Enzymes of porcine brain hydrolyzing 2-arachidonoylglycerol, an endogenous ligand of cannabinoid receptors.

Abstract:

:Anandamide and 2-arachidonoylglycerol (2-AG) are two endogenous ligands for the cannabinoid receptors, and their cannabimimetic activities are lost when they are hydrolyzed enzymatically. Cytosol and particulate fractions of porcine brain exhibited a high 2-AG hydrolyzing activity of 100 nmol/min/mg protein. Most of the activity could be attributed to a monoacylglycerol lipase-like enzyme that did not hydrolyze anandamide. It was separated by hydroxyapatite chromatography from anandamide amidohydrolase, which is also capable of hydrolyzing 2-AG as well as anandamide. Thus, porcine brain has at least two enzymes capable of hydrolyzing 2-AG. The 2-AG hydrolase activities of both the cytosolic and particulate enzymes were irreversibly and time-dependently inhibited by methyl arachidonyl fluorophosphonate with IC50 values as low as 2-3 nM.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Goparaju SK,Ueda N,Taniguchi K,Yamamoto S

doi

10.1016/s0006-2952(98)00314-1

subject

Has Abstract

pub_date

1999-02-15 00:00:00

pages

417-23

issue

4

eissn

0006-2952

issn

1873-2968

pii

S0006295298003141

journal_volume

57

pub_type

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