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豚鼠盲肠带肠平滑肌中对维拉帕米敏感和不太敏感的收缩

Verapamil-sensitive and less sensitive contractions in the intestinal smooth muscle of the guinea-pig taenia caeci.

作者信息

Karaki H, Mitsui M

机构信息

Department of Veterinary Pharmacology, Faculty of Agriculture, University of Tokyo, Japan.

出版信息

Jpn J Pharmacol. 1988 Apr;46(4):325-30. doi: 10.1254/jjp.46.325.

Abstract

Effect of verapamil, a Ca2+ channel blocker, on the contractions in the intestinal smooth muscle of taenia isolated from guinea-pig caecum was examined. In normal medium, 10 mM-80 mM KCl or 10(-7) M-10(-5) M carbachol induced a transient contraction followed by a sustained one. When the muscle strips were treated with a Ca2+-free solution for 2 min, these stimulants failed to induce contraction except an initial transient contraction induced by 10(-6) M-10(-5) M carbachol. Cumulative application of verapamil during the sustained contraction induced muscle relaxation. Higher concentration of verapamil was needed to inhibit the sustained contraction induced by 10 mM or 20 mM K+ than that induced by 40 mM or 80 mM K+. Similarly, the sensitivity to verapamil of the sustained contraction induced by 10(-7) M carbachol was lower than that induced by 10(-6) M or 10(-5) M carbachol. In the presence of verapamil, addition of either high K+ or carbachol induced an initial transient contraction, although the sustained contraction was strongly inhibited. These results suggest that high K+ and carbachol activate two types of Ca2+ channels; lower concentrations of the stimulants open the channel which is less sensitive to verapamil, and higher concentrations open the channel which is more sensitive to verapamil.

摘要

研究了钙离子通道阻滞剂维拉帕米对从豚鼠盲肠分离的带绦虫肠道平滑肌收缩的影响。在正常培养基中,10 mM - 80 mM氯化钾或10(-7)M - 10(-5)M卡巴胆碱诱导短暂收缩,随后是持续收缩。当肌肉条用无钙溶液处理2分钟时,除了10(-6)M - 10(-5)M卡巴胆碱诱导的初始短暂收缩外,这些刺激剂未能诱导收缩。在持续收缩期间累积应用维拉帕米可诱导肌肉松弛。抑制10 mM或20 mM钾诱导的持续收缩所需的维拉帕米浓度高于40 mM或80 mM钾诱导的持续收缩所需的浓度。同样,10(-7)M卡巴胆碱诱导的持续收缩对维拉帕米的敏感性低于10(-6)M或10(-5)M卡巴胆碱诱导的持续收缩。在维拉帕米存在的情况下,添加高钾或卡巴胆碱均诱导初始短暂收缩,尽管持续收缩受到强烈抑制。这些结果表明,高钾和卡巴胆碱激活两种类型的钙通道;较低浓度的刺激剂打开对维拉帕米不太敏感的通道,较高浓度的刺激剂打开对维拉帕米更敏感的通道。

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