Kolajová M, Antalík M, Sturdík E
Institute of Experimental Physics, Slovak Academy of Sciences, Kosice.
Gen Physiol Biophys. 1993 Jun;12(3):213-29.
Spectroscopic evidence is presented which indicates that the anionic uncoupler carbonyl cyanide-4-nitro-2-chloro-phenylhydrazone and the amine local anesthetics form a complex in aqueous solution. The complex formation studies were carried out for several pharmacologically important tertiary amines and some primary amines. Their relative potencies to form a complex with uncoupler have followed the order: procaine < trimecaine < tetracaine < dibucaine < dodecylamine < dicyclohexylamine < hexadecylamine. As to the more lipophilic nature of the complex the emphasized penetration into octanol and reinforced retention into mitochondria was observed. The higher ability of the complex to colapse the mitochondrial membrane potential confirms this fact. The effective concentration of amine local anesthetics to form a complex was correlated with their physicochemical properties namely lipophilicity and acidobasicity. The highest effectivities for complex formation is shown by the most lipophilic and the most ionized molecules of amines. Present results point to the importance of considering the role of amine anesthetic-uncoupler complex in interpreting physiological or ion transport data in which these substances have been used together.
有光谱学证据表明，阴离子解偶联剂羰基氰化物-4-硝基-2-氯苯腙与胺类局部麻醉药在水溶液中形成复合物。对几种具有药理学重要性的叔胺和一些伯胺进行了复合物形成研究。它们与解偶联剂形成复合物的相对效能顺序为：普鲁卡因＜三甲卡因＜丁卡因＜布比卡因＜十二胺＜二环己胺＜十六胺。关于复合物更具亲脂性的性质，观察到其在辛醇中的渗透性增强以及在线粒体中的保留增强。复合物使线粒体膜电位崩溃的能力更强证实了这一事实。胺类局部麻醉药形成复合物的有效浓度与其物理化学性质即亲脂性和酸碱性质相关。胺类中最具亲脂性和最易离子化的分子表现出形成复合物的最高效能。目前的结果表明，在解释同时使用这些物质的生理或离子转运数据时，考虑胺类麻醉药-解偶联剂复合物的作用非常重要。
