产品
编 号：F726166
分子式：C17H14O3
分子量：266.29
分子式：C17H14O3
分子量：266.29
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CAS No: 89112-85-6
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 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.
体内研究：
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.
体外研究：
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.
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