(E)-Alprenoxime

(E)-Alprenoxime is the isomer of the Alprenoxime. Alprenoxime is a site-activated ocular β-blocker.

Signaling Pathways >> Others >> Others

Research Areas >> Cardiovascular Disease

β blocker[1]

The purpose of the present study is to explore the pharmacological significance of Alprenoxime peripheral /βblocking activity in a non-rodent animal model. Interspecies scaling considerations predict that the doses selected in this study (1 and 5 mg/kg) are pharmacologically comparable or greater than doses used in rodent studies (2 and 6 mg/kg). More importantly, the prolonged ocular antihypertensive effects that are shown with 1% ophthalmic solutions indicate that the i.v. dose tested in the present study is likely to be more than two orders of magnitude greater than probable therapeutic doses[1].

Dogs[1] Seven adult mongrel dogs (20-27 kg) are used in this study. A loading dose of Alprenoxime is administered (1 mg/kg, i.v.) followed by Alprenoxime infusion (150 μg/kg/min) after recording baseline electrophysiological parameters. Cardiac electrophysiological testing is then repeated 10 min after beginning Alprenoxime infusion. Alprenoxime (1 or 5 mg/kg, i.v.) is injected as a bolus injection and cardiac electrophysiological response is monitored. Different dogs with isoproterenol induced tachycardia are evaluated at each Alprenoxime dose.

[1]. Polgar P, et al. Minimal cardiac electrophysiological activity of alprenoxime, a site-activated ocular beta-blocker, in dogs. Life Sci. 1995;56(14):1207-13.

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