Current Topics in Medicinal Chemistry - Volume 8, Issue 3, 2008

The utilization of the hemp plant, Cannabis sativa L. has a millenia long history. The therapeutic potential of the plant was recognized early and most parts of the plant have been exploited, for example, in medicine or in various religious rituals. The major psychoactive substance of cannabis, Δ9-tetrahydrocannabinol (THC), was isolated only in the 1960s. THC and other structurally similar compounds characterized from this pl Read More

Advances in understanding the physiology and pharmacology of the endogenous cannabinoid system have potentiated the interest of cannabinoid receptors as potential therapeutic targets. Cannabinoids have been shown to modulate a variety of immune cell functions and have therapeutic implications on central nervous system (CNS) inflammation, chronic inflammatory conditions such as arthritis, and may be therapeuticall Read More

Two subtypes of the mammalian cannabinoid receptor have been identified and successfully cloned since 1990. The CB1 receptor is primarily located in the central nervous system and the CB2 receptor is almost exclusively expressed in cells of the immune system. The CB1 and CB2 receptors are both G-protein coupled receptors and are involved in the inhibition of adenylate cyclase. The CB2 receptor is of particular Read More

During the last decade there has been a growing interest towards the modulation of the cannabinoid CB1 receptor. The identification of CB1 cannabinoid receptor antagonists has been one of the major advances in cannabinoid research. Thus, the development of these ligands has opened new therapeutic applications. Since the discovery of the first cannabinoid receptor antagonist, rimonabant, by Sanofi in 1994, a l Read More

Monoacylglycerol lipase (MAGL) has been recently proposed as the main enzymatic activity responsible for the in vivo hydrolysis of the most abundant endocannabinoid in the brain, the 2-arachidonoylglycerol (2-AG). The endocannabinoids, mainly anandamide (AEA) and 2-AG, are a class of lipid messengers that modulate a broad number of physiological processes both in the central nervous system and in the periphery. T Read More

The family of the endogenous agonists of the cannabinoid receptors - i.e., the endocannabinoids - includes several polyunsaturated fatty acid amides and esters. Arachidonoylethanolamide (anandamide, AEA) and 2-arachidonoylglycerol (2-AG) are, respectively, the leads of these chemical families. So far, two enzymes responsible for the metabolism of AEA and 2-AG have been described: Fatty Acid Amide Hydrolase (FAAH) Read More

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