Types of opioid receptors: relation to antinociception.
Types of opioid receptors: relation to antinociception.
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阿片受体的类型：与抗伤害作用的关系。
DOI：
10.1098/rstb.1985.0029
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发表时间：
1985
期刊：
影响因子：
--
通讯作者：
Paterson,SJ
中科院分区：
文献类型：
--
作者：
Kosterlitz,HW;Paterson,SJ
内源性阿片肽来源于三大前体。前阿片皮质素和前脑啡肽产生[甲硫氨酸]脑啡肽、羧基扩展的[甲硫氨酸]脑啡肽和[亮氨酸]脑啡肽。前强啡肽的片段都是羧基延伸的[Leu]-脑啡肽。对于分析不同内源性阿片肽的生理功能，有三种方法是重要的。首先，由于这些多肽与不止一个μ-，δ和K结合位点相互作用，从而与它们的受体相互作用，因此有必要合成仅与其中一个结合的多肽或非肽。就麻醉性镇痛剂而言，吗啡满足这些条件，因为它几乎只与μ受体相互作用。其次，要求拮抗剂只对一种阿片受体具有选择性，即使在高浓度使用时也是如此。最后，重要的是找到神经系统中只有一种阿片受体的限定区域。现在已经知道，在兔的小脑中，阿片受体几乎完全是P型的，而在豚鼠的小脑中，它们几乎完全是K型的。
The endogenous opioid peptides are derived from three large precursors. Pro-opiocortin and proenkephalin yield [Met]enkephalin, carboxy-extended [Met]enkephalins and [Leu]enkephalin. The fragments of prodynorphin are all carboxy-extended [Leu]- enkephalins. Three approaches are of importance for an analysis of the physiological functions of the different endogenous opioid peptides. First, since these peptides interact with more than one of the μ-, δ- and K-binding sites and thus with their receptors, it is necessary to synthesize peptides or non-peptides, which bind to only one of the sites. As far as narcotic analgesics are concerned, morphine fulfils these conditions since it interacts almost exclusively with the μ-receptor. Secondly, antagonists are required that are selective for only one of the opioid receptors, even when used in high concentrations. Finally, it is important to find circumscribed areas in the nervous system that possess only one type of opioid receptor. It is now known that in the rabbit cerebellum the opioid receptors are almost exclusively of the p-type whereas in the guinea-pig cerebellum they are almost exclusively of the K-type.