Cannabinoid

Cannabinoid

Cannabinoid

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The broader definition of cannabinoids refers to a group of substances that are structurally related to tetrahydrocannabinol THC or that bind to cannabinoid receptors. The chemical definition encompasses a variety of distinct chemical classes: At the present time, there are three general types of cannabinoids: It uses material from the Wikipedia article on 'Cannabinoid' All material adapted used from Wikipedia is available under the terms of the Creative Commons Attribution-ShareAlike License. Before the s, it was often speculated that cannabinoids produced their physiological and behavioral effects via nonspecific interaction with cell membranes, instead of interacting with specific membrane-bound receptors. These receptors are common in animals, and have been found in mammals, birds, fish, and reptiles. At present, there are two known types of cannabinoid receptors, termed CB1 and CB2, with mounting evidence of more. CB1 receptors are found primarily in the brain, to be specific in the basal ganglia and in the limbic system, including the hippocampus. They are also found in the cerebellum and in both male and female reproductive systems. CB1 receptors are absent in the medulla oblongata, the part of the brain stem responsible for respiratory and cardiovascular functions. Thus, there is not a risk of respiratory or cardiovascular failure as there is with many other drugs. CB1 receptors appear to be responsible for the euphoric and anticonvulsive effects of cannabis. CB2 receptors are almost exclusively found in the immune system, with the greatest density in the spleen. While found only in the peripheral nervous system, a report does indicate that CB2 is expressed by a subpopulation of microglia in the human cerebellum. CB2 receptors appear to be responsible for the anti-inflammatory and possibly other therapeutic effects of cannabis. In addition to cannabinoids, the resin is rich in terpenes, which are largely responsible for the odour of the cannabis plant. Phytocannabinoids are nearly insoluble in water but are soluble in lipids, alcohols, and other non-polar organic solvents. However, as phenols, they form more water-soluble phenolate salts under strongly alkaline conditions. All-natural cannabinoids are derived from their respective 2-carboxylic acids 2-COOH by decarboxylation catalyzed by heat, light, or alkaline conditions. At least 66 cannabinoids have been isolated from the cannabis plant To the right the main classes of natural cannabinoids are shown. All classes derive from cannabigerol-type compounds and differ mainly in the way this precursor is cyclized. Other common cannabinoids are listed below:. Tetrahydrocannabinol THC is the primary psychoactive component of the plant. It appears to ease moderate pain analgetic and to be neuroprotective. Its effects are perceived to be more cerebral. It appears to relieve convulsion, inflammation, anxiety, and nausea. Cannabigerol CBG is non-psychotomimetic but still affects the overall effects of Cannabis. It also binds to the CB2 receptor. Cannabichromene CBC is non-psychoactive and does not affect the psychoactivity of THC It is found in nearly all tissues in a wide range of animals. In , a third, ether-type endocannabinoid, 2-arachidonyl glyceryl ether noladin ether , was isolated from porcine brain. Prior to this discovery, it had been synthesized as a stable analog of 2-AG; indeed, some controversy remains over its classification as an endocannabinoid, as another group failed to detect the substance at 'any appreciable amount' in the brains of several different mammalian species. It binds primarily to the CB1 receptor, and only weakly to the CB2 receptor. In rats, virodhamine was found to be present at comparable or slightly lower concentrations than anandamide in the brain, but 2- to 9-fold higher concentrations peripherally. Although in this intercellular signaling role they are similar to the well-known monoamine neurotransmitters, such as acetylcholine and dopamine, endocannabinoids differ in numerous ways from them. For instance, they use retrograde signaling. Furthermore, endocannabinoids are lipophilic molecules that are not very soluble in water. They are not stored in vesicles, and exist as integral constituents of the membrane bilayers that make up cells. The mechanisms and enzymes underlying the biosynthesis of endocannabinoids remain elusive and continue to be an area of active research. They are, in effect, released from the postsynaptic cell and act on the presynaptic cell, where the target receptors are densely concentrated on axonal terminals in the zones from which conventional neurotransmitters are released. Activation of cannabinoid receptors temporarily reduces the amount of conventional neurotransmitter released. This endocannabinoid mediated system permits the postsynaptic cell to control its own incoming synaptic traffic. The ultimate effect on the endocannabinoid-releasing cell depends on the nature of the conventional transmitter being controlled. For instance, when the release of the inhibitory transmitter GABA is reduced, the net effect is an increase in the excitability of the endocannabinoid-releasing cell. On the converse, when release of the excitatory neurotransmitter glutamate is reduced, the net effect is a decrease in the excitability of the endocannabinoid-releasing cell. Endocannabinoids are hydrophobic molecules. They cannot travel unaided for long distances in the aqueous medium surrounding the cells from which they are released, and therefore act locally on nearby target cells. Hence, although emanating diffusely from their source cells, they have much more restricted spheres of influence than do hormones, which can affect cells throughout the body. Endocannabinoids constitute a versatile system for affecting neuronal network properties in the nervous system. The current understanding recognizes the role that endocannabinoids play in almost every major life function in the human body. In The U. Historically, laboratory synthesis of cannabinoids were often based on the structure of herbal cannabinoids, and a large number of analogs have been produced and tested, especially in a group led by Roger Adams as early as and later in a group led by Raphael Mechoulam. Newer compounds are no longer related to natural cannabinoids or are based on the structure of the endogenous cannabinoids. Synthetic cannabinoids are particularly useful in experiments to determine the relationship between the structure and activity of cannabinoid compounds, by making systematic, incremental modifications of cannabinoid molecules. The discovery of the first cannabinoid receptors in the s helped to resolve this debate. Cannabinoid receptor type 1 CB1 receptors are found primarily in the brain, to be specific in the basal ganglia and in the limbic system, including the hippocampus. Cannabinoid receptor type 2 CB2 receptors are almost exclusively found in the immune system, with the greatest density in the spleen. Types At least 66 cannabinoids have been isolated from the cannabis plant To the right the main classes of natural cannabinoids are shown. Other common cannabinoids are listed below: Cannabigerol Cannabigerol CBG is non-psychotomimetic but still affects the overall effects of Cannabis. Cannabichromene Cannabichromene CBC is non-psychoactive and does not affect the psychoactivity of THC It is found in nearly all tissues in a wide range of animals. The endocannabinoid 2-AG has been found in bovine and human maternal milk. Range Endocannabinoids are hydrophobic molecules. Other thoughts Endocannabinoids constitute a versatile system for affecting neuronal network properties in the nervous system. Patent In The U. Medications containing natural or synthetic cannabinoids or cannabinoid analogs: Sativex develops whole-plant cannabinoid medicines Rimonabant SR , a selective cannabinoid CB1 receptor antagonist used as an anti-obesity drug under the proprietary name Acomplia. It is also used for smoking cessation Other notable synthetic cannabinoids include: CP, produced in , this synthetic cannabinoid receptor agonist is many times more potent than THC Dimethylheptylpyran HU, about times as potent as THC HU a potential anti-cancer drug derived from cannabidiol that specifically inhibits topoisomerase II.

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