Soft drugs. 7. Soft. beta.-blockers for systemic and ophthalmic use

…, AA El-Koussi, M Kano, MM Khalifa

Index: Bodor, Nicholas; El-Koussi, Alaaeldin A.; Kano, Masanobu; Khalifa, Mohamed M. Journal of Medicinal Chemistry, 1988 , vol. 31, # 8 p. 1651 - 1656

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Citation Number: 56

Abstract

The “inactive metabolite approach” was used to design a series of “soft” drugs derived from the acidic metabolite of metoprolol. Pharmacokinetic and pharmacodynamic properties of these novel “soft” 0-adrenoceptor antagonists were determined: half-lives in human blood ranged from 5 to 754 min. The rates of in vivo disappearance of representative slow, medium, and fast hydrolyzing esters were determined in rats. In each case rapid and ...