ArticleNaunyn-Schmiedeberg's archives of pharmacology2010
Lack of positive allosteric modulation of mutated alpha(1)S267I glycine receptors by cannabinoids.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
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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.
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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
14 citing papers in PubMed, 1 synthesis or guideline pooled it, 26 citations in OpenAlex.
- Cys-loop receptors on cannabinoids: All high?Frontiers in physiology · 2022Pooled it
- A millisecond coarse-grained simulation approach to decipher allosteric cannabinoid binding at the glycine receptor α1.Nature communications · 2024Article
- Positive Allosteric Modulators of Glycine Receptors and Their Potential Use in Pain Therapies.Pharmacological reviews · 2022Review
- 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
- The (Poly)Pharmacology of Cannabidiol in Neurological and Neuropsychiatric Disorders: Molecular Mechanisms and Targets.International journal of molecular sciences · 2021Review
- A Balanced Approach for Cannabidiol Use in Chronic Pain.Frontiers in pharmacology · 2020Review
- Binding and Signaling Studies Disclose a Potential Allosteric Site for Cannabidiol in Cannabinoid CBFrontiers in pharmacology · 2017Article
- Mutations at beta N265 in γ-aminobutyric acid type A receptors alter both binding affinity and efficacy of potent anesthetics.PloS one · 2014Article
- Cannabinoids suppress inflammatory and neuropathic pain by targeting α3 glycine receptors.The Journal of experimental medicine · 2012Article
- A common molecular basis for exogenous and endogenous cannabinoid potentiation of glycine receptors.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2012Article
- Allosteric modulation of glycine receptors.British journal of pharmacology · 2011Review
- Molecular sites for the positive allosteric modulation of glycine receptors by endocannabinoids.PloS one · 2011Article
- Molecular Targets of the Phytocannabinoids: A Complex Picture.Progress in the chemistry of organic natural productsReview
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Loss of inhibitory synaptic transmission within the dorsal horn of the spinal cord plays a key role in the development of chronic pain following inflammation or nerve injury. Inhibitory postsynaptic transmission in the adult spinal cord involves mainly glycine. Ajulemic acid and HU210 are non-psychotropic, synthetic cannabinoids. Cannabidiol is a non-psychotropic plant constituent of cannabis sativa. There are hints that non-cannabinoid receptor mechanisms of these cannabinoids might be mediated via glycine receptors. In this study, we investigated the impact of the amino acid residue serine at position 267 on the glycine-modulatory effects of ajulemic acid, cannabidiol and HU210. Mutated alpha(1)S267I glycine receptors transiently expressed in HEK293 cells were studied by utilising the whole-cell clamp technique. The mutation of the alpha(1) subunit TM2 serine residue to isoleucine abolished the co-activation and the direct activation of the glycine receptor by the investigated cannabinoids. The nature of the TM2 (267) residue of the glycine alpha(1) subunit is crucial for the glycine-modulatory effect of ajulemic acid, cannabidiol and HU210. An investigation of the impact of such mutations on the in vivo interaction of cannabinoids with glycine receptors should permit a better understanding of the molecular determinants of action of cannabinoids.
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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.