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大鼠膀胱中的阿托品抵抗与毒蕈碱受体

Atropine resistance and muscarinic receptors in the rat urinary bladder.

作者信息

Carpenter F G

出版信息

Br J Pharmacol. 1977 Jan;59(1):43-9. doi: 10.1111/j.1476-5381.1977.tb06975.x.

Abstract

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.

摘要

在20赫兹的跨壁刺激过程中,研究了抗胆碱酯酶药和抗毒蕈碱药对大鼠膀胱神经诱发收缩的作用。通过限制刺激串的持续时间来对反应幅度进行分级。2 短刺激串产生的低幅度反应不受阿托品影响;然而,长刺激串产生的最大反应幅度减小且持续时间缩短。3 短刺激串引发的小幅度反应涉及紧邻神经效应器接头的毒蕈碱受体,且对阿托品有抗性。4 长刺激串引发的最大反应涉及“接头处”毒蕈碱受体以及位于接头周边的受体;“接头外”受体被阿托品阻断。5 短刺激串产生的低幅度反应不受依可碘酯影响;然而,长刺激串产生的最大反应的持续时间延长。6 胆碱酯酶的抑制并未增加递质对毒蕈碱受体的占据;然而,在长刺激串释放大量递质后,受体与乙酰胆碱之间的结合延长。

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本文引用的文献

1
RESPONSES OF THE RAT URINARY BLADDER IN SITU TO DRUGS AND TO NERVE STIMULATION.大鼠膀胱原位对药物及神经刺激的反应
Br J Pharmacol Chemother. 1965 Apr;24(2):591-600. doi: 10.1111/j.1476-5381.1965.tb01750.x.
2
OBSERVATIONS ON AN ISOLATED, INNERVATED PREPARATION OF RAT URINARY BLADDER.对大鼠离体神经支配膀胱制备物的观察
Br J Pharmacol Chemother. 1965 Feb;24(1):178-88. doi: 10.1111/j.1476-5381.1965.tb02093.x.
10
Atropine-resistance of the urinary bladder innervation.膀胱神经支配的阿托品抵抗
J Pharm Pharmacol. 1971 Mar;23(3):222-5. doi: 10.1111/j.2042-7158.1971.tb08649.x.

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