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3D model of 2-Arachidonoylglycerol, an endocannaboid. The endocannabinoid system (ECS) is a biological system composed of endocannabinoids, which are neurotransmitters that bind to cannabinoid receptors, and cannabinoid receptor proteins that are expressed throughout the central nervous system (including the brain) and peripheral nervous system.
Other molecular biology studies have suggested that the orphan receptor GPR55 should in fact be characterised as a cannabinoid receptor, on the basis of sequence homology at the binding site. Subsequent studies showed that GPR55 does indeed respond to cannabinoid ligands.
Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene. [5] And discovered, by determination and characterization in 1988, [6] and cloned in 1990 for the first time.
The cannabinoid receptor 2 (CB2), is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the CNR2 gene. [5] [6] It is closely related to the cannabinoid receptor 1 (CB1), which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol (THC), the active agent in ...
These include the heat shock proteins and fatty acid-binding proteins for anandamide (FABPs). [ 6 ] [ 7 ] FABPs such as FABP1, FABP3, FABP5, and FABP7 have been shown to bind endocannabinoids. [ 8 ] [ 9 ] FABP inhibitors attenuate the breakdown of anandamide by the enzyme fatty acid amide hydrolase (FAAH) in cell culture. [ 6 ]
Anandamide, the first discovered endocannabinoid, engages with the body's endocannabinoid system by binding to the same cannabinoid receptors that THC found in cannabis acts on. Anandamide can be found within tissues in a wide range of animals. [1] [2] It has also been found in plants, such as the cacao tree. [3]
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Another endocannabinoid, 2-arachidonoylglycerol, binds to both the CB 1 and CB 2 receptors with similar affinity, acting as a full agonist at both. [ 76 ] 2-AG is present at significantly higher concentrations in the brain than anandamide, [ 81 ] and there is some controversy over whether 2-AG rather than anandamide is chiefly responsible for ...