INTERACTIONS OF BEFUNOLOL, A BETA-ADRENERGIC PARTIAL AGONIST, AND ITS DERIVATIVES WITH HIGH AND LOW AFFINITY SITES IN BETA-ADRENOCEPTORS

概要

論文の詳細を見る
Modes of action of befunolol and its derivatives were tested in guinea pig isolated taenia caecum. The pA_2-values of BFE-60 (befunolol), -61 and -69 against isoprenaline, which measures interactions with the high affinity sites on beta-adrenoceptors, were significantly larger than their pD_2-values, which were equal to their pA_2-values against carteolol. Carteolol is a beta-adrenergic partial agonist with higher intrinsic activity, to which the response results from interaction with low affinity sites. These results suggest that BFE-60,-61 and -69 discriminate the high and low affinity sites on beta-adrenoceptors. The pA_2-values of BFE-37,-41,-47 and -72 against isoprenaline were, however, equal to their pD_2-values and pA_2-values against carteolol. These drugs seem to have little or no ability to discriminate between the high and low affinity sites. BFE-55 antagonized isoprenaline but not carteolol suggesting that BFE-55 interacted with only the high affinity sites.
公益社団法人日本薬学会の論文