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Atropine resistance and muscarinic receptors in the rat urinary bladder.

机译:大鼠膀胱中的阿托品抗性和毒蕈碱受体。

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摘要

The action of an anticholinesterase and an antimuscarinic drug upon nerve-induced contractions of the rat urinary bladder were examined during transmural stimulation at 20 Hz. Responses were graded in magnitude by limiting the duration of the stimulus trains. 2 Responses of low magnitude produced by short stimulus trains were unchanged by atropine; however, maximal responses resulting from long stimulus trains were diminished in magnitude and shortened in duration. 3 Responses of small magnitude elicited by short stimulus trains involve muscarinic receptors in close proximity to the neuroeffector junction and are resistant to atropine. 4 Maximal responses elicited by long stimulus trains involve 'junctional' muscarinic receptors as well as receptors located at the periphery of the junction; the 'extrajunctional' receptors are blocked by atropine. 5 Responses of low magnitude produced by short stimulus trains were unaffected by echothiophate; however, the duration of maximal responses resulting from the long stimulus trains was extended. 6 The inhibition of cholinesterase did not increase the occupation of muscarinic receptors by the transmitter; however, after large quantities of transmitter were released by the long stimulus trains the association between the receptors and acetylcholine was prolonged.
机译:在20 Hz的透壁刺激过程中,检查了抗胆碱酯酶和抗毒蕈碱药物对神经诱导的大鼠膀胱收缩的作用。通过限制刺激训练的持续时间,对反应的幅度进行分级。 2阿托品对短刺激序列产生的低响应无影响;然而,长刺激序列产生的最大反应在大小上减少了,持续时间缩短了。 3短刺激序列引起的小反应涉及毒蕈碱受体,该受体与神经效应连接点非常接近,并且对阿托品具有抗性。 4长刺激序列引起的最大反应涉及“接合”毒蕈碱受体以及位于交界处的受体。 “结外”受体被阿托品阻断。 5短刺激序列产生的低强度响应不受硫代硫酸盐的影响。但是,长刺激序列导致的最大反应持续时间延长了。 6胆碱酯酶的抑制作用不会增加受体对毒蕈碱受体的占用;然而,在长期的刺激训练中释放了大量的递质后,受体与乙酰胆碱之间的联系得以延长。

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