الصفحة الرئيسية>>Signaling Pathways>> Membrane Transporter/Ion Channel>> GABA Receptor>>2'MeO6MF

2'MeO6MF

رقم الكتالوجGC70652

2'MeO6MF هو معدل تفارغي إيجابي في الدماغ عند α2β1γ2L وجميع مستقبلات GABAA التي تحتوي على α1.

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2'MeO6MF التركيب الكيميائي

Cas No.: 89112-85-6

الحجم السعر المخزون الكميّة
1 mg
199٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
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.

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[1].
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[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 RAWblueTM macrophage cells[2].

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].

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.

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