Cannabinoids for the Treatment of Neuropathic Pain

Abstract and Introduction

Introduction

The isolation of Δ⁹-tetrahydrocannabinol (THC), the major psychoactive ingredient in cannabis, set the stage for the discovery of an endogenous cannabinoid (endocannabinoid) transmitter system.^[1] Endogenous signaling molecules for this system were subsequently isolated.^[2,3] Anandamide^[4] and 2-arachidonoylglycerol (2-AG),^[2,3] the best characterized endocannabinoids isolated to date, bind to and activate cannabinoid CB₁ and CB₂ receptors. CB₁ is the primary cannabinoid receptor found in the CNS,^[5] whereas CB₂ is predominantly, but not exclusively, found in the immune system.^[6–8] The discovery of cannabinoid receptors allowed researchers to synthesize cannabinoids and characterize their pain-relieving properties. Anandamide and 2-AG are degraded by the enzymes fatty-acid amide hydrolase and monoacylglycerol lipase,^[9] respectively. Enzymes catalyzing endocannabinoid breakdown also represent targets for analgesic drug development. This article will briefly summarize the findings of preclinical and clinical studies evaluating the therapeutic and side-effect profile of cannabinoids as pharmacotherapies for neuropathic pain.

Future Neurology. 2011;6(2):129-133. © 2011 Future Medicine Ltd.

Cite this: Cannabinoids for the Treatment of Neuropathic Pain - Medscape - Mar 01, 2011.