A major glucuronidated metabolite of JWH-018 is a neutral antagonist at CB1 receptors.
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ABSTRACT:
SUBMITTER: Seely KA
PROVIDER: S-EPMC3921679 | biostudies-literature | 2012 Apr
REPOSITORIES: biostudies-literature
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A major glucuronidated metabolite of JWH-018 is a neutral antagonist at CB1 receptors.
Seely Kathryn A KA Brents Lisa K LK Radominska-Pandya Anna A Endres Gregory W GW Keyes Gregory S GS Moran Jeffery H JH Prather Paul L PL
Chemical research in toxicology 20120315 4
Recently, hydroxylated metabolites of JWH-018, a synthetic cannabinoid found in many K2/Spice preparations, have been shown to retain affinity and activity for cannabinoid type 1 receptors (CB1Rs). The activity of glucuronidated metabolites of JWH-018 is not known; hence, this study investigated the affinity and activity of a major metabolite, JWH-018-N-(5-hydroxypentyl) β-D-glucuronide (018-gluc), for CB1Rs. The 018-gluc binds CB1Rs (K(i) = 922 nM), has no effect on G-protein activity, but anta ...[more]
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