Ciofalo F R
Eur J Pharmacol. 1980 Jul 25;65(2-3):309-12. doi: 10.1016/0014-2999(80)90408-2.
The effects of the antiarrhythmics quinidine, propranolol, procainamide and lidocaine were determined on the specific binding of [3H]clonidine to the alpha 2-adrenergic receptor. Quinidine is effective in decreasing specific [3H]clonidine binding to the alpha 2 receptor within the range of therapeutic blood levels (Ki = 6 x 10 (-8) M). The effectiveness of all compounds tested, with the exception of quinidine and procainamide, correlate with the membrane/buffer partition coefficient, suggesting a relationship with the local anesthetic activity.
研究了抗心律失常药奎尼丁、普萘洛尔、普鲁卡因胺和利多卡因对[³H]可乐定与α₂-肾上腺素能受体特异性结合的影响。在治疗血药浓度范围内(Ki = 6×10⁻⁸ M),奎尼丁可有效降低[³H]可乐定与α₂受体的特异性结合。除奎尼丁和普鲁卡因胺外,所有受试化合物的有效性均与膜/缓冲液分配系数相关,提示其与局部麻醉活性有关。