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两栖动物血管收缩反应中的胆碱能受体机制。

Cholinergic receptor mechanisms in amphibian vasoconstrictor responses.

作者信息

Gambhir S S, Das P K

出版信息

Pharmacology. 1978;16(2):115-20. doi: 10.1159/000136755.

Abstract

The four choline esters, namely acetylcholine, carbachol, methacholine and bethanechol, produced constriction of frog's perfused systemic blood vessels, acetylcholine and carbachol being more potent than methacholine and bethanechol. Pentolinium and dihydroergotamine, in submaximal receptor-blocking doses, also produced a uniform partial inhibition of all choline esters and other agonists including the direct-acting barium chloride. On the other hand atropine markedly inhibited the responses of the four choline esters without affecting the adrenaline and barium responses. Compound AHR-602, a specific ganglionic muscarinic excitatory receptor stimulant, did not produce any effect in these experiments. Eserine in higher doses produced slight vasoconstriction and markedly potentiated acetylcholine responses, but it inhibited partially those of the other three choline esters without significantly affecting adrenaline and barium responses. The results provide strong evidence in favor of involvement of the postganglionic muscarinic receptors only in vasoconstriction after choline esters. There seems to be a considerable nonspecific inhibitory activity in ganglionic and alpha-adrenergic blockers in their submaximal receptor-blocking doses. It may be that in frog the adrenergic and nicotinic receptors are not as well differentiated as muscarinic receptors are. The ganglionic muscarinic receptors also seem to be absent in the frog.

摘要

四种胆碱酯类物质,即乙酰胆碱、卡巴胆碱、醋甲胆碱和氨甲酰甲胆碱,可使蛙的灌注体循环血管收缩,乙酰胆碱和卡巴胆碱的作用比醋甲胆碱和氨甲酰甲胆碱更强。潘托铵和双氢麦角胺在亚最大受体阻断剂量时,也对所有胆碱酯类物质及其他激动剂(包括直接作用的氯化钡)产生一致的部分抑制作用。另一方面,阿托品显著抑制四种胆碱酯类物质的反应,而不影响肾上腺素和钡的反应。化合物AHR - 602,一种特异性神经节毒蕈碱兴奋性受体刺激剂,在这些实验中未产生任何作用。高剂量的毒扁豆碱产生轻微的血管收缩,并显著增强乙酰胆碱的反应,但它部分抑制其他三种胆碱酯类物质的反应,而对肾上腺素和钡的反应无明显影响。这些结果提供了有力证据,支持仅节后毒蕈碱受体参与胆碱酯类物质后的血管收缩。神经节和α - 肾上腺素能阻滞剂在亚最大受体阻断剂量时似乎存在相当大的非特异性抑制活性。在蛙中,肾上腺素能受体和烟碱受体可能不像毒蕈碱受体那样分化良好。蛙中似乎也不存在神经节毒蕈碱受体。

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