2-arachidonylglycerol, a putative endogenous cannabinoid receptor ligand, induces rapid, transient elevation of intracellular free Ca2+ neuroblastoma X glioma hybrid NG108-15 cells

  • Takayuki Sugiura
  • , Tomoko Kodaka
  • , Sachiko Kondo
  • , Takashi Tonegawa
  • , Shinji Nakane
  • , Seishi Kishimoto
  • , Atsushi Yamashita
  • , Keizo Waku

Research output: Contribution to journalArticlepeer-review

152 Scopus citations

Abstract

Low concentrations of 2-arachidonoylycerol were found to induce rapid, transient elevation of intracellular free Ca2+ 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, 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.

Original languageEnglish
Pages (from-to)58-64
Number of pages7
JournalBiochemical and Biophysical Research Communications
Volume229
Issue number1
DOIs
StatePublished - 4 Dec 1996

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