2'MeO6MF

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

2'MeO6MF 是 α2β1γ2L 和所有含 α1 GABAA 受体的脑渗透性正变构调节剂。

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.It?offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.?2'MeO6MF has anxiolytic and sedative effects.

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.

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. 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.

——

Membrane Transporter/Ion Channel

Other Targets

GABAA

——

——

89112-85-6

266.29

C17H14O3?

>98% (HPLC)

DMSO:10 mM

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

——

(-20℃)

With Ice Pack

≥ 2 years