Calcium channel agonist and antagonist effects of the stereoisomers of the dihydropyridine 202-791.
Calcium channel agonist and antagonist effects of the stereoisomers of the dihydropyridine 202-791.
复制标题
二氢吡啶 202-791 立体异构体的钙通道激动剂和拮抗剂作用。
DOI：
10.1016/0006-291x(85)90393-6
复制
发表时间：
1985
影响因子：
3.1
通讯作者：
Sanguinetti,MC
中科院分区：
文献类型：
--
作者：
Kongsamut,S;Kamp,TJ;Miller,RJ;Sanguinetti,MC
研究了新型二氢吡啶202-791的纯立体异构体对神经和心肌电压敏感钙通道的影响。（−）-异构体阻断NG108-15神经母细胞瘤x胶质瘤细胞对45ca2 +的去极化诱导摄取，阻断PC12细胞对[3H]-去甲肾上腺素的去极化诱导释放，降低豚鼠乳头肌慢反应动作电位的Vmax。相反，(+)-异构体增强了这些相同的过程。在乳头肌中，在较低的刺激频率下观察到更大的慢反应增强。因此，202-791的（−）和（+）立体异构体可以分别被证明是钙通道拮抗剂和激动剂。
The effects of the pure stereoisomers of the novel dihydropyridine 202–791 on voltage sensitive calcium channels in nerve and cardiac muscle were examined. The (−)-isomer blocked depolarization-induced uptake of45Ca2+into NG108-15 neuroblastoma x glioma cells, blocked the depolarization-induced release of [3H]-norepinephrine from PC12 cells and reduced the Vmax of the slow response action potential recorded from guinea pig papillary muscle. In contrast, the (+)-isomer enhanced these same processes. In papillary muscle, greater enhancement of the slow responses was observed at lower stimulation frequencies. Thus, the (−) and (+) stereoisomers of 202–791 can be shown to be calcium channel antagonist and agonist respectively.