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AZ11713908, a peripheral CB1 agonist for pain

Peripheral cannabinoid receptors are also clearly pathyways leading to analgesic effects, that is the lesson learned after exploring the analgesic effects of AZ11713908, a peripheral CB1 agonist for pain.

The authors addressed the issue of peripheral CB 1 agonism by exploring the analgesic properties and site of action of AZ11713908. This compound is a peripherally restricted CB1R agonist and was tested in rodent pain models.

Systemic administration of AZ11713908 produced robust efficacy in rat pain models, comparable to a mixed CB1R and CB2R agonist with central activity, but AZ11713908 generated less CNS side-effects.

Intraplantar administered AZ11713908 was also sufficient to induce robust analgesia.

These results of AZ11713908, demonstrate the analgesic efficacy of peripheral CB1 receptor agonists. ^[1]

August 2010, Jan M. Keppel Hesselink, MD, PhD

Referenties

[1]: Yu XH, Cao CQ, Martino G, Puma C, Morinville A, St-Onge S, Lessard E, Perkins MN, Laird JM. | A peripherally restricted cannabinoid receptor agonist produces robust anti-nociceptive effects in rodent models of inflammatory and neuropathic pain. | Pain. | 2010 Nov;151(2):337-44. Epub 2010 Aug 8.