Physiological roles of 2‐arachidonoylglycerol, an endogenous cannabinoid receptor ligand

Sugiura, Takayuki

doi:10.1002/biof.18

Cited by 176 publications

(195 citation statements)

References 79 publications

Supporting

Mentioning

187

Contrasting

Unclassified

Order By: Relevance

“…Application of a CB 1 R agonist (or antagonist) enhanced (or prevented) DSE and DSI, suggesting that it was mediated by an endogenous cannabinoid ligand [29][30][31]. These endocannabinoids were identified as the hydrophobic ligands N-arachidonoyl ethanolamide (anandamide) [32] and 2-arachidonoyl glycerol (2-AG) [33,34].…”

Section: The Endocannabinoid Systemmentioning

confidence: 99%

Cannabinoids and Epilepsy

et al. 2015

View full text Add to dashboard Cite

Cannabis has been used for centuries to treat seizures. Recent anecdotal reports, accumulating animal model data, and mechanistic insights have raised interest in cannabisbased antiepileptic therapies. In this study, we review current understanding of the endocannabinoid system, characterize the pro-and anticonvulsive effects of cannabinoids [e.g., Δ9-tetrahydrocannabinol and cannabidiol (CBD)], and highlight scientific evidence from pre-clinical and clinical trials of cannabinoids in epilepsy. These studies suggest that CBD avoids the psychoactive effects of the endocannabinoid system to provide a well-tolerated, promising therapeutic for the treatment of seizures, while whole-plant cannabis can both contribute to and reduce seizures. Finally, we discuss results from a new multicenter, open-label study using CBD in a population with treatment-resistant epilepsy. In all, we seek to evaluate our current understanding of cannabinoids in epilepsy and guide future basic science and clinical studies.

show abstract

Section: The Endocannabinoid Systemmentioning

confidence: 99%

Cannabinoids and Epilepsy

et al. 2015

View full text Add to dashboard Cite

show abstract

“…The other widely investigated endocannabinoid, 2-arachidonoylglycerol (2-AG), is the arachidonate ester of glycerol that was isolated from peripheral tissues. This molecule is able to activate CB 1 and CB 2 receptors with similar potency and efficacy (7,8) , and to interact with γ-aminobutyric acid receptors (9) . Other endocannabinoids might be represented by both 2-AG ether (noladin ether), that binds to CB 1 receptors with relatively more affinity that to CB 2 ( 10) , and virodhamine, that is a CB 2 receptor agonist and CB 1 receptor partial agonist/antagonist (11) .…”

mentioning

confidence: 99%

PUFA-derived endocannabinoids: an overview

Cascio

2013

Proc. Nutr. Soc.

View full text Add to dashboard Cite

Following on from the discovery of cannabinoid receptors, of their endogenous agonists (endocannabinoids) and of the biosynthetic and metabolic enzymes of the endocannabinoids, significant progress has been made towards the understanding of the role of the endocannabinoid system in both physiological and pathological conditions. Endocannabinoids are mainly n-6 long-chain PUFA (LCPUFA) derivatives that are synthesised by neuronal cells and inactivated via a two-step process that begins with their transport from the extracellular to the intracellular space and culminates in their intracellular degradation by hydrolysis or oxidation. Although the enzymes responsible for the biosynthesis and metabolism of endocannabinoids have been well characterised, the processes involved in their cellular uptake are still a subject of debate. Moreover, little is yet known about the roles of endocannabinoids derived from n-3 LCPUFA such as EPA and DHA. Here, I provide an overview of what is currently known about the mechanisms for the biosynthesis and inactivation of endocannabinoids, together with a brief analysis of the involvement of the endocannabinoids in both food intake and obesity. Owing to limited space, recent reviews will be often cited instead of original papers.

show abstract

“…These are the CB 1 and CB 2 receptors, which both signal through G i/o protein (reviewed in Howlett et al, 2002;Pertwee, 2005aPertwee, , 2006. A second equally momentous discovery was that mammalian tissues can synthesize and release compounds that activate cannabinoid receptors, the first of these 'endocannabinoids' to be identified being N-arachidonoylethanolamine (anandamide) and 2-arachidonoylglycerol (Devane et al, 1992;Mechoulam et al, 1995;Sugiura et al, 1995). Together with their receptors, these and other more recently discovered endocannabinoids (reviewed in Pertwee, 2005b) form a part of the 'endocannabinoid system'.…”

mentioning

confidence: 99%

GPR55: a new member of the cannabinoid receptor clan?

Pertwee

2007

British J Pharmacology

208

154

View full text Add to dashboard Cite

In this issue of the British Journal of Pharmacology, Ryberg et al. present convincing in vitro evidence that the orphan GPCR, GPR55, is a cannabinoid receptor. GPR55 was activated by a range of plant, synthetic and endogenous cannabinoids and blocked by the non-psychoactive phytocannabinoid, cannabidiol. Their experiments have revealed several differences between the pharmacology of GPR55 and the established cannabinoid CB 1 and CB 2 receptors. For example, the CB 1 receptor antagonist, AM251, activated GPR55 and the main psychoactive constituent of cannabis, D 9 -tetrahydrocannabinol, displayed greater efficacy at GPR55 than at CB 1 or CB 2 receptors. They also compared the distribution of GPR55 and CB 1 mRNA in mouse and report that GPR55 couples to Ga 13 , that it is activated by virodhamine, palmitoylethanolamide and oleoylethanolamide, and that virodhamine displays relatively high efficacy as a GPR55 agonist. Still to be identified are the main roles played by GPR55 in health and disease and any potential therapeutic benefits of activating or blocking this receptor.

show abstract

Physiological roles of 2‐arachidonoylglycerol, an endogenous cannabinoid receptor ligand

Cited by 176 publications

References 79 publications

Cannabinoids and Epilepsy

Cannabinoids and Epilepsy

PUFA-derived endocannabinoids: an overview

GPR55: a new member of the cannabinoid receptor clan?

Contact Info

Product

Resources

About