Multiple opiate receptors in peripheral tissue preparations.
Multiple opiate receptors in peripheral tissue preparations.
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DOI：
10.1016/0006-2952(81)90194-5
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发表时间：
1981-07
影响因子：
5.8
通讯作者：
M. Wüster;Rüdiger Schulz;Albert Herz
中科院分区：
文献类型：
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作者：
M. Wüster;Rüdiger Schulz;Albert Herz
阿片研究领域的主要兴趣集中在阿片受体的异质性问题上。虽然阿片受体大分子的分子结构仍然未知，但必须假设两个可分离的功能：（1）受体识别特定药物的能力和（2）翻译接收信号的能力。因此，近年来，阿片受体的识别以及药理学反应已被用于表征阿片受体。然而，人们必须记住，识别位点的描述通常涉及用放射性标记的化合物进行的结合研究，其价值有限。与受体识别和介导接收到的特定信息的能力相比。事实上，多种阿片受体的概念源于对吗啡和结构相关化合物引起的不同药理学作用的仔细观察[1，21]。最近，随着阿片肽的发现，这一概念得到了进一步的关注，如许多论文所记载的，强调阿片识别位点的分化，特别是在中枢神经系统（CNS）中。这些发现已被其他人全面审查[3-51]。显然，阿片类药物结合位点之间的进一步区别可以通过特异性阿片类药物对与钠离子或鸟嘌呤核苷酸GTP结合的烷基化抑制剂[6，71]的选择性保护来实现[8]。对多种阿片受体概念的重大贡献来自分离的制剂。研究阿片类药物作用的经典方法是电刺激豚鼠回肠（GPI）。最近，小鼠输精管（MVD）和后来的大鼠输精管（RVD）受到特别关注，因为它们对阿片肽表现出特定的敏感性。由于许多阿片类药物的效力在这些组织之间并不平行变化，因此提出不同的受体群体是每个组织中固有的。
Major interest in the field of opiate research focuses on the issue of a heterogeneity of receptors for opioids. Although the molecular structure of the opioid receptor macromolecule remains unknown, two separable functions have to be postulated:(1) the ability of the receptor to recognize a specific drug and (2) the capacity to translate a received signal. Thus, during recent years both the recognition of an opioid as well as the pharmacologic response have been employed for the characterization of opiate receptors. However, one has to keep in mind that description of recognition sites, which in general relates to binding studies conducted with radioactively labelled compounds, is limited in its value as. compared to the ability of the receptor both to recognize and to mediate a specific information received. In fact, the concept of multiple opiate receptors originates from careful observations of different pharmacological effects being elicited by morphine and structurally related compounds [l, 21. More recently, following the discovery of the opioid peptides, this concept gained further attention as documented by numerous papers, putting emphasis on the differentiation of opiate recognition sites particularly in the central nervous system (CNS). These findings have been comprehensively reviewed by others [3-51. Apparently, further distinctions between opiate binding sites can be achieved by their selective protection with specific opioids against alkylating inhibitors of binding [6, 71, with sodium ions or with the guanine nucleotide GTP [8]. Significant contributions to the concept of multiple opiate receptors come from isolated preparations. The classical preparation for investigation into the action of opioids is the electrically stimulated guinea-pig ileum (GPI). More recently, the mouse vas deferens (MVD) and later the rat vas deferens (RVD) received particular attention as they exhibit specific sensitivity to opioid peptides. Since the potency of a number of opioids does not vary in parallel between these tissues, a different receptor population was proposed to be inherent in each tissue.