Synthesis and pharmacological activity of adaprolol enantiomers: a new soft drug for treating glaucoma.

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Adaprolol maleate is a new beta-adrenergic antagonist that is being developed to treat glaucoma. The soft drug was designed to minimize systemic activity through facile inactivation to an inactive metabolite. Studies with other potent beta-adrenergic antagonists indicated that tissue specific receptor differences might be more stringent for selected beta-adrenergic blocking activities and suggested that R enantiomers of traditional beta-blockers should be developed for controlling glaucoma. The present studies demonstrate that the potent ocular hypotensive effects of adaprolol are not stereoselective. In contrast, cardiac effects could be detected after intravenous S(+) adaprolol, but not R(-) adaprolol. The studies confirm that adaprolol functions as a potent beta-adrenergic antagonist. The negligible systemic beta-blocking activity detected with opthalmic administration of adaprolol is consistent with soft drug design.