The antinociceptive triterpene β-amyrin inhibits 2-arachidonoylglycerol (2-AG) hydrolysis without directly targeting cannabinoid receptors.

ABSTRACT:

Background and purpose

Pharmacological activation of cannabinoid CB(1) and CB(2) receptors is a therapeutic strategy to treat chronic and inflammatory pain. It was recently reported that a mixture of natural triterpenes α- and β-amyrin bound selectively to CB(1) receptors with a subnanomolar K(i) value (133 pM). Orally administered α/β-amyrin inhibited inflammatory and persistent neuropathic pain in mice through both CB(1) and CB(2) receptors. Here, we investigated effects of amyrins on the major components of the endocannabinoid system.

Experimental approach

We measured CB receptor binding interactions of α- and β-amyrin in validated binding assays using hCB(1) and hCB(2) transfected CHO-K1 cells. Effects on endocannabinoid transport in U937 cells and breakdown using homoge

SUBMITTER: Chicca A 

PROVIDER: S-EPMC3525863 | biostudies-literature | 2012 Dec

REPOSITORIES: biostudies-literature