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大鼠颈上神经节两种毒蕈碱反应的体外药理学差异。

Pharmacological differences between two muscarinic responses of the rat superior cervical ganglion in vitro.

作者信息

Newberry N R, Priestley T

机构信息

Neuroscience Research Centre, Merck Sharp and Dohme Research Laboratories, Harlow, Essex.

出版信息

Br J Pharmacol. 1987 Dec;92(4):817-26. doi: 10.1111/j.1476-5381.1987.tb11386.x.

Abstract

1 Pharmacological differences have been observed between the muscarinic agonist-induced depolarizing and hyperpolarizing responses of the rat isolated superior cervical ganglion. 2 Pirenzepine (0.3 microM) selectively reduced the depolarizing response and unmasked the hyperpolarizing response. No such selectivity was observed with a concentration of N-methylatropine which was equipotent with pirenzepine in antagonizing the depolarizing response. 3 The neuromuscular blocking agents gallamine (10 microM) and pancuronium (3 microM) exhibited the oppositive selectivity to pirenzepine, both dramatically reduced the hyperpolarization but only slightly antagonized the depolarization. 4 The potencies of a range of agonists in evoking the depolarizing and hyperpolarizing responses, the latter in the presence of 0.3 microM pirenzepine, have been determined. Methylfurmethide failed to hyperpolarize the ganglion at concentrations which evoked maximal depolarizations. 5 The muscarinic hyperpolarization did not appear to be mediated by the secondary release of catecholamines. 6 It was concluded that the two muscarinic responses on the rat superior cervical ganglion, the slow depolarization and faster hyperpolarization, are mediated by different muscarinic receptor subtypes.

摘要
  1. 在大鼠离体颈上神经节中,已观察到毒蕈碱激动剂诱导的去极化和超极化反应之间的药理学差异。2. 哌仑西平(0.3微摩尔)选择性降低去极化反应并揭示超极化反应。在拮抗去极化反应方面与哌仑西平等效的N - 甲基阿托品浓度未观察到这种选择性。3. 神经肌肉阻滞剂加拉明(10微摩尔)和泮库溴铵(3微摩尔)对哌仑西平表现出相反的选择性,两者都显著降低超极化但仅轻微拮抗去极化。4. 已确定一系列激动剂在引发去极化和超极化反应时的效力,后者是在存在0.3微摩尔哌仑西平的情况下。甲基呋甲酯在引发最大去极化的浓度下未能使神经节超极化。5. 毒蕈碱超极化似乎不是由儿茶酚胺的二次释放介导的。6. 得出的结论是,大鼠颈上神经节上的两种毒蕈碱反应,即缓慢去极化和更快的超极化,是由不同的毒蕈碱受体亚型介导的。

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