2'MEO6MF
2'MEO6MF 用途与合成方法
GABA A receptor
2'MeO6MF (100-300 µM; 60 min) weakly displaces [
3
H]-flunitrazepam binding to rat brain synaptosomal membranes by 5-10%. 2'MeO6MF enhances [
3
H]-muscimol binding to rat brain synaptic membranes in a concentration-dependent manner yielding a mean E
max
of 219.8% and apparent EC
50
=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.
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. |
