β-Adrenoceptor antagonists and human sperm motility

Abstract

Several beta-adrenoceptor blocking agents have been evaluated for spermicidal activity using a transmembrane migration method. The rank order of potency of the active compounds was: penbutolol greater than (+)-propranolol greater than bufuralol greater than (-)-alprenolol greater than oxprenolol greater than metoprolol. Atenolol, pindolol, practolol, tolamolol were without activity. The observed potencies of spermicidal activity are believed to be unrelated to beta-blocking activities, and we have shown that whilst they are not predictable from lipid solubility or nonspecific membrane properties of the compound alone, both these aspects appear to play a role in this pharmacological activity.

The Effect of Propranolol on Sperm Parameters, CatSper 2 Gene and Protein Expression, and Oxidative Stress in Adult Mice

“…Another study reported that damages of penbutolol and propranolol on sperm are greater than alprenolol, oxprenolol and metoprolol [6].…”

“…The in-vitro administration of propranolol have significantly reduced sperm motility [5][6][7] and it had adverse effects on sperm capacity, acrosome reaction, and sperm penetration in oocyte [8]. On the other hand, no study has been conducted about the effect of propranolol on CatSper gene and protein expression.…”

β‐Adrenergic antagonists and carp (Cyprinus carpio L.) sperm motility

“…Adrenergic monoamines possibly modulate sperm motility by both a calcium-dependent and a cyclic nucleotide-dependent mechanism. In mammals most of the results indicate that B-adrenergic antagonists may act on sperm motility independently of /&receptor blockade, although their actual action mechanisms still have to be elucidated (Stanger, 1983;Curtis-Prior & Gadd, 1990).…”

Comparative effects of (+)-propranolol and nonoxynol-9 on human sperm motility in-vitro

“…Another group of compounds, the so-called membrane stabilizing agents, also inhibit sperm motility by exerting a non-specific action on membranes, including local anaesthetic or quinidine-like activity, physical stabilization of membranes and protection against cell lysis (Smith 1982). The P-adrenoceptor antagonist, propranolol, in addition to its specific therapeutic action in cardiovascular disease, and a t concentrations in the millimolar range, displays membrane stabilizing activity and inhibits sperm motility (Peterson & Freund 1973;Curtis-Prior & Gadd 1990). Interestingly, the racemic mixture and both isomers of propranolol possess non-specific membrane effects and exhibit spermicidal activities, but the (+)-isomer is only a weak P-adrenoceptor antagonist (Barrett & Cullum 1968), so we have investigated the effects of (+)-propranolol and nonoxynol-9, alone and in combination, on human sperm motility, in-vitro.…”