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A potent and selective endogenous agonist for the mu-opiate receptor

机译：一种有效的选择性阿片受体内源性激动剂

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Peptides have been identified in mammalian brain that are considered to be endogenous agonists for the delta (enkephalins) and kappa (dynorphins) opiate receptors, but none has been found to have any preference for the mu receptor. Because morphine and other compounds that are clinically useful and open to abuse act primarily at the mu receptor, it could be important to identify endogenous peptides specific for this site. Here we report the discovery and isolation from brain of such a peptide, endomorphin-1 (Tyr-Pro-Trp-Phe-NH2), which has a high affinity (Ki = 360 pM) and selectivity (4,000- and 15,000-fold preference over the delta and kappa receptors) for the mu receptor. This peptide is more effective than the mu-selective analogue DAMGO in vitro and it produces potent and prolonged analgesia in mice. A second peptide, endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), which differs by one amino acid, was also isolated. The new peptides have the highest specificity and affinity for the mu receptor of any endogenous substance so far described and they may be natural ligands for this receptor.
机译：在哺乳动物脑中已鉴定出被认为是δ（脑啡肽）和κ（强啡肽）阿片受体的内源性激动剂的肽，但没有发现对mu受体有任何偏好。由于吗啡和其他在临床上有用且易于滥用的化合物主要作用于mu受体，因此鉴定对该位点特异性的内源肽可能很重要。在这里，我们报告发现并从大脑中分离出了这种肽，endomorphin-1（Tyr-Pro-Trp-Phe-NH2），它具有高亲和力（Ki = 360 pM）和选择性（4,000和15,000倍的优先选择） mu受体的δ和kappa受体）。该肽在体外比mu选择性类似物DAMGO更有效，并且在小鼠中产生有效且延长的镇痛作用。还分离了第二个肽，endomorphin-2（Tyr-Pro-Phe-Phe-NH2），它们相差一个氨基酸。迄今为止，新肽对任何内源物质的mu受体都具有最高的特异性和亲和力，它们可能是该受体的天然配体。

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