Curtis-Prior P B, Gadd A L
Cambridge Research Institute, Histon, UK.
J Pharm Pharmacol. 1990 Mar;42(3):220-2. doi: 10.1111/j.2042-7158.1990.tb05395.x.
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.
已使用跨膜迁移方法对几种β-肾上腺素能受体阻滞剂的杀精活性进行了评估。活性化合物的效力排序为:喷布洛尔大于(+)-普萘洛尔大于丁呋洛尔大于(-)-阿普洛尔大于氧烯洛尔大于美托洛尔。阿替洛尔、吲哚洛尔、普拉洛尔、托拉洛尔无活性。观察到的杀精活性效力被认为与β-阻断活性无关,并且我们已经表明,虽然仅根据化合物的脂溶性或非特异性膜性质无法预测这些效力,但这两个方面似乎在这种药理活性中都起作用。