ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2012
A common molecular basis for exogenous and endogenous cannabinoid potentiation of glycine receptors.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 22 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 61 citations in OpenAlex.
- A millisecond coarse-grained simulation approach to decipher allosteric cannabinoid binding at the glycine receptor α1.Nature communications · 2024Article
- Deformable Vesicles with Edge Activators for the Transdermal Delivery of Non-Psychoactive Cannabinoids.Current pharmaceutical design · 2024Article
- Review
- Cannabidiol as a modulator of α7 nicotinic receptors.Cellular and molecular life sciences : CMLS · 2022Article
- Positive Allosteric Modulators of Glycine Receptors and Their Potential Use in Pain Therapies.Pharmacological reviews · 2022Review
- Structural basis for cannabinoid-induced potentiation of alpha1-glycine receptors in lipid nanodiscs.Nature communications · 2022Article
- Considerations for Cannabinoids in Perioperative Care by Anesthesiologists.Journal of clinical medicine · 2022Review
- Effects of cannabinoids on ligand-gated ion channels.Frontiers in physiology · 2022Review
- Membrane cholesterol dependence of cannabinoid modulation of glycine receptor.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020Article
- The synthetic cannabinoid dehydroxylcannabidiol restores the function of a major GABAThe Journal of biological chemistry · 2020Article
- CBNeurochemical research · 2018Article
- Glycine receptors and glycine transporters: targets for novel analgesics?Cellular and molecular life sciences : CMLS · 2018Review
- CBNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2018Review
- Recent advances in managing chronic prostatitis/chronic pelvic pain syndrome.F1000Research · 2017Review
- Ethanol effects on glycinergic transmission: From molecular pharmacology to behavior responses.Pharmacological research · 2015Review
- Selective potentiation of alpha 1 glycine receptors by ginkgolic acid.Frontiers in molecular neuroscience · 2015Article
- Long-term potentiation of glycinergic synapses triggered by interleukin 1β.Proceedings of the National Academy of Sciences of the United States of America · 2014Article
- Presynaptic glycine receptors as a potential therapeutic target for hyperekplexia disease.Nature neuroscience · 2014Article
- Seeking structural specificity: direct modulation of pentameric ligand-gated ion channels by alcohols and general anesthetics.Pharmacological reviews · 2014Review
- Why do cannabinoid receptors have more than one endogenous ligand?Philosophical transactions of the Royal Society of London. Series B, Biological sciences · 2012Review
Corrections and comments
- Erratum issuedLi, Fuying [added]; Cheng, Kejun [added]; Rice, Kenner C [added]
Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Both exogenous and endogenous cannabinoids can allosterically modulate glycine receptors (GlyRs). However, little is known about the molecular basis of cannabinoid-GlyR interactions. Here we report that sustained incubation with the endocannabinoid anandamide (AEA) substantially increased the amplitude of glycine-activated current in both rat cultured spinal neurons and in HEK-293 cells expressing human α1, rat α2 and α3 GlyRs. While the α1 and α3 subunits were highly sensitive to AEA-induced potentiation, the α2 subunit was relatively insensitive to AEA. Switching a serine at 296 and 307 in the TM3 (transmembrane domain 3) of the α1 and α3 subunits with an alanine (A) at the equivalent position in the α2 subunit converted the α1/α3 AEA-sensitive receptors to sensitivity resembling that of α2. The S296 residue is also critical for exogenous cannabinoid-induced potentiation of I(Gly). The magnitude of AEA potentiation decreased with removal of either the hydroxyl or oxygen groups on AEA. While desoxy-AEA was significantly less efficacious in potentiating I(Gly), desoxy-AEA inhibited potentiation produced by both Δ(9)-tetrahydrocannabinol (THC), a major psychoactive component of marijuana, and AEA. Similarly, didesoxy-THC, a modified THC with removal of both hydroxyl/oxygen groups, did not affect I(Gly) when applied alone but inhibited the potentiation of I(Gly) induced by AEA and THC. These findings suggest that exogenous and endogenous cannabinoids potentiate GlyRs via a hydrogen bonding-like interaction. Such a specific interaction likely stems from a common molecular basis involving the S296 residue in the TM3 of the α1 and α3 subunits.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.