2-Arachidonoylgylcerol: A Possible Endogenous Cannabinoid Receptor Ligand in Brain

Sugiura, T.; Kondo, S.; Sukagawa, A.; Nakane, S.; Shinoda, A.; Itoh, K.; Yamashita, A.; Waku, K.

doi:10.1006/bbrc.1995.2437

Cited by 2,196Cannabis and Cannabinoid ResearchNeuroscience and Neuropharmacology ResearchReceptor Mechanisms and Signaling

2-Arachidonoylgylcerol: A Possible Endogenous Cannabinoid Receptor Ligand in Brain

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Sugiura, T., Kondo, S., Sukagawa, A., Nakane, S., Shinoda, A., Itoh, K., Yamashita, A., Waku, K.·1995·Biochemical and Biophysical Research Communications

DOI 10.1006/bbrc.1995.2437

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Abstract

The effects of anadamide, 2-arachidonoylglycerol and related compounds on the specific binding of a radiolabeled cannabinoid receptor ligand,[3H]CP55940, to synaptosomal membranes were examined. Anandamide, an endogenous cannabinoid receptor ligand, reduced the specific binding of [3H]CP55940 to synaptosomal membranes in a dose-dependent manner: the Ki value was 89 nM. 2-Arachidonoylglycerol was also shown to bind appreciably to the cannabinoid receptor in competitive inhibition experiments. The apparent binding affinity was markedly increased when the binding assay was carried out in the presence of the esterase inhibitor DFP or at 0 degrees C. Free arachidonic acid and N-palmitoylethanolamine were almost inactive in terms of binding to the cannabinoid receptor in synaptosomal membranes. 2-Arachidonoylglycerol may be an endogenous cannabinoid receptor ligand in the brain.

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The most studied endogenous ligands that bind cannabinoid receptors are AEA and 2-AG.
“The most studied endogenous ligands that bind cannabinoid receptors are AEA (Devane et al, 1992) and 2arachidonoylglycerol (2-AG) (Mechoulam et al, 1995;Sugiura et al, 1995).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Sugiura et al, 1995

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Authors: Sugiura, T., Kondo, S., Sukagawa, A., Nakane, S., Shinoda, A., Itoh, K., Yamashita, A., & Waku, K.
Affiliations: Teikyo University (JP)
ORCID: Yamashita, A.
Venue: Biochemical and Biophysical Research Communications
Publisher: Elsevier BV
Published: 1995-10
Volume: 215
Issue: 1
Pages: 89-97
ISSN: 0006-291X (ISSN-L)
DOI: 10.1006/bbrc.1995.2437
OpenAlex: W2085741941
Cited by: 2,196
References: 0
Citations by year: 2026: 22 · 2025: 61 · 2024: 68 · 2023: 63 · 2022: 59 · 2021: 113 · 2020: 97 · 2019: 68 · 2018: 77 · 2017: 74 · 2016: 79 · 2015: 84 · 2014: 87 · 2013: 82 · 2012: 95
FWCI: 14.31
Type: journal article
Language: en
Open access: green
teikyo-u.repo.nii.ac.jp
Licence: cc-by-nc-nd
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Biochemical and Biophysical Research Communications (publishedVersion)
PubMed (publishedVersion)
Institutional Repositories DataBase (IRDB) (submittedVersion, cc-by-nc-nd)
Topics: Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords: 2-arachidonoylglycerol, anandamide, endocannabinoid system, cannabinoid receptors, synaptosomal membranes, competitive inhibition, esterase inhibition, DFP, arachidonic acid, N-palmitoylethanolamine, brain
MeSH terms: Animals, Arachidonic Acids, Binding, Competitive, Brain, Cannabinoids, Cyclohexanols, Dose-Response Relationship, Drug, Glycerides, Lipase, Male, Receptors, Drug, Synaptic Membranes, Tritium, Rats, Wistar, Receptors, Cannabinoid, Rats, Polyunsaturated Alkamides, Endocannabinoids

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2-Arachidonoylgylcerol: A Possible Endogenous Cannabinoid Receptor Ligand in Brain

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