CB2 cannabinoid receptor agonists offer analgesia against neuropathic and other types of pain despite their lack of binding within the CNS

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CB2 cannabinoid receptor agonists offer analgesia against neuropathic and other types of pain despite their lack of binding within the CNS

Cannabinoid CB2 receptor agonists produce analgesia despite their inactivity within the CNS. This has now been shown to relate to the release of endogenous beta-endorphin from the periphery which in turn acts to prevent activation of primary afferent neurons.

Pain products generated global sales of nearly US$40 billion in 2003 (including anesthetics and antimigraine agents) and this is expected to double by 2010 (see the analgesia section of our feature CNS Drug Discoveries: What the future holds). Pain is associated with a broad range of diseases and is often poorly diagnosed and treated. There has been tremendous research activity into the treatment of pain and many types of pain remain relatively unexplored.

Neuropathic pain represents a particular focus of the pharmaceutical industry. Approximately 26 million patients worldwide suffer from some form of neuropathic pain, spending an estimated US$2.5 billion globally in 2003. A number of companies are evaluating therapeutic agents that act on the cannabinoid system as a novel approach to pain.

GW pharmaceuticals is one of the leaders in the field of cannabinoid-based analgesics. Their lead, Sativex, is currently being assessed by both UK and Canadian regulatory bodies. Sativex is a whole plant medicinal cannabis extract and activates both CB1 and CB2 cannabinoid receptors. CB1 receptors are widely distributed both systemically and centrally and their activation produces numerous effects including psychoactivity associated with cannabis. The role of the second type of receptor, CB2 receptor, is still under investigation but it is believed to mediate the immunological effects of cannabinoids. Current cannabinoid research is focusing on the development of CB2 receptor agonists that may exert therapeutic activity without producing psychoactive side-effects.

CB2 agonists produce analgesia in models of neuropathic as well as inflammatory pain suggesting that selective agonists could produce analgesia without psychoactivity; the mechanism of this effect is however unclear. The highlighted PNAS paper reports that CB2 receptor activation stimulates the release of endogenous beta-endorphin from the periphery which in turn acts to prevent activation of primary afferent neurons.

Entry date Sunday, March 06, 2005

Proc Natl Acad Sci U S A. 2005 Feb 10; [Epub ahead of print]

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