Therapeutic Utility of Cannabinoid Receptor Type 2 (CB2) Selective Agonists

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• 作者：Sangdon Han ; Jayant Thatte ; Daniel J. Buzard ; Robert M. Jones
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：November 14, 2013
• 年：2013
• 卷：56
• 期：21
• 页码：8224-8256
• 全文大小：1206K
• 年卷期：v.56,no.21(November 14, 2013)
• ISSN：1520-4804

文摘

The cannabinoid receptor type 2 (CB₂) is a class A GPCR that was cloned in 1993 while looking for an alternative receptor that could explain the pharmacological properties of 螖⁹-tetrahydrocannabinol. CB₂ was identified among cDNAs based on its similarity in amino acid sequence to the CB₁ receptor and helped provide an explanation for the established effects of cannabinoids on the immune system. In addition to the immune system, CB₂ has widespread tissue expression and has been found in brain, peripheral nervous system, and gastrointestinal tract. Several 鈥渕ixed鈥?cannabinoid agonists are currently in clinical use primarily for controlling pain, and it is believed that selective CB₂ agonism may afford a superior analgesic agent devoid of the centrally mediated CB₁ effects. Thus, selective CB₂ receptor agonists represent high value putative therapeutics for treating pain and other disease states. In this Perspective, we seek to provide a concise update of progress in the field.