Drug intelligence / Profile preview

6-methoxyflavanone

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

6-Methoxyflavanone (6-MeOF) is a flavonoid small molecule primarily utilized as a research-use-only reagent. It acts as a blood-brain-barrier-penetrant positive allosteric modulator (PAM) of GABA-A receptors, specifically targeting the α1β2γ2L and α2β2γ2L subtypes while remaining relatively inactive at α1β2 receptors. Additionally, 6-methoxyflavanone acts as an antagonist of the bitter taste receptors hTAS2R14 (T2R14) and hTAS2R39 (T2R39). Preclinical studies in rodent models suggest that 6-methoxyflavanone possesses anxiolytic, analgesic, and anti-inflammatory properties, demonstrating efficacy in reducing neuropathic pain, allodynia, and vulvodynia. In vitro and in vivo research also indicates that by targeting T2R14, 6-methoxyflavanone can modulate CD4+ T-cell differentiation, suppressing Th1 and Th17 differentiation while promoting Th2 polarization, which highlights its potential therapeutic application in immune thrombocytopenia (ITP).

Other names
6-MeOF6-methoxy-2-phenyl-2,3-dihydro-4H-chromen-4-one6-methoxy-2-phenylchroman-4-one
02

Targets

GABAA (Gamma-aminobutyric acid receptor)TAS2R14 (Taste receptor type 2 member 14)

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