Adachi-Akahane S, Amano Y, Okuyama R, Nagao T
Department of Toxicology and Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Jpn J Pharmacol. 1993 Mar;61(3):263-6. doi: 10.1254/jjp.61.263.
A quaternary derivative of diltiazem (quat-DTZ) was tested to determine whether diltiazem approaches L-type Ca2+ channels from the outside or inside of the cell membrane. In single ventricular myocytes, both extra- and intracellular application of quat-DTZ effectively blocked the L-type Ca2+ channel current, whereas D890 was effective only when applied intracellularly. These results strongly suggest that diltiazem binds to the channel from the outside as well as the inside of the membrane in a manner different from that of phenylalkylamines.
对一种地尔硫䓬的季铵衍生物（季铵 - 地尔硫䓬）进行了测试，以确定地尔硫䓬是从细胞膜外侧还是内侧接近L型Ca2 +通道。在单个心室肌细胞中，细胞外和细胞内应用季铵 - 地尔硫䓬均能有效阻断L型Ca2 +通道电流，而D890仅在细胞内应用时有效。这些结果有力地表明，地尔硫䓬以与苯烷基胺不同的方式从细胞膜外侧以及内侧与通道结合。
