Rothman R B, Barrett R W, Vaught J L
Neuropeptides. 1983 Jul;3(5):367-77. doi: 10.1016/0143-4179(83)90025-2.
The existence of distinct mu and delta opioid receptors is now well accepted. Most investigators favor the hypothesis that these receptors are physically distinct and that the enkephalins are only 2-10 fold selective for the delta receptor. Rothman and Westfall (Mol. Pharmacol. 21:548-557) recently challenged this hypothesis, proposing that at least some population of mu and delta receptors coexist in an opioid receptor complex and that the enkephalins are at least 100 fold selective for the delta receptor. In this paper we describe a generally applicable method we have used to design and analyze ligand binding experiments which distinguish between the two different models.
现在,不同的μ和δ阿片受体的存在已被广泛接受。大多数研究人员支持这样的假说,即这些受体在物理上是不同的,并且脑啡肽对δ受体的选择性仅为2至10倍。罗斯曼和韦斯特福尔(《分子药理学》21:548 - 557)最近对这一假说提出了质疑,他们提出至少有一些μ和δ受体群体共存于一个阿片受体复合物中,并且脑啡肽对δ受体的选择性至少为100倍。在本文中,我们描述了一种普遍适用的方法,我们用它来设计和分析区分这两种不同模型的配体结合实验。