Profile of the oppositely acting enantiomers of the dihydropyridine 202-791 in cardiac preparations: receptor binding, electrophysiological, and pharmacological studies.
Profile of the oppositely acting enantiomers of the dihydropyridine 202-791 in cardiac preparations: receptor binding, electrophysiological, and pharmacological studies.
复制标题
心脏制剂中二氢吡啶 202-791 的相反作用对映体的概况：受体结合、电生理学和药理学研究。
DOI：
10.1016/0006-291x(85)91763-2
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发表时间：
1985
影响因子：
3.1
通讯作者：
Brown,AM
中科院分区：
文献类型：
--
作者：
Williams,JS;Grupp,IL;Grupp,G;Vaghy,PL;Dumont,L;Schwartz,A;Yatani,A;Hamilton,S;Brown,AM
在心脏制备物中研究了纯二氢吡啶对映体（+）S202-791和（−）R202-791的受体结合、电生理和变力作用。（+）S202-791结合的KI与收缩力增加和钙电流增加的ED 50相关，后者的作用发生在去极化和静息保持电位下。（−）R202-791结合的KI远低于在−80或−90 mV保持电位下测量的钙电流抑制IC 50和负性肌力作用，但与在−30 mV测量的钙电流抑制IC 50密切相关。因此，（+）S202-791是电压非依赖性钙通道激活剂，（-）R202-791是电压依赖性钙通道抑制剂。
Receptor binding, electrophysiological, and inotropic effects of the pure dihydropyridine enantiomers (+)S202-791 and (−)R202-791 were studied in cardiac preparations. The KIfor (+)S202-791 binding correlated with the ED50's for an increase in contractile force and an increase in calcium current, the latter effect occurring at depolarized as well as resting holding potentials. The KIfor (−)R202-791 binding was much lower than the IC50's for inhibition of calcium current measured at holding potentials of −80 or −90 mV and a negative inotropic effect, but correlated closely with the IC50for inhibition of calcium current measured at −30 mV. Thus, (+)S202-791, is a voltage independent calcium channel activator and (−)R202-791 is a voltage dependent calcium channel inhibitor.