Variable receptor affinity hypothesis.
Variable receptor affinity hypothesis.
复制标题
可变受体亲和力假说。
DOI：
10.1096/fasebj.3.6.2564831
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发表时间：
1989
期刊：
影响因子：
--
通讯作者：
Shreeve,SM
中科院分区：
文献类型：
--
作者：
Bevan,JA;Bevan,RD;Shreeve,SM
在实验室中常用的三种哺乳动物的多种动脉对去甲肾上腺素（NE）的收缩反应的测量提供了证据，表明组织敏感性和α1-肾上腺素受体对NE的亲和力在几个数量级的范围内协变。定量关系表明，亲和力的变化可以在很大程度上解释在许多情况下发现的灵敏度的变化。此外，有人认为，亲和力的变化似乎是连续的，因此不提供受体类型细分的基础。也有证据表明，肾上腺素能拮抗剂的亲和力可以在组织中显着变化。可能解释这种变化的因素包括受体化学结构、局部膜微环境和许多细胞内过程的差异。已提出可变受体亲和力的假说。如果它是正确的，那么受体亲和力的变化是一个重要的功能相关变量，可以解释组织对循环激素反应的选择性，并可能代表完整生物体和疾病的变化机制。Bevan，J. A.;贝万河D.的; Shreeve，S. M.可变受体亲和力假说.FASEB J.3：1696 - 1704; 1989.
Measurements of the contractile response to norepinephrine (NE) of a variety of arteries of three mammalian species that are commonly used in the laboratory provide evidence that tissue sensitivity and affinity of the α1‐adrenoceptor for NE covary over a range of several orders of magnitude. The quantitative relationship suggests that variation in affinity can, to a great extent, account for the variation in sensitivity found in a number of circumstances. Furthermore, it is argued that the variation in affinity appears to be continuous and thus does not provide a basis for receptor type subdivision. There is also evidence that adrenergic antagonist affinity can vary significantly in tissues. The factors that might account for this variation include differences in receptor chemical structure, in the local membrane microenvironment, and in a number of intracellular processes. A hypothesis of variable receptor affinity has been proposed. If it is correct, then variation in receptor affinity is an important functionally relevant variable that could account for selectivity of tissue responses to circulating hormones and may represent a mechanism of change in the intact organism and in disease.—Bevan, J. A.; Bevan, R. D.; Shreeve, S. M. Variable receptor affinity hypothesis.FASEB J.3: 1696‐1704; 1989.