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Anandamide amidohydrolase reacting with 2‐arachidonoylglycerol, another cannabinoid receptor ligand

Year: 1998

Type: article

Abstract: Two endogenous ligands for cannabinoid receptors, anandamide (arachidonylethanolamide) and 2-arachidonoylglycerol, lose their biological activities by enzymatic hydrolysis. A cDNA for a rat liver enzyme hydrolyzing anandamide as well as oleamide was overexpressed in COS-7 cells. When the particulate fraction was allowed to react with 2-arachidonoylglycerol, arachidonic acid was produced. In contrast, this hydrolytic reaction did not occur with the control cells. The hydrolysis of 2-arachidonoylglycerol proceeded about 4-fold faster than the anandamide hydrolysis with a Km value as low as 6 microM and an optimal pH of 10. Phenylmethylsulfonyl fluoride and methyl arachidonyl fluorophosphonate inhibited the hydrolysis of both anandamide and 2-arachidonoylglycerol in parallel. Furthermore, the hydrolysis of [14C]2-arachidonoylglycerol was inhibited by anandamide dose-dependently. These results suggest that anandamide and 2-arachidonoylglycerol can be inactivated by the same enzyme.

Source: FEBS Letters

DOI: 10.1016/s0014-5793(97)01603-7

Authors: Sravan Kumar Goparaju, Natsuo Ueda, Hiroko Yamaguchi, Shozo Yamamoto

Institution: Tokushima University

Language: English

Topic: Cannabis and Cannabinoid Research

Subfield: Pharmacology (medical)

Field: Medicine

Domain: Health Sciences

Open Access status: bronze

Funders: Japan Foundation for Applied Enzymology, Kissei, Ono Medical Research Foundation, Ono Pharmaceutical, Daiichi Sankyo Company

OpenAlex ID: W2152872852

FWCI: 14.81

Cites: 35

Cited by: 331

Related to: 10