2'MeO6MF free base

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.

For research use only. Not for human or veterinary use.

Target GABA Receptor

Research area Neurological Disease Inflammation/Immunology

Purity >98% Stock Inquire

Data Sheet SDS COA

2'MeO6MF structure

CAS No.: 89112-85-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 360.00	BP-02442-50mg	In stock	Get quote
100 mg	USD 580.00	BP-02442-100mg	In stock	Get quote
250 mg	USD 1,150.00	BP-02442-250mg	In stock	Get quote
500 mg	USD 1,840.00	BP-02442-500mg	In stock	Get quote
1 g	USD 2,950.00	BP-02442-1g	In stock	Get quote
2 g	USD 4,700.00	BP-02442-2g	In stock	Get quote
3 g	Inquire	BP-02442-3g	In stock	Inquire

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Description

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

Biological activity

In Vitro 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 Emax of 219.8% and apparent EC50=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 GABAA receptors expressed in XenopusM oocytes. 2'MeO6MF enhances the response elicited by GABA at recombinant α1β1,3γ2L and α1β2 GABAA 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 RAWblueTM macrophage cells. In Vivo 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. 2'MeO6MF (30 mg/kg; i.p.) increases tonic currents in layer 2/3 pyramidal neurons of mice after stroke. 2'MeO6MF (0.1-30 mg/kg; i.p.) is neuroprotective and enhances functional recovery after focal cerebral ischaemia in mice.

Identifiers

SMILES: O=C1C=C(C2=CC=CC=C2OC)OC3=CC=C(C)C=C13
InChIKey: QEIHFNZSIRWEBX-UHFFFAOYSA-N

Specifications

MW (average): 266.2913
Formula: C₁₇H₁₄O₃
CAS No.: 89112-85-6
Physical state: Solid
Color: White to off-white
Shipping: —
Storage: —

Documents

References

[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.

[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.

Same target

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Same research area

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