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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Recent Development of CB2 Selective and Peripheral CB1/CB2 Cannabinoid Receptor Ligands

Author(s): Tapio Nevalainen

Volume 21, Issue 2, 2014

Page: [187 - 203] Pages: 17

DOI: 10.2174/09298673113206660296

Price: $65


Cannabinoids have potential therapeutic value e.g. in pain relief, cancer therapy, control of nausea and vomiting, and appetite stimulation, but their therapeutic benefits are limited by unwanted central nervous system (CNS) side-effects. Separating the therapeutic effects of cannabinoid agonists from their undesired CNS effects can be achieved by either increasing the selectivity of the ligands for the CB2 receptor or by developing peripherally restricted CB1/CB2 ligands. A vast number of structurally diverse CB2 ligands have been developed during the past 3 years, stemming from the screening hits, which are further optimized towards lead compounds and drug candidates. Some of CB2 ligands may ultimately enter into clinical use as pain relief, anticancer, or antipruritic agents. This review focuses on the recent literature dealing with selective CB2 receptor ligands, with a particular emphasis on the CB2 agonists developed from 2009 onwards.

Keywords: Agonist, anti-proliferative, antipruritics, cannabinoid, CB1, CB2, inverse agonist, pain, partial agonists, peripheral ligands.

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