Abstract
Celiprolol is a novel β-adrenoceptor blocking drug that displays clinically favorable effects on glucose and lipid metabolism. Because some other atypical β-adrenoceptor blocking drugs have been described to act as agonists on β 3-adrenoceptors, we aimed to investigate the effects of celiprolol on brown fat and β 3-adrenoceptors. Chronic treatment of obese fa/fa Zucker rats with celiprolol (50 mg/kg/day orally for 20 days) increased GDP binding to brown fat mitochondria by 1.5-fold, whereas β 3-adrenoceptor agonist ZD7114 ((S)-4-[2-[(2-hydroxy-3-phenoxypropyl)amino]ethoxy]-N-(2-methoxyethyl)phenoxyacetamide, 3 mg/kg/day) increased the binding by 3.3-fold. Weight gain was reduced by 19% due to decreased water and food intakes in celiprolol-treated rats. Celiprolol did not activate lipolysis in rat adipocytes in vitro or stimulate human β 3-adrenoceptors expressed in Chinese hamster ovary cells as measured with Cytosensor microphysiometer. Therefore, celiprolol does not seem to activate brown fat via β 3-adrenoceptors.
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