAM-BSA) was prepared by diazotizing p-aminobenzoyl-BSA to morphine. Rabbits immunized with 2-DAM-BSA produced antibodies directed to morphine. A 50 percent reduction in 3H-morphine binding required 4.4 pmol of morphine, and 60, 225, and 350 pmol of normorphine, morphine-3-glucuronide, and codeine, respectively. A radioimmunoassay for brain morphine is described, validated, and used to determine if naloxone alters brain morphine in morphine pelleted mice. The apparent biological half-life of morphine in brain was approximately 52 hours between 24 and 72 hours after pellet implantation, and decreased to 1.25 hours after pellet removal. Naloxone (10 mg/kg) administered 24, 48, or 72 hours after implantation and in doses of 1.0–100 mg/kg administered at 48 hours resulted in either no significant change, or, in a few experiments, increased the brain concentration of morphine. The present experiments could not detect a fraction of total brain morphine that is reduced by naloxone.
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