ArticlePloS one2013
Partial agonism of taurine at gamma-containing native and recombinant GABAA receptors.
Article in PloS one, 2013. 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 16 papers.
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Who cites it
16 citing papers in PubMed, 27 citations in OpenAlex.
- Cerebellar tonic inhibition orchestrates the maturation of information processing and motor coordination.Experimental & molecular medicine · 2026Article
- Orphan receptor GPR158 serves as a metabotropic glycine receptor: mGlyR.Science (New York, N.Y.) · 2023Article
- Maternal taurine as a modulator of ClFrontiers in cellular neuroscience · 2023Review
- Taurine: A Maternally Derived Nutrient Linking Mother and Offspring.Metabolites · 2022Review
- Taurine and Astrocytes: A Homeostatic and Neuroprotective Relationship.Frontiers in molecular neuroscience · 2022Review
- Activation of the α1β2γ2L GABABiomolecules · 2021Article
- Pharmacological Evaluation of Drugs in Animal Models of Tinnitus.Current topics in behavioral neurosciences · 2021Review
- Enhancing neuronal chloride extrusion rescues α2/α3 GABANature communications · 2020Article
- Taurine Suppression of Central Amygdala GABAergic Inhibitory Signaling via Glycine Receptors Is Disrupted in Alcohol Dependence.Alcoholism, clinical and experimental research · 2020Article
- Steady-state activation of the high-affinity isoform of the α4β2δ GABAScientific reports · 2019Article
- Steady-state activation and modulation of the synaptic-type α1β2γ2L GABAPhysiological reports · 2019Article
- Taurine as an Essential Neuromodulator during Perinatal Cortical Development.Frontiers in cellular neuroscience · 2017Review
- Roles of taurine-mediated tonic GABAA receptor activation in the radial migration of neurons in the fetal mouse cerebral cortex.Frontiers in cellular neuroscience · 2014Article
- Benzodiazepine-site pharmacology on GABAA receptors in histaminergic neurons.British journal of pharmacology · 2013Article
- Taurine Promotes Retinal Ganglion Cell Survival Through GABAAdvances in experimental medicine and biologyArticle
- Putative Role of Taurine as Neurotransmitter During Perinatal Cortical Development.Advances in experimental medicine and biologyArticle
Corrections and comments
- Erratum issued
Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Taurine is a semi-essential sulfonic acid found at high concentrations in plasma and mammalian tissues which regulates osmolarity, ion channel activity and glucose homeostasis. The structural requirements of GABAA-receptors (GABAAR) gated by taurine are not yet known. We determined taurine potency and efficacy relative to GABA at different types of recombinant GABAAR occurring in central histaminergic neurons of the mouse hypothalamic tuberomamillary nucleus (TMN) which controls arousal. At binary α(1/2)β(1/3) receptors taurine was as efficient as GABA, whereas incorporation of the γ(1/2) subunit reduced taurine efficacy to 60-90% of GABA. The mutation γ(2F77I), which abolishes zolpidem potentiation, significantly reduced taurine efficacy at recombinant and native receptors compared to the wild type controls. As taurine was a full- or super- agonist at recombinant αxβ1δ-GABAAR, we generated a chimeric γ(2) subunit carrying the δ subunit motif around F77 (MTVFLH). At α(1/2)β(1)γ2(MTVFLH) receptors taurine became a super-agonist, similar to δ-containing ternary receptors, but remained a partial agonist at β3-containing receptors. In conclusion, using site-directed mutagenesis we found structural determinants of taurine's partial agonism at γ-containing GABAA receptors. Our study sheds new light on the β1 subunit conferring the widest range of taurine-efficacies modifying GABAAR function under (patho)physiological conditions.
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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.