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某些神经节兴奋剂的特异性。

Specificity of some ganglion stimulants.

作者信息

Barlow R B, Franks F

出版信息

Br J Pharmacol. 1971 May;42(1):137-42. doi: 10.1111/j.1476-5381.1971.tb07093.x.

Abstract
  1. The specificity of several ganglion stimulants has been tested on the isolated guinea-pig ileum by measuring the dose ratios produced by concentrations of hexamethonium.2. Most ganglion stimulants are also active at postganglionic receptors, some as blocking agents (for example, lobeline and dimethylphenylpiperazinium), others as agonists (for example, o-aminophenethyltrimethylammonium and, to a lesser extent, nicotine). The most specific ganglion stimulant, with the least activity at postganglionic receptors, was p-aminophenethyltrimethylammonium.3. The affinity constants of lobeline and dimethylphenylpiperazinium for the muscarine sensitive receptors in the guinea-pig ileum are 1.05 x 10(6) and 3.71 x 10(4), respectively.4. The antagonism of p-aminophenethyltrimethylammonium by hexamethonium gave results consistent with competition up to dose ratios of about 20. Such results could also be obtained if the antagonism were non-competitive, however, provided large responses could be obtained with less than about 5% of the receptors in the ganglia activated. The affinity constant of hexamethonium is about 2.6 x 10(5).5. It is suggested that the affinity of hexamethonium can largely be ascribed to hydrophobic bonding.
摘要
  1. 通过测量六甲铵浓度产生的剂量比,在离体豚鼠回肠上测试了几种神经节兴奋剂的特异性。

  2. 大多数神经节兴奋剂在神经节后受体上也有活性,有些作为阻断剂(例如,洛贝林和二甲基苯基哌嗪鎓),另一些作为激动剂(例如,邻氨基苯乙三甲基铵,以及在较小程度上的尼古丁)。在神经节后受体上活性最低的最具特异性的神经节兴奋剂是对氨基苯乙三甲基铵。

  3. 洛贝林和二甲基苯基哌嗪鎓对豚鼠回肠中毒蕈碱敏感受体的亲和常数分别为1.05×10⁶和3.71×10⁴。

  4. 六甲铵对氨基苯乙三甲基铵的拮抗作用在剂量比约为20之前产生了与竞争一致的结果。然而,如果拮抗作用是非竞争性的,只要用不到约5%的神经节受体激活就能获得大的反应,也能得到这样的结果。六甲铵的亲和常数约为2.6×10⁵。

  5. 有人提出,六甲铵的亲和力在很大程度上可归因于疏水键合。

相似文献

1
Specificity of some ganglion stimulants.某些神经节兴奋剂的特异性。
Br J Pharmacol. 1971 May;42(1):137-42. doi: 10.1111/j.1476-5381.1971.tb07093.x.
9
THE GANGLION BLOCKING ACTION OF PROCAINAMIDE.普鲁卡因胺的神经节阻断作用。
Br J Pharmacol Chemother. 1964 Feb;22(1):143-53. doi: 10.1111/j.1476-5381.1964.tb01552.x.

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A search for selective antagonists at M2 muscarinic receptors.对M2毒蕈碱受体选择性拮抗剂的研究。
Br J Pharmacol. 1985 Jun;85(2):427-35. doi: 10.1111/j.1476-5381.1985.tb08878.x.

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