Do N-arachidonyl-glycine (NA-glycine) and 2-arachidonoyl glycerol (2-AG) share mode of action and the binding site on the β2 subunit of GABAA receptors?

NA-glycine is an endogenous lipid molecule with analgesic properties, which is structurally similar to the endocannabinoids 2-AG and anandamide but does not interact with cannabinoid receptors. NA-glycine has been suggested to act at the G-protein coupled receptors GPR18 and GPR92. Recently, we have described that NA-glycine can also modulate recombinant α1β2γ2 GABAA receptors. Here we characterize in more detail this modulation and investigate the relationship of its binding site with that of the endocannabinoid 2-AG.

• Publication year

  2013

• Venue

  PeerJ

• Publication date

  2013-09-10

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.7717/peerj.149PMID 24058880PMCID 3775635
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Molecular analysis of the site for 2‐arachidonylglycerol (2‐AG) on the β2 subunit of GABAA receptors

  2013cited by this paper
• N-arachidonoyl glycine suppresses Na+/Ca2+ exchanger-mediated Ca2+ entry into endothelial cells and activates BKCa channels independently of GPCRs

  2013cited by this paper
• Structure, Function, and Modulation of GABAA Receptors*

  2012cited by this paper
• The major central endocannabinoid directly acts at GABAA receptors

  2011cited by this paper
• Molecular Sites for the Positive Allosteric Modulation of Glycine Receptors by Endocannabinoids

  2011cited by this paper
• Minocycline treatment inhibits microglial activation and alters spinal levels of endocannabinoids in a rat model of neuropathic pain

  2009influential reference
• T-Type Calcium Channel Inhibition Underlies the Analgesic Effects of the Endogenous Lipoamino Acids

  2009cited by this paper
• International Union of Pharmacology. LXX. Subtypes of γ-Aminobutyric AcidA Receptors: Classification on the Basis of Subunit Composition, Pharmacology, and Function. Update

  2008cited by this paper
• Identification of Farnesyl Pyrophosphate and N-Arachidonylglycine as Endogenous Ligands for GPR92*

  2008cited by this paper
• Self-assembling cannabinomimetics: supramolecular structures of N-alkyl amides.

  2007cited by this paper
• Actions of N-arachidonyl-glycine in a rat inflammatory pain model

  2007cited by this paper
• A GABAA receptor of defined subunit composition and positioning: Concatenation of five subunits

  2006cited by this paper
• Identification of N-arachidonylglycine as the endogenous ligand for orphan G-protein-coupled receptor GPR18.

  2006cited by this paper
• The Xenopus oocyte: system for the study of functional expression and modulation of proteins.

  2005cited by this paper
• Neurosteroids: endogenous regulators of the GABAA receptor

  2005cited by this paper
• Positioning of the alpha-subunit isoforms confers a functional signature to gamma-aminobutyric acid type A receptors.

  2004cited by this paper
• Positioning of the α-subunit isoforms confers a functional signature to γ-aminobutyric acid type A receptors

  2004cited by this paper
• Individual Properties of the Two Functional Agonist Sites in GABAA Receptors

  2003cited by this paper
• International Union of Pharmacology: Approaches to the Nomenclature of Voltage-Gated Ion Channels

  2003cited by this paper
• Subunit composition, distribution and function of GABA(A) receptor subtypes.

  2002cited by this paper
• The relative amount of cRNA coding for gamma2 subunits affects stimulation by benzodiazepines in GABA(A) receptors expressed in Xenopus oocytes.

  2002cited by this paper
• Forced Subunit Assembly in α1β2γ2 GABAAReceptors

  2002cited by this paper
• Forced subunit assembly in α1β2γ2 GABAA receptors: insight into the absolute arrangement

  2002cited by this paper
• Forced subunit assembly in alpha1beta2gamma2 GABAA receptors. Insight into the absolute arrangement.

  2002cited by this paper
• Subunit Arrangement of γ-Aminobutyric Acid Type A Receptors*

  2001cited by this paper
• Identification of a New Class of Molecules, the Arachidonyl Amino Acids, and Characterization of One Member That Inhibits Pain*

  2001influential reference
• Stoichiometry of a Ligand-gated Ion Channel Determined by Fluorescence Energy Transfer*

  1999cited by this paper
• Structural requirements for binding of anandamide-type compounds to the brain cannabinoid receptor.

  1997cited by this paper
• Stoichiometry and Assembly of a Recombinant GABAA Receptor Subtype

  1997cited by this paper
• Stoichiometry of a Recombinant GABAA Receptor

  1996cited by this paper
• GABA A Receptor Channels

  1996cited by this paper
• Structure and pharmacology of gamma-aminobutyric acidA receptor subtypes.

  1995cited by this paper
• GABAA receptor channels.

  1994cited by this paper
• The effect of subunit composition of rat brain GABAA receptors on channel function.

  1990cited by this paper
• Properties of single sodium channels translated by Xenopus oocytes after injection with messenger ribonucleic acid.

  1987cited by this paper

• Mind Even the First Steps: Colonization by an Alien Perennial Grass, Paspalum Distichum Poses a Threat to the Native Floodplain Vegetation in Hungary

  2025cites this paper
• GABAA receptor modulation by the endocannabinoid system: insights into the regulatory mechanisms involving glutamine synthetase and MAPK mediators

  2024cites this paper
• Goods and Bads of the Endocannabinoid System as a Therapeutic Target: Lessons Learned after 30 Years

  2023cites this paper
• Effects of cannabinoids on ligand-gated ion channels

  2022cites this paper
• Cys-loop receptors on cannabinoids: All high?

  2022cites this paper
• GABAA receptors: structure, function, pharmacology, and related disorders

  2021cites this paper
• MS Binding Assays for Glycine Transporter 2 (GlyT2) Employing Org25543 as Reporter Ligand

  2020cites this paper
• N-Acyl Amino Acids: Metabolism, Molecular Targets, and Role in Biological Processes

  2019cites this paper
• Protective Effect of N-Arachidonoyl Glycine-GPR18 Signaling after Excitotoxical Lesion in Murine Organotypic Hippocampal Slice Cultures

  2019cites this paper
• Fatty Acid Amides and Their Biosynthetic Enzymes Found in Insect Model Systems

  2018cites this paper
• Interactions of endocannabinoid virodhamine and related analogs with human monoamine oxidase‐A and ‐B

  2018cites this paper
• Stereoselective Synthesis of the Isomers of Notoincisol A: Assigment of the Absolute Configuration of this Natural Product and Biological Evaluation

  2018cites this paper
• N-FATTY ACYLGLYCINES: UNDERAPPRECIATED ENDOCANNABINOID-LIKE FATTY ACID AMIDES?

  2017cites this paper
• Synthesis and Characterization of Novel Acyl-Glycine Inhibitors of GlyT2.

  2017cites this paper
• Lid domain plasticity and lipid flexibility modulate enzyme specificity in human monoacylglycerol lipase.

  2017cites this paper
• Endocannabinoid transport revisited.

  2015cites this paper
• Structural analogues of the natural products magnolol and honokiol as potent allosteric potentiators of GABA(A) receptors.

  2014cites this paper
• Endothelial atypical cannabinoid receptor: do we have enough evidence?

  2014cites this paper