Bepridil (CERM-1978) blockade of action potentials in cultured rat aortic smooth muscle cells.

Bepridil (CERM-1978) blockade of action potentials in cultured rat aortic smooth muscle cells.
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Bepridil (CERM-1978) 阻断培养的大鼠主动脉平滑肌细胞的动作电位。

DOI:
10.1016/0014-2999(81)90382-4
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发表时间:
1981
影响因子:
5
通讯作者:
Sperelakis,N
Sperelakis,N
中科院分区:
医学2区
文献类型:
--
作者:
Mras,S;Sperelakis,N

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用酶分散的大鼠主动脉血管平滑肌(VSM)细胞制备重组培养(原代)。培养7~10d后,用细胞内微电极技术进行研究。细胞处于电静止状态(平均静息电位−为47 mV),细胞外电刺激通常不会引起膜反应。加入10 mM四乙基铵可快速诱导兴奋性,使VSM细胞对电刺激产生钙依赖的动作电位。电反应通常有两个成分,一个是初始的尖峰波,另一个是后来的平台型成分。动作电位的平均波幅为22 mV,但偶尔超调;高原的平均时程(50%复极时)为3.8秒。新的抗心绞痛药苯丙地尔(10−8-10−5M)可剂量依赖性地抑制平台的幅度和时程,阻断动作电位的尖峰成分,但不影响静息电位。这一发现与苯丙地尔作为钙拮抗剂阻止动作电位的产生的观点一致,这一作用可以解释其抗心绞痛的作用。
Reaggregate cultures (primary) were prepared from enzyme-dispersed vascular smooth muscle (VSM) cells from rat aortas. The cultures were incubated for 7–10 days, and then studied by the intracellular microelectrode technique. The cells were electrically quiescent (mean resting potential of −47 mV), and extracellular electrical stimulation usually did not elicit a membrane response. Addition of 10 mM tetraethylammonium rapid induced excitability, allowing the VSM cells to fire Ca2+-dependent action potentials in response to electrical stimulation. The electrical responses often had two components, an intial spike and a later plateau-like component. The action potential spikes had a mean amplitude of 22 mV but occasionally were overshooting; the plateaus had a mean duration (at 50% repolarization) of 3.8 sec. A new anti-anginal agent,, bepridil (10−8–10−5M), depressed the amplitude and duration of the plateau and blocked the spike component of the action potential in a dose-dependent fashion without affecting the resting potential. This finding is consistent with the view that bepridil acts as a Ca2+-antagonistic agent to prevent the generation of the action potentials, and this action can be explain its anti-anginal properties.
新型抗心绞痛药贝普地尔的抗心律失常和电生理作用。
DOI: 10.1097/00005344-198003000-00010
发表时间: 1980
影响因子: 3
作者:
K. Kane;E. Winslow
通讯作者: E. Winslow
维拉帕米可区分心脏慢钠通道的两种药理学类型。
DOI: 10.1016/0014-2999(74)90250-7
发表时间: 1974
影响因子: 5
作者:
M. McLean;K. Shigenobu;N. Sperelakis
通讯作者: N. Sperelakis
原代培养中大鼠主动脉平滑肌细胞重新聚集的动作电位产生。
DOI: 10.1159/000158206
发表时间: 1979
期刊: Blood vessels
影响因子: --
作者:
D. Harder;N. Sperelakis
通讯作者: N. Sperelakis
DOI: 10.1113/jphysiol.1970.sp009286
发表时间: 1970
期刊: The Journal of Physiology
影响因子: --
作者:
Y. Ito;H. Kuriyama;Y. Sakamoto
通讯作者: Y. Sakamoto
DOI: 10.1152/ajpcell.1979.237.1.c75
发表时间: 1979
期刊: The American journal of physiology
影响因子: --
作者:
D. Harder;N. Sperelakis
通讯作者: N. Sperelakis