MK 0343

Catalog # Availability Size / Price Qty
4415/10
4415/50
MK 0343 | CAS No. 233275-76-8 | GABA-A Receptor Agonists
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Description: GABAA partial agonist; displays subtype selectivity

Chemical Name: 7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazo[4,3-b]pyridazine

Purity: ≥99%

Product Details
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Biological Activity

Subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively); occupies the benzodiazepine site of GABAA receptors. Displays greater agonist efficacy at α3 compared to α1. Exhibits anxiolytic and non-sedating properties in rodent models. Brain penetrant.

Technical Data

M.Wt:
397.38
Formula:
C19H17F2N7O
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
233275-76-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.
    Atack et al.
    J.Psychopharmacol., 2011;25:314
  2. Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABAA α2,3 subtype-selective agonist, compared to L.pam and placebo in healthy male volunteers.
    de Haas et al.
    J.Psychopharmacol., 2008;22:24
  3. Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, prima
    Atack et al.
    J.Pharmacol.Exp.Ther., 2010;332:17

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