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2＇MeO6MF

CAS No. : 89112-85-6

MCE 站：2＇MeO6MF

产品活性：2＇MeO6MF 是一种可透过血脑屏障的 α2β1γ2L 和所有含 α1 的 GABA_A 受体的正变构调节剂。2＇MeO6MF 也可以直接激活 α2β2/3 和 α2β2/3γ2L GABA_A 受体。2＇MeO6MF 具有抗焦虑和镇静作用。2＇MeO6MF 可提供神经保护作用并改善功能恢复，还可抑制中风诱发的炎症反应。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：GABA Receptor

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 E_max 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 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.
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 RAWblue^TM 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.

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