2'MeO6MF

SKU: orb1217523

Description

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.

Key Properties

• CAS Number: 89112-85-6
• MW: 266.29
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₄O₃?
• SMILES: O=C1C=C(C2=CC=CC=C2OC)OC3=CC=C(C)C=C13
• Target: GABAA
• Solubility: DMSO:10 mM

Bioactivity

• 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. 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.
• 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 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 α1β2γ2 L GABAA receptors expressed in XenopusM oocytes. 2'MeO6MF enhances the response elicited by GABA at recombinant α1β1, 3γ2 L 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

GABAA