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Updated: Feb 26, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
N-arachidonoyl glycine, another endogenous agonist of GPR55
Linda Console-Bram1, Sandra M Ciuciu1, Pingwei Zhao1
1Center for Substance Abuse Research, Lewis Katz School of Medicine at Temple University, 3500 N. Broad St., Philadelphia, PA, 19140, USA.
Abstract:
Interest in lipoamino acids as endogenous modulators of G-protein coupled receptors has escalated due to their involvement in a variety of physiologic processes. In particular, a role for these amino acid conjugates has emerged in the endocannabinoid system. The study presented herein investigated the effects of N-arachidonoyl glycine (NAGly) on a candidate endocannabinoid receptor, GPR55. Our novel findings reveal that NAGly induces concentration dependent increases in calcium mobilization and mitogen-activated protein kinase activities in HAGPR55/CHO cells. These increases were attenuated by the selective GPR55 antagonist ML193 (N-[4-[[(3,4-Dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide), supporting receptor mediated signaling. To our knowledge this is the first report identifying GPR55 as a target of the endogenous lipoamino acid, NAGly.
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