ArticleNeurochemical research2014
Modulation of ionotropic GABA receptors by 6-methoxyflavanone and 6-methoxyflavone.
Article in Neurochemical research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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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
10 citing papers in PubMed.
- 6-Hydroxyflavanone treats anxiety and chemotherapy-induced neuropathy in Sprague-Dawley rats.Frontiers in pharmacology · 2024Article
- Metabolite Production inmSystems · 2022Article
- Phenolics as GABAMolecules (Basel, Switzerland) · 2022Review
- 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway in HeLa cells.Bioengineered · 2022Article
- 6-Methoxyflavone and Donepezil Behavioral Plus Neurochemical Correlates in Reversing Chronic Ethanol and Withdrawal Induced Cognitive Impairment.Drug design, development and therapy · 2022Article
- Antinociceptive effect of plant-based natural products in chemotherapy-induced peripheral neuropathies: A systematic review.Frontiers in pharmacology · 2022Review
- Natural Medicines for the Treatment of Epilepsy: Bioactive Components, Pharmacology and Mechanism.Frontiers in pharmacology · 2021Review
- Exploring the Promise of Flavonoids to Combat Neuropathic Pain: From Molecular Mechanisms to Therapeutic Implications.Frontiers in neuroscience · 2020Review
- Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative.Molecules (Basel, Switzerland) · 2017Article
- GABA-ρ receptors: distinctive functions and molecular pharmacology.British journal of pharmacology · 2017Review
Corrections and comments
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We evaluated the effects of 6-methoxyflavanone and 6-methoxyflavone on wild-type α1/α2β2γ2L GABAA and ρ1 GABAC receptors and on mutant ρ1I307S, ρ1W328 M, ρ1I307S/W328 M GABAC receptors expressed in Xenopus oocytes using two-electrode voltage clamp and radioligand binding. 6-Methoxyflavanone and 6-methoxyflavone act as a flumazenil-insensitive positive allosteric modulator of GABA responses at human recombinant α1β2γ2L and α2β2γ2L GABAA receptors. However, unlike 6-methoxyflavone, 6-methoxyflavanone was relatively inactive at α1β2 GABAA receptors. 6-Methoxyflavanone inhibited [(3)H]-flunitrazepam binding to rat brain membranes. Both flavonoids were found to be inactive as modulators at ρ1, ρ1I307S and ρ1W328 M GABA receptors but acted as positive allosteric modulators of GABA at the benzodiazepine sensitive ρ1I307S/W328 M GABA receptors. This double mutant retains ρ1 properties of being insensitive to bicuculline and antagonised by TPMPA and THIP. Additionally, 6-methoxyflavanone was also a partial agonist at ρ1W328 M GABA receptors. The relative inactivity of 6-methoxyflavanone at α1β2 GABAA receptors and it's partial agonist action at ρ1W328 M GABA receptors suggest that it exhibits a unique profile not matched by other flavonoids.
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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.