Name | 2-(2-METHOXYPHENYL)-6-METHYL-4H-1-BENZOPYRAN-4-ONE |
Synonyms | 2'MeO6MF 2'MEO6MF 2-(2-METHOXYPHENYL)-6-METHYL-4H-1-BENZOPYRAN-4-ONE 4H-1-Benzopyran-4-one, 2-(2-methoxyphenyl)-6-methyl- |
CAS | 89112-85-6 |
Molecular Formula | C17H14O3 |
Molar Mass | 266.29 |
In vitro study | 2'MeO6MF (100-300 µM; 60 min) weakly displaces [ 3 H]-flunitrazepam binding to rat brain synaptosomal membranes by 5-10%. 2'MeO6MF enhances [ 3 H]-muscimol binding to rat brain synaptic membranes in a concentration-dependent manner yielding a mean E max of 219.8% and apparent EC 50 =20.8 nM. 2'MeO6MF (1-300 µM) enhances the response elicited by a low concentration of GABA in a concentration-dependent manner at recombinant α1β2γ2L GABA A receptors expressed in XenopusM oocytes. 2'MeO6MF enhances the response elicited by GABA at recombinant α1β1,3γ2L and α1β2 GABA A receptors without any direct activation. 2'MeO6MF (1-10 µM; 60 min) increases tonic inhibitory currents in a concentration-dependent manner in granule cells. 2'MeO6MF (100-1000 µM; 6.5 h) inhibits the LPS-induced increase of NFkB activity in RAWblue TM macrophage cells. |
Biological activity | 2'MeO6MF is a positive allosteric regulator of α2β1γ2L that can penetrate the blood-brain barrier and all α1-containing GABAA receptors. 2 'MeO6MF can also directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anti-anxiety and sedative effects. 2 'MeO6MF provides neuroprotection and improves functional recovery, and also inhibits stroke-induced inflammatory responses. |
target | GABA A receptor |
Animal Model: | Male Balb-c mice (8-10 weeks, 25-35 g) |
Dosage: | 1, 10, 30, 100 mg/kg |
Administration: | I.p. |
Result: | No overt acute toxicity was observed. Exerted anxiolytic effects at low doses and sedative effects at high doses without myorelaxant effects. |