TESTING MODELS OF AGONISM FOR G-PROTEIN-COUPLED RECEPTORS

TESTING MODELS OF AGONISM FOR G-PROTEIN-COUPLED RECEPTORS
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DOI:
10.1016/0165-6147(91)90606-s
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发表时间:
1991-10-01
影响因子:
13.8
通讯作者:
KEEN, M
KEEN, M
中科院分区:
医学1区
文献类型:
--
作者:
KEEN, M

文献摘要

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尽管对于不同激动模型的有效性存在很多争议,但在实践中显然几乎没有什么可供选择的。 然而,大多数测试各种模型的实验都使用经典的分离组织系统。 在这些系统中,测量到的反应与受体激活相去甚远,并且受体事件的特性很可能被更远端的过程所掩盖。 在这篇文章中,Mary Keen 研究了激动剂对 G 蛋白偶联受体激活后反应的影响。 这些数据似乎与任何当前的激动模型不一致。
Despite much debate as to the validity of different models of agonism, there is apparently very little to choose between them in practice. However, most experiments to test the various models have used classical isolated tissue systems. In these systems, the response that is measured is far removed from receptor activation, and it is likely that the properties of the events at the receptor may be masked by more distal processes. In this article, Mary Keen examines the effects of agonists on responses that follow, very closely, activation of G protein-coupled receptors. The data appear to be inconsistent with any of the current models of agonism.