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胆碱摄取抑制剂托昔溴铵对大鼠膀胱兴奋性神经支配的影响。

The effect of troxypyrrolidinium, a choline uptake inhibitor, on the excitatory innervation of the rat urinary bladder.

作者信息

Choo L K, Mitchelson F

出版信息

Eur J Pharmacol. 1980 Feb 8;61(3):293-301. doi: 10.1016/0014-2999(80)90131-4.

Abstract

Troxypyrrolidinium, a choline uptake inhibitor, reduced but failed to abolish responses of the rat urinary bladder to electrical stimulation at 1-100 Hz although it reduced acetylcholine output during stimulation at 10 Hz to a level similar to that of spontaneous release. Inhibition of the response to stimulation was more complete at faster rates of stimulation and was partially reversed by choline. Troxypyrrolidinium produced a greater inhibition of the 'tonic' component of the response to electrical stimulation than of the 'phasic' component. Hemicholinium-3 or hyoscine produced a similar selective effect on the 'tonic' component. Hemicholinium-3 also reduced acetylcholine output during electrical stimulation to a similar extent as troxypyrrolidinium but hyoscine increased transmitter output. The results support the concept of a second transmitter in the excitatory innervation of the bladder.

摘要

曲洛吡咯铵是一种胆碱摄取抑制剂,它虽能降低大鼠膀胱对1 - 100赫兹电刺激的反应,但未能完全消除这种反应,尽管它能将10赫兹刺激期间的乙酰胆碱输出量降低到与自发释放水平相似的程度。在更快的刺激速率下,对刺激反应的抑制更为完全,且胆碱能部分逆转这种抑制。曲洛吡咯铵对电刺激反应的“紧张性”成分的抑制作用比对“相性”成分的抑制作用更大。半胱胺酸-3或东莨菪碱对“紧张性”成分产生了类似的选择性作用。半胱胺酸-3在电刺激期间也能将乙酰胆碱输出量降低到与曲洛吡咯铵相似的程度,但东莨菪碱却增加了递质输出量。这些结果支持了膀胱兴奋性神经支配中存在第二种递质的概念。

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