ArticleBritish journal of pharmacology2012
2'-Methoxy-6-methylflavone: a novel anxiolytic and sedative with subtype selective activating and modulating actions at GABA(A) receptors.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers, 1 of them a synthesis that pooled it.
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Who cites it
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 50 citations in OpenAlex.
- Flavonoids as Anxiolytics in Animal Tests: Systematic Review, Meta-Analysis, and Bibliometrical Analysis.Phytotherapy research : PTR · 2026Pooled it
- Attenuation of Streptozotocin-Induced Diabetic Neuropathic Allodynia by Flavone Derivative Through Modulation of GABA-ergic Mechanisms and Endogenous Biomarkers.Neurochemical research · 2024Article
- Antioxidants in neuropsychiatric disorder prevention: neuroprotection, synaptic regulation, microglia modulation, and neurotrophic effects.Frontiers in neuroscience · 2024Review
- Antidepressant Activities of Synthesized Benzodiazepine Analogues in Mice.Brain sciences · 2023Article
- Antiamnesic Effects of Feralolide Isolated from Aloe vera Resin Miller against Learning Impairments Induced in MiceAntioxidants (Basel, Switzerland) · 2023Article
- Phenolics as GABAMolecules (Basel, Switzerland) · 2022Review
- Involvement of selective GABA-A receptor subtypes in amelioration of cisplatin-induced neuropathic pain by 2'-chloro-6-methyl flavone (2'-Cl-6MF).Naunyn-Schmiedeberg's archives of pharmacology · 2021Article
- The flavonoid, 2'-methoxy-6-methylflavone, affords neuroprotection following focal cerebral ischaemia.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2019Article
- Anti-nociceptive and Anti-inflammatory Activities of Asparacosin A Involve Selective Cyclooxygenase 2 and Inflammatory Cytokines Inhibition: AnFrontiers in immunology · 2019Article
- Phytochemical analysis and antidiabetic potential of Elaeagnus umbellata (Thunb.) in streptozotocin-induced diabetic rats: pharmacological and computational approach.BMC complementary and alternative medicine · 2018Article
- Hepatoprotective activity of viscosine is mediated by attenuation of hepatic macrophages and iNOS expression in CClToxicology research · 2016Article
- Zolpidem is a potent stoichiometry-selective modulator of α1β3 GABAA receptors: evidence of a novel benzodiazepine site in the α1-α1 interface.Scientific reports · 2016Article
- Anticonvulsant, Anxiolytic, and Sedative Activities ofFrontiers in pharmacology · 2016Article
- GABA-A Receptor Modulation and Anticonvulsant, Anxiolytic, and Antidepressant Activities of Constituents from Artemisia indica Linn.Evidence-based complementary and alternative medicine : eCAM · 2016Article
- Article
- Modulation of ionotropic GABA receptors by 6-methoxyflavanone and 6-methoxyflavone.Neurochemical research · 2014Article
- Flavonoids as GABAA receptor ligands: the whole story?Journal of experimental pharmacology · 2012Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeFlavonoids are known to have anxiolytic and sedative effects mediated via actions on ionotropic GABA receptors. We sought to investigate this further. EXPERIMENTAL APPROACH: We evaluated the effects of 2'-methoxy-6-methylflavone (2'MeO6MF) on native GABA(A) receptors in new-born rat hippocampal neurons and determined specificity from 18 human recombinant GABA(A) receptor subtypes expressed in Xenopus oocytes. We used ligand binding, two-electrode voltage clamp and patch clamp studies together with behavioural studies. KEY
results2'MeO6MF potentiated GABA at α2β1γ2L and all α1-containing GABA(A) receptor subtypes. At α2β2/3γ2L GABA(A) receptors, however, 2'MeO6MF directly activated the receptors without potentiating GABA. This activation was attenuated by bicuculline and gabazine but not flumazenil indicating a novel site. Mutation studies showed position 265 in the β1/2 subunit was key to whether 2'MeO6MF was an activator or a potentiator. In hippocampal neurons, 2'MeO6MF directly activated single-channel currents that showed the hallmarks of GABA(A) Cl(-) currents. In the continued presence of 2'MeO6MF the single-channel conductance increased and these high conductance channels were disrupted by the γ2(381-403) MA peptide, indicating that such currents are mediated by α2/γ2-containing GABA(A) receptors. In mice, 2'MeO6MF (1-100 mg·kg(-1) ; i.p.) displayed anxiolytic-like effects in two unconditioned models of anxiety: the elevated plus maze and light/dark tests. 2'MeO6MF induced sedative effects at higher doses in the holeboard, actimeter and barbiturate-induced sleep time tests. No myorelaxant effects were observed in the horizontal wire test. CONCLUSIONS AND IMPLICATIONS: 2'MeO6MF will serve as a tool to study the complex nature of the activation and modulation of GABA(A) receptor subtypes.
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