Activation of phospholipase A2 by cannabinoids. Lack of correlation with CNS effects

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Abstract

Cannabinoids Δ1-tetrahydrocannabinol, cannabinol, cannabidiol and cannabigerol have been shown to affect directly the activity of phospholipase A2 in a cell-free assay. The compounds produced a biphasic activation of the enzyme, with EC50 values in the range 6.0-20.0 × 10-6 M and IC50 values in the range 50.0-150.0 × 10-6M. These results correlated well with the relative potencies reported for the stimulation of prostaglandin release from human synovial cells in vitro, confirming that activation of phospholipase A2 is the predominant action of cannabinoids on arachidonate metabolism in tissue culture. However, since Δ1-tetrahydrocannabinol is unique among these compounds in possessing cataleptic activity, it is unlikely that phospholipase A2 is the major receptor mediating the psychotropic effects of cannabis. © 1987.

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Evans, A. T., Formukong, E., & Evans, F. J. (1987). Activation of phospholipase A2 by cannabinoids. Lack of correlation with CNS effects. FEBS Letters, 211(2), 119–122. https://doi.org/10.1016/0014-5793(87)81420-5

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