Singh V K, Bajpai K, Biswas S, Haq W, Khan M Y, Mathur K B
Department of Immunology, Sanjay Gandhi Post-Graduate Institute of Medical Sciences, Lucknow, India.
Neuroimmunomodulation. 1997 Sep-Dec;4(5-6):285-97. doi: 10.1159/000097349.
Endogenous opioid peptides and opiates like morphine produce their pharmacological effects through the membrane bound opioid receptors. These receptors belong to a superfamily of G-protein-coupled receptors, all of which possess seven membrane-spanning regions. Structure-activity relationship studies of opioids opened up new avenues for the pharmacological characterization of the opioid receptors. As a further advancement in this direction, molecular cloning has led to the identification of three different types of opioid receptors -- OP1 (delta), OP2 (kappa) and OP3 (mu) -- thereby supporting the results of earlier pharmacological studies which postulated their existence. The three opioid receptors are highly homologous. Consequent to the development of highly specific and selective agonists and antagonists, it was proposed that the three types of opioid receptors could be further categorized into different subtypes. However, the molecular biology data generated so far do not support the presence of the various subtypes of the three well-characterized opioid receptors. Recent strides towards the advancement of our knowledge relating to the molecular biology of these receptors have been reviewed in this article.
内源性阿片肽和吗啡等阿片类药物通过膜结合阿片受体产生其药理作用。这些受体属于G蛋白偶联受体超家族，所有这些受体都具有七个跨膜区域。阿片类药物的构效关系研究为阿片受体的药理学特性开辟了新途径。作为这一方向的进一步进展，分子克隆已导致鉴定出三种不同类型的阿片受体——OP1（δ）、OP2（κ）和OP3（μ）——从而支持了早期药理学研究假设它们存在的结果。三种阿片受体高度同源。随着高特异性和选择性激动剂和拮抗剂的开发，有人提出三种类型的阿片受体可进一步分为不同的亚型。然而，迄今为止产生的分子生物学数据并不支持三种特征明确的阿片受体存在各种亚型。本文综述了近期在这些受体分子生物学知识进展方面取得的进展。
