Cannabinoids and endocannabinoids

Abstract

Marijuana is a common name for the plant Cannabis sativa, whose intoxicating and medicinal effects have been known for thousand of years. The active principle of marijuana, (-)-trans-Δ9-tetrahydrocannabinol (Δ9-THC), exerts its pharmacological effects by binding to selective receptors present on the membranes of neurons and other cells. These cannabinoid receptors are normally engaged by a family of lipid mediators, called endocannabinoids, which are thought to participate in the regulation of a diversity of brain functions, including pain, mood, appetite and memory. The endocannabinoid system is comprised of the endocannabinoids, mainly anandamide (arachidonoylethanolamide) and 2-arachidonoylglycerol (2-AG), proteins that control their formation and deactivation, and cell-surface receptors (CB1 and CB2) that transduce their actions. The key components of endocannabinoid signaling are found in the brain and spinal cord, but also in many peripheral organs and tissues. In this chapter, we outline current views on how endocannabinoid substances are produced, act on cannabinoid receptors, and are deactivated in the brain. In addition, we review recent progress on the development of pharmacological agents that interfere with endocannabinoid deactivation and discuss their potential utility in the treatment of cannabinoid-based therapeutics.