Receptors and channels targeted by synthetic cannabinoid receptor agonists and antagonists.
Receptors and channels targeted by synthetic cannabinoid receptor agonists and antagonists.
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DOI：
10.2174/092986710790980050
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发表时间：
2010
影响因子：
4.1
通讯作者：
Pertwee RG
中科院分区：
文献类型：
--
作者：
Pertwee RG
广泛接受的是，靶向CB 1和/或CB 2受体的非内源性化合物具有用于临床管理越来越多的疾病的治疗潜力。这些病症中只有少数已经用Δ9-四氢大麻酚或大麻酮（两者都是CB 1/CB 2受体激动剂）治疗，并且现在对扩展此类激动剂的临床应用以及开发CB 2选择性激动剂、外周限制性CB 1/CB 2受体激动剂和CB 1/CB 2拮抗剂和反向激动剂作为药物存在相当大的兴趣。已经开发了许多大麻素受体配体，并且它们与CB 1和CB 2受体的相互作用得到了很好的表征。本文综述了目前已知的这些化合物以正构或变构方式结合、激活、抑制或阻断非CB 1、非CB 2 G蛋白偶联受体如GPR 55、递质门控通道、离子通道和核受体的能力。它首先简要描述了这些配体中的每一种如何与CB 1和/或CB 2受体相互作用。
It is widely accepted that non-endogenous compounds that target CB1 and/or CB2 receptors possess therapeutic potential for the clinical management of an ever growing number of disorders. Just a few of these disorders are already treated with Δ9-tetrahydrocannabinol or nabilone, both CB1/CB2 receptor agonists, and there is now considerable interest in expanding the clinical applications of such agonists and also in exploiting CB2-selective agonists, peripherally restricted CB1/CB2 receptor agonists and CB1/CB2 antagonists and inverse agonists as medicines. Already, numerous cannabinoid receptor ligands have been developed and their interactions with CB1 and CB2 receptors well characterized. This review describes what is currently known about the ability of such compounds to bind to, activate, inhibit or block non-CB1, non-CB2 G protein-coupled receptors such as GPR55, transmitter gated channels, ion channels and nuclear receptors in an orthosteric or allosteric manner. It begins with a brief description of how each of these ligands interacts with CB1 and/or CB2 receptors.
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