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功能拮抗与协同作用的分析。

An analysis of functional antagonism and synergism.

作者信息

Mackay D

出版信息

Br J Pharmacol. 1981 May;73(1):127-34. doi: 10.1111/j.1476-5381.1981.tb16781.x.

Abstract

1 A method is described for deriving null equations for functional antagonism and synergism. These null equations relate together the concentrations of agonist required to produce equivalent states of a cell or tissue in the presence and in the absence of a functional interactant. 2 In one particular case the null equation leads to conclusions which are very similar to those reached by an earlier author who did not use the null method. However, the null equations give a clearer insight into the quantitative aspects of functional interaction. 3 It is concluded that the use of functional antagonism to estimate affinity constants and relative intrinsic efficacies of agonists has serious limitations. On the other hand, it may be possible to use the null equations, or similar principles, to test the validity of postulated mechanisms and sites of action of functional interactants.

摘要
  1. 本文描述了一种推导功能性拮抗和协同作用零方程的方法。这些零方程将在存在和不存在功能性相互作用剂的情况下,产生细胞或组织等效状态所需的激动剂浓度联系在一起。2. 在一个特定案例中,零方程得出的结论与一位早期作者得出的结论非常相似,该作者未使用零方法。然而,零方程能更清晰地洞察功能性相互作用的定量方面。3. 得出的结论是,使用功能性拮抗来估计激动剂的亲和力常数和相对内在效能存在严重局限性。另一方面,可能可以使用零方程或类似原理来检验功能性相互作用剂假定机制和作用位点的有效性。

相似文献

1
An analysis of functional antagonism and synergism.功能拮抗与协同作用的分析。
Br J Pharmacol. 1981 May;73(1):127-34. doi: 10.1111/j.1476-5381.1981.tb16781.x.
2
A test of the null equation for functional antagonism.功能性拮抗无效方程的检验。
Br J Pharmacol. 1981 May;73(1):135-41. doi: 10.1111/j.1476-5381.1981.tb16782.x.

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Br J Pharmacol Chemother. 1956 Dec;11(4):379-93. doi: 10.1111/j.1476-5381.1956.tb00006.x.
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A general analysis of the receptor-drug interaction.受体-药物相互作用的综合分析。
Br J Pharmacol Chemother. 1966 Jan;26(1):9-16. doi: 10.1111/j.1476-5381.1966.tb01805.x.

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