2'MeO6MF 

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABA_A receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABA_A receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response^[1][2].

GABA_A receptor^[1]

2'MeO6MF (100-300 µM; 60 min) weakly displaces [³H]-flunitrazepam binding to rat brain synaptosomal membranes by 5-10%. 2'MeO6MF enhances [³H]-muscimol binding to rat brain synaptic membranes in a concentration-dependent manner yielding a mean E_max of 219.8% and apparent EC₅₀=20.8 nM^[1].
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^[1].
2'MeO6MF (1-10 µM; 60 min) increases tonic inhibitory currents in a concentration-dependent manner in granule cells^[2].
2'MeO6MF (100-1000 µM; 6.5 h) inhibits the LPS-induced increase of NFkB activity in RAWblue^TM macrophage cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

2'MeO6MF (1-100 mg/kg; i.p.) displays anxiolytic-like effects in the elevated plus maze and light/dark tests. 2'MeO6MF induces sedative effects at higher doses in the holeboard, actimeter and barbiturate-induced sleep time tests^[1].
2'MeO6MF (30 mg/kg; i.p.) increases tonic currents in layer 2/3 pyramidal neurons of mice after stroke^[2].
2'MeO6MF (0.1-30 mg/kg; i.p.) is neuroprotective and enhances functional recovery after focal cerebral ischaemia in mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

266.29

C₁₇H₁₄O₃

89112-85-6

O=C1C=C(C2=CC=CC=C2OC)OC3=CC=C(C)C=C13

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Karim N, et, al. 2'-Methoxy-6-methylflavone: a novel anxiolytic and sedative with subtype selective activating and modulating actions at GABA(A) receptors. Br J Pharmacol. 2012 Feb;165(4):880-96.  [Content Brief]

  [2]. Clarkson AN, et, al. The flavonoid, 2'-methoxy-6-methylflavone, affords neuroprotection following focal cerebral ischaemia. J Cereb Blood Flow Metab. 2019 Jul;39(7):1266-1282.  [Content Brief]