依福地平的R(-)-对映体可阻断豚鼠心室肌中的T型钙电流，但不阻断L型钙电流。
The R(-)-enantiomer of efonidipine blocks T-type but not L-type calcium current in guinea pig ventricular myocardium.
作者信息
Tanaka Hikaru, Komikado Chisa, Shimada Hideaki, Takeda Kentaro, Namekata Iyuki, Kawanishi Toru, Shigenobu Koki
机构信息
Department of Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba 274-8510, Japan.
出版信息
J Pharmacol Sci. 2004 Dec;96(4):499-501. doi: 10.1254/jphs.rcj04001x. Epub 2004 Dec 15.
In guinea pig ventricular cardiomyocytes, the R(-)-enantiomer of efonidipine concentration-dependently blocked T-type Ca2+ current with 85% inhibition at 1 microM. In contrast, R(-)-efonidipine (1 microM) had no effect on the L-type Ca2+ current and Ca2+ transient in cardiomyocytes and contractile force in papillary muscles. Thus, R(-)-efonidipine is a highly selective blocker of the T-type Ca2+ current in native myocardia.
在豚鼠心室肌细胞中，依福地平的R(-)-对映体浓度依赖性地阻断T型Ca2+电流，在1微摩尔时抑制率达85%。相比之下，R(-)-依福地平（1微摩尔）对心肌细胞中的L型Ca2+电流和Ca2+瞬变以及乳头肌收缩力无影响。因此，R(-)-依福地平是天然心肌中T型Ca2+电流的高度选择性阻断剂。
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