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在拮抗剂亲和力常数估计中不同激动剂的使用。

The use of different agonists in antagonist affinity constant estimations.

作者信息

Roberts F, Stephenson R P

出版信息

Br J Pharmacol. 1976 Jul;57(3):395-8. doi: 10.1111/j.1476-5381.1976.tb07679.x.

Abstract

1 The affinities of 4 muscarinic antagonists were estimated on intact pieces of guinea-pig ileum using the agonists carbachol and pentyl trimethylammonium both in separate experiments and in the same experiment. 2 The apparent affinities were slightly but consistently higher when estimated from the responses produced by pentyl trimethylammonium than when estimated from the responses produced by carbachol. 3 This difference was greatly reduced or abolished if totally denervated logitudinal muscle strips were used rather than intact pieces of ileum. It is therefore suggested that the difference is due to the presence of receptors in the ganglionic layer. 4 To explain the difference in apparent affinity of the antagonists these receptors can not be identical to the muscarinic receptors on the smooth muscle. 5 In addition they can not be nicotinic ganglionic receptors as the difference did not appear to be affected by the presence or absence of hexamethonium.

摘要
  1. 在豚鼠回肠完整组织上,分别使用激动剂卡巴胆碱和戊基三甲基铵进行实验,以及在同一实验中同时使用这两种激动剂,对4种毒蕈碱拮抗剂的亲和力进行了评估。2. 从戊基三甲基铵产生的反应估算出的表观亲和力,比从卡巴胆碱产生的反应估算出的表观亲和力略高且较为稳定。3. 如果使用完全去神经的纵行肌条而非完整的回肠组织,这种差异会大大减小或消除。因此,有人认为这种差异是由于神经节层中存在受体所致。4. 为了解释拮抗剂表观亲和力的差异,这些受体与平滑肌上的毒蕈碱受体不同。5. 此外,它们也不可能是烟碱型神经节受体,因为这种差异似乎不受六甲铵存在与否的影响。

相似文献

6
Cholinoceptive sites in the ganglia of myenteric plexus subserving the peristaltic reflex of guinea-pig isolated ileum.
Neuropharmacology. 1974 Nov;13(10-11):1091-4. doi: 10.1016/0028-3908(74)90100-2.

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