Kurachi Y, Nakajima T, Sugimoto T
Naunyn Schmiedebergs Arch Pharmacol. 1987 Feb;335(2):216-8. doi: 10.1007/BF00177726.
Postsynaptic mechanisms underlying the anticholinergic effects of quinidine were examined in single atrial cells, using the tight-seal whole-cell recording technique. The solution in the glass pipettes contained guanosine-5'-triphosphate (GTP) or guanosine-5'-O-(3-thiotriphosphate) (GTP-gamma S, a non-hydrolyzable GTP analogue). In both cases, acetylcholine (ACh), applied to the bath, induced a specific K+ current. In GTP-loaded cells, quinidine in the bath solution depressed the ACh-induced K+ current concentration-dependently. Atropine also blocked the K+ current. On the other hand, in GTP-gamma S-loaded cells, the ACh-induced current was not blocked by atropine and persisted even when ACh was washed out from the bath, indicating that GTP-gamma S causes uncoupling of the K+ channels from the muscarine receptors. Quinidine, however, did depress the increased K+ current concentration-dependently. The percent inhibition curves for quinidine to depress the K+ current were very similar between GTP-loaded and GTP-gamma S-loaded cells. From these observations, we suggest that direct inhibition of the muscarine receptor-activated K+ channel current by quinidine, and not blockade of the muscarine receptor itself, is mainly responsible for the anticholinergic effects of the drug in atrial myocytes.
采用全细胞封接记录技术,在单个心房细胞中研究了奎尼丁抗胆碱能作用的突触后机制。玻璃微电极内的溶液含有鸟苷-5'-三磷酸(GTP)或鸟苷-5'-O-(3-硫代三磷酸)(GTP-γS,一种不可水解的GTP类似物)。在这两种情况下,施加于浴槽中的乙酰胆碱(ACh)均可诱导出一种特异性钾电流。在加载GTP的细胞中,浴槽溶液中的奎尼丁浓度依赖性地抑制ACh诱导的钾电流。阿托品也可阻断该钾电流。另一方面,在加载GTP-γS的细胞中,ACh诱导的电流不受阿托品阻断,即使将ACh从浴槽中冲洗掉,该电流仍持续存在,这表明GTP-γS可使钾通道与毒蕈碱受体解偶联。然而,奎尼丁确实浓度依赖性地抑制了增加的钾电流。在加载GTP的细胞和加载GTP-γS的细胞中,奎尼丁抑制钾电流的百分比抑制曲线非常相似。根据这些观察结果,我们认为奎尼丁对毒蕈碱受体激活的钾通道电流的直接抑制作用,而非对毒蕈碱受体本身的阻断作用,是该药物在心房肌细胞中产生抗胆碱能作用的主要原因。