Opioids and their receptors: Are we there yet?
Opioids and their receptors: Are we there yet?
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DOI：
10.1016/j.neuropharm.2013.03.039
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发表时间：
2014-01
影响因子：
4.7
通讯作者：
Pasternak GW
中科院分区：
文献类型：
--
作者：
Pasternak GW
阿片类药物在药理学中占有重要地位。虽然它们作为镇痛剂的临床使用是医学的基础，但它们的使用受到其副作用和滥用潜力的限制。药理学家一直在寻找没有副作用和现有药物滥用倾向的镇痛药。1973年阿片受体的发现标志着我们开始了解这些药物的分子机制。阿片肽的分离很快就完成了，沿着的是阿片受体的三个家族的分类。长期以来，临床医生一直意识到μ阿片类药物之间的微妙差异，这些差异不容易与单一受体和选择性拮抗剂相协调，这意味着μ受体有两个亚类。然而，μ阿片样物质受体莫尔-1的克隆已经使人们认识到μ阿片样物质受体基因及其大量剪接变体的广泛复杂性。这些剪接变体中的许多被截短并且不符合传统G蛋白偶联受体的结构。然而，现在的证据表明，它们是非常重要的，并可能证明在缺乏当前阿片类药物的不良特性的强效镇痛药的开发中有价值的目标。
Opioids have an important place in pharmacology. While their clinical use as analgesics is fundamental in medicine, their use is constrained by their side-effects and abuse potential. Pharmacologists have sought analgesics lacking side-effects and the abuse liability of the current agents. The identification of the opioid receptors in 1973 marked the beginning of our understanding of the molecular mechanisms of these agents. The isolation of the opioid peptides quickly followed, along with the classification of three families of opioid receptors. Clinicians have long been aware of subtle differences among the mu opioids that were not easily reconciled with a single receptor and selective antagonists implied two subdivisions of mu receptors. However, the cloning of the mu opioid receptor MOR-1 has led to the realization of the extensive complexity of the mu opioid receptor gene and its vast array of splice variants. Many of these splice variants are truncated and do not conform to the structure of traditional G-protein coupled receptors. Yet, evidence now shows that they are quite important and may prove valuable targets in the development of potent analgesics lacking the undesirable properties of current opioids.
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影响因子：
3.5
作者：
Doyle, Glenn A.;Sheng, X. Rebecca;Berrettini, Wade H.
通讯作者：
Berrettini, Wade H.
影响因子：
64.8
作者：
HUGHES, J;SMITH, TW;MORRIS, HR
通讯作者：
MORRIS, HR
影响因子：
3.5
作者：
BUNZOW, JR;SAEZ, C;GRANDY, DK
通讯作者：
GRANDY, DK
影响因子：
3.3
作者：
Abbadie, C;Pasternak, GW;Aicher, SA
通讯作者：
Aicher, SA
影响因子：
1.7
作者：
Abbadie, C;Pasternak, GW
通讯作者：
Pasternak, GW