2-Arachidonoylglycerol, a Putative Endogenous Cannabinoid Receptor Ligand, Induces Rapid, Transient Elevation of Intracellular Free Ca 2+ in Neuroblastoma x Glioma Hybrid NG108-15 Cells

Authors: Sugiura T.; Kodaka T.; Kondo S.; Tonegawa T.; Nakane S.; Kishimoto S.; Yamashita A.; Waku K.

Source: Biochemical and Biophysical Research Communications, Volume 229, Number 1, December 1996 , pp. 58-64(7)

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Abstract:

Low concentrations of 2-arachidonoylglycerol were found to induce rapid, transient elevation of intracellular free Ca 2+ in NG108-15 cells (EC50 was 150 nM). Free arachidonic acid, 2-palmitoylglycerol, 2-oleoylglycerol, 2-linoleoylglycerol and 2-docosahexaenoylglycerol were inactive. Anandamide acted as a partial agonist. Importantly, desensitization was observed upon sequential challenge with 2-arachidonoylglycerol. Furthermore, cross-desensitization was observed between 2-arachidonoylglycerol and WIN 55212-2, a cannabinoid receptor agonist. Pretreatment of the cells with SR141716A, a cannabinoid receptor antagonist, abolished the activities of both 2-arachidonoylglycerol and WIN 55212-2. These results strongly suggest that 2-arachidonoylglycerol and WIN 55212-2 bind to a common cannabinoid receptor to elicit cellular responses and that 2-arachidonoylglycerol has some physiological role in nervous tissues.

Language: English

Document Type: Research article

Affiliations: Faculty of Pharmaceutical Sciences, Teikyo University, Kanagawa, 199-01, Japan

Publication date: 1996-12-01