Effects of diltiazem and verapamil on responses to acetylcholine

Effects of diltiazem and verapamil on responses to acetylcholine
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地尔硫卓和维拉帕米对乙酰胆碱反应的影响

DOI:
--
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发表时间:
1987
影响因子:
7.3
通讯作者:
R. Wachtel
R. Wachtel
中科院分区:
医学2区
文献类型:
--
作者:
R. Wachtel

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1钙通道拮抗剂地尔硫卓和维拉帕米可改变乙酰胆碱(ACh)激活的离子通道的平均寿命。2平均通道寿命是从小鼠半横膈神经肌肉接头处的微型终板电流的衰减相和直接记录培养的BC 3 H1小鼠肿瘤细胞的ACh激活的单通道电流来确定的。3地尔硫卓和维拉帕米均以剂量依赖性方式降低平均通道寿命。对于每种药物,需要高达20 μm-100 μm的浓度才能将通道寿命降低50%。4单通道记录实验也表明,地尔硫卓和维拉帕米在2 μm ~ 5 μm浓度下均能显著降低开放事件的频率。这一发现与受体脱敏的增强一致。
1 The calcium channel antagonists diltiazem and verapamil were found to alter the average lifetime of ion channels activated by acetylcholine (ACh). 2 Average channel lifetime was determined from the decay phase of miniature endplate currents at the neuromuscular junction of mouse hemidiaphragms and from direct recording of single channel currents activated by ACh from BC3H1 mouse tumour cells in culture. 3 Both diltiazem and verapamil reduced average channel lifetime in a dose‐dependent manner. For each drug, concentrations as high as 20 μm‐100 μm were required to decrease channel lifetime by 50%. 4 Single channel recording experiments also showed that both diltiazem and verapamil greatly decreased the frequency of opening events at concentrations as low as 2 μm to 5 μm. This finding is consistent with an enhancement of receptor desensitization.
DOI: --
发表时间: 1981
期刊: The Journal of biological chemistry
影响因子: --
作者:
Sine,SM;Taylor,P
通讯作者: Taylor,P
烟碱乙酰胆碱受体的激活。
DOI: 10.1016/s0006-3495(84)84146-6
发表时间: 1984
影响因子: 3.4
作者:
Sine,SM;Steinbach,JH
通讯作者: Steinbach,JH
钙拮抗剂药物对哺乳动物骨骼肌纤维钙电流的影响。
DOI: --
发表时间: 1986
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
作者:
Walsh,KB;Bryant,SH;Schwartz,A
通讯作者: Schwartz,A