Abstract
The purpose of this review is to discuss the cellular synthesis and inactivation of two putative endogenous ligands of the cannabinoid receptor, N-arachidonylethanolamine (AEA) and 2-arachidonylglycerol (2-AG). Both ligands are synthesized by neurons and brain tissue in response to increased intracellular calcium concentrations. Both ligands are substrates for fatty acid amide hydrolase (FAAH). Both AEA and 2-AG bind to the neuronal form of the cannabinoid receptor (CB1). AEA binds the receptor with moderate affinity and has the characteristics of a partial agonist, whereas, 2-AG binds with low affinity but exhibits full efficacy. Two possible physiological roles of the endocannabinoids and the CB1 receptor are discussed: the regulation of gestation and the regulation of gastrointestinal motility.
Publication types
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Research Support, U.S. Gov't, P.H.S.
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Review
MeSH terms
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Adjuvants, Immunologic / pharmacology
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Amidohydrolases / metabolism
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Animals
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Arachidonic Acids / chemistry
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Arachidonic Acids / metabolism*
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Arachidonic Acids / pharmacology*
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Cannabinoid Receptor Modulators
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Cannabinoids / chemistry
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Cannabinoids / metabolism
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Cannabinoids / pharmacology
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Digestive System Physiological Phenomena
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Endocannabinoids
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Glycerides / chemistry
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Glycerides / metabolism*
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Glycerides / pharmacology*
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Humans
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Polyunsaturated Alkamides
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Receptors, Cannabinoid
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Receptors, Drug / metabolism
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Reproduction / physiology
Substances
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Adjuvants, Immunologic
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Arachidonic Acids
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Cannabinoid Receptor Modulators
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Cannabinoids
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Endocannabinoids
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Glycerides
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Polyunsaturated Alkamides
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Receptors, Cannabinoid
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Receptors, Drug
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glyceryl 2-arachidonate
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Amidohydrolases
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fatty-acid amide hydrolase
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anandamide