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N-arachidonoyl glycine, another endogenous agonist of GPR55.


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.

SUBMITTER: Console-Bram L 

PROVIDER: S-EPMC5576593 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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N-arachidonoyl glycine, another endogenous agonist of GPR55.

Console-Bram Linda L   Ciuciu Sandra M SM   Zhao Pingwei P   Zipkin Robert E RE   Brailoiu Eugen E   Abood Mary E ME  

Biochemical and biophysical research communications 20170708 4


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  ...[more]

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