1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. 2'MeO6MF

2'MeO6MF 

Cat. No.: HY-131997
Handling Instructions

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 sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.

For research use only. We do not sell to patients.

2'MeO6MF Chemical Structure

2'MeO6MF Chemical Structure

CAS No. : 89112-85-6

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Description

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 sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response[1][2].

IC50 & Target

GABAA receptor[1]

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[1].
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[1].
2'MeO6MF (1-10 µM; 60 min) increases tonic inhibitory currents in a concentration-dependent manner in granule cells[2].
2'MeO6MF (100-1000 µM; 6.5 h) inhibits the LPS-induced increase of NFkB activity in RAWblueTM macrophage cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].
2'MeO6MF (30 mg/kg; i.p.) increases tonic currents in layer 2/3 pyramidal neurons of mice after stroke[2].
2'MeO6MF (0.1-30 mg/kg; i.p.) is neuroprotective and enhances functional recovery after focal cerebral ischaemia in mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Balb-c mice (8-10 weeks, 25-35 g)[1]
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.
Molecular Weight

266.29

Formula

C₁₇H₁₄O₃

CAS No.

89112-85-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

2'MeO6MFGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorα2β1γ2Lα1GABAAα2β2/3α2β2/3γ2LanxiolyticsedativeneuroprotectionstrokeinflammatoryInhibitorinhibitorinhibit

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2'MeO6MF
Cat. No.:
HY-131997
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