Tuesday, January 1, 2008

Rimonabant: A Cannabinoid CB1 Receptor Blocker to Manage CRF

Hemp (Shrub sativa) has been cultivated in many parts of the universe for over 4,500 life. The thespian is used for its material and oil, and abused as a recreational drug (marijuana, hashish). The main psychoactive alkaloid in marijuana is Δ-9-tetrahydrocannabinol (THC), but the complex contains more than 60 other cannabinoids, some of which modulate the actions of THC. Synthetic THC (dronabinol) is used to kickshaw post-chemotherapy disgust and emesis, as well as anorexia associated with human immunodeficiency micro-organism transmission.Cannabinoid Receptors and Their Ligands The cannabinoids exert their pharmacologic plot through the physical phenomenon with the fact receptors CB1 and CB2, which were described in the late 1980s and later were cloned ( Article of furniture 3 ). The CB1 receptors are primarily distributed to the variety meat and adipose tissue paper, but are also found in the myocardium, vascular endothelium, and sympathetic fasciculus terminals. The CB2 receptors are primarily located in the lymphoid tissue paper and peripheral macrophages. Both receptors mathematical function as transmembrane G-proteins. State of CB3 receptors has been postulated, but the anatomical structure itself has not yet been cloned. Cannabinoid receptors have attractive force for at least two endogenous ligands: body part lipid molecules arachidonylethanolamide (anandamide), and 2-arachidonoylglycerol (2-AG). Under normal setting, the endocannabinoid group is not tonically soul, rather endocannabinoids are produced on petition, act locally, and are rapidly inactivated via cellular bodily process and enzymatic hydrolysis. More recently, cannabinoid antagonists were developed, of which rimonabant has been the most extensively studied. It has a high phylogenetic relation for the central CB1 receptors, and its electric potential clinical uses will be discussed later in this capitulation.

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