Faculty Collaboration Database

Biochemistry and pharmacology of the endocannabinoids arachidonylethanolamide and 2-arachidonylglycerol. Prostaglandins Other Lipid Mediat 2000 Apr;61(1-2):3-18

Date

04/29/2000

Pubmed ID

10785538

DOI

10.1016/s0090-6980(00)00051-4

Scopus ID

2-s2.0-0033998951 (requires institutional sign-in at Scopus site)   212 Citations

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.

Author List

Hillard CJ

Author

Cecilia J. Hillard PhD Associate Dean, Center Director, Professor in the Pharmacology and Toxicology department at Medical College of Wisconsin

MESH terms used to index this publication - Major topics in bold

Adjuvants, Immunologic
Amidohydrolases
Animals
Arachidonic Acids
Cannabinoid Receptor Modulators
Cannabinoids
Digestive System Physiological Phenomena
Endocannabinoids
Glycerides
Humans
Polyunsaturated Alkamides
Receptors, Cannabinoid
Receptors, Drug
Reproduction