Characterization of ^3H-Dihydroalprenolol Binding to β-Adrenergic Receptors of Rat Brain : Two Binding Sites of Racemic Propranolol in Displacement Experiments(Pharmacological)

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The binding affinities of racemic derivatives of propranolol to β-adrenoceptors were examined by means of radioligand binding assay to determine whether racemic propranolol shows biphasic binding to β-adrenoceptors in a displacement experiment. Rat brain was used and the β-adrenoceptor binding assay was carried out with ^3H-dihydroalprenolol as the radioligand. A higher affinity of l-propranolol than of d-propranolol was observed and d- and l-propranolol each gave a uniphasic curve. However, dl-propranolol showed a biphasic curve. Furthermore, a mixture of d- and l-propranolol also showed a biphasic curve. These results imply that β-adrenoceptors of rat brain may bind the d- and l-isomers at distinct sites.
社団法人日本薬学会の論文
1987-07-25