ArticleThe Journal of biological chemistry2010
Fragrant dioxane derivatives identify beta1-subunit-containing GABAA receptors.
Article in The Journal of biological chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 47 citations in OpenAlex.
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- Effects of Quinine, Quinidine and Chloroquine on Human Muscle Nicotinic Acetylcholine Receptors.Frontiers in pharmacology · 2018Article
- Nuclear Respiratory Factor 1 (NRF-1) Controls the Activity Dependent Transcription of the GABA-A Receptor Beta 1 Subunit Gene in Neurons.Frontiers in molecular neuroscience · 2018Article
- Molecular tools for GABAScientific reports · 2017Article
- Potentiating effect of glabridin fromBiochemistry and biophysics reports · 2016Article
- Kampo Medicine: Evaluation of the Pharmacological Activity of 121 Herbal Drugs on GABAA and 5-HT3A Receptors.Frontiers in pharmacology · 2016Article
- Pharmacological characterisation of murine α4β1δ GABAA receptors expressed in Xenopus oocytes.BMC neuroscience · 2015Article
- Identification of amino acids involved in histamine potentiation of GABA A receptors.Frontiers in pharmacology · 2015Article
- GABA(A) receptor modulation by terpenoids from Sideritis extracts.Molecular nutrition & food research · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels.British journal of pharmacology · 2013Article
- Benzodiazepine-site pharmacology on GABAA receptors in histaminergic neurons.British journal of pharmacology · 2013Article
- Alterations in Purkinje cell GABAA receptor pharmacology following oxygen and glucose deprivation and cerebral ischemia reveal novel contribution of β1 -subunit-containing receptors.The European journal of neuroscience · 2013Article
- Transient receptor potential channels encode volatile chemicals sensed by rat trigeminal ganglion neurons.PloS one · 2013Article
- Partial agonism of taurine at gamma-containing native and recombinant GABAA receptors.PloS one · 2013Article
- GABAergic inhibition of histaminergic neurons regulates active waking but not the sleep-wake switch or propofol-induced loss of consciousness.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2012Article
- α4βδ GABA(A) receptors are high-affinity targets for γ-hydroxybutyric acid (GHB).Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- A novel GABA(A) receptor pharmacology: drugs interacting with the α(+) β(-) interface.British journal of pharmacology · 2012Review
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nineteen GABA(A) receptor (GABA(A)R) subunits are known in mammals with only a restricted number of functionally identified native combinations. The physiological role of beta1-subunit-containing GABA(A)Rs is unknown. Here we report the discovery of a new structural class of GABA(A)R positive modulators with unique beta1-subunit selectivity: fragrant dioxane derivatives (FDD). At heterologously expressed alpha1betaxgamma2L (x-for 1,2,3) GABA(A)R FDD were 6 times more potent at beta1- versus beta2- and beta3-containing receptors. Serine at position 265 was essential for the high sensitivity of the beta1-subunit to FDD and the beta1N286W mutation nearly abolished modulation; vice versa the mutation beta3N265S shifted FDD sensitivity toward the beta1-type. In posterior hypothalamic neurons controlling wakefulness GABA-mediated whole-cell responses and GABAergic synaptic currents were highly sensitive to FDD, in contrast to beta1-negative cerebellar Purkinje neurons. Immunostaining for the beta1-subunit and the potency of FDD to modulate GABA responses in cultured hypothalamic neurons was drastically diminished by beta1-siRNA treatment. In conclusion, with the help of FDDs we reveal a functional expression of beta1-containing GABA(A)Rs in the hypothalamus, offering a new tool for studies on the functional diversity of native GABA(A)Rs.
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