2-arachidonoylglycerol in the context of "Endocannabinoid system"

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👉 2-arachidonoylglycerol in the context of Endocannabinoid system

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. It is found in animals as simple as hydras, but absent in insects, who are hypothesized to have lost it due to a lack of arachidonic acid. The endocannabinoid system is still not fully understood, but may be involved in regulating physiological and cognitive processes, including fertility, pregnancy, pre- and postnatal development, various activity of immune system, appetite, pain-sensation, mood, and memory, and in mediating the pharmacological effects of cannabis. The ECS plays an important role in multiple aspects of neural functions, including the control of movement and motor coordination, learning and memory, emotion and motivation, addictive-like behavior and pain modulation, among others.

Two primary cannabinoid receptors have been identified: CB1, first cloned (or isolated) in 1990; and CB2, cloned in 1993. CB1 receptors are found predominantly in the brain and nervous system, as well as in peripheral organs and tissues, and are the main molecular target of the fatty-acid neurotransmitter anandamide, as well as the most known active component of cannabis, tetrahydrocannabinol (THC). Another endocannabinoid, 2-arachidonoylglycerol (2-AG), also interacts with both CB receptors. It is significantly more abundant in the mammalian brain than anandamide, exceeding it by two to three orders of magnitude.

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2-arachidonoylglycerol in the context of CB1 receptor

Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene. It was discovered by determination and characterization in 1988, and cloned in 1990 for the first time. The human CB1 receptor is expressed in the peripheral nervous system and central nervous system. It is activated by endogenous cannabinoids called endocannabinoids, a group of retrograde neurotransmitters that include lipids, such as anandamide and 2-arachidonoylglycerol; plant phytocannabinoids, such as docosatetraenoylethanolamide found in wild dagga, the compound tetrahydrocannabinol which is an active constituent of the psychoactive drug cannabis; and synthetic analogs of tetrahydrocannabinol. CB1 is antagonized by the phytocannabinoid tetrahydrocannabivarin at low doses and at higher doses, it activates the CB1 receptor as an agonist, but with less potency than tetrahydrocannabinol.

The primary endogenous agonist of the human CB1 receptor is anandamide.

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