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MK 0343Cat. No. 4415 |
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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 |
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.Certificate of Analysis / Safety Data Sheet
References
de Haas et al (2008) Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABAA α2,3 subtype-selective agonist, compared to lorazepam and placebo in healthy male volunteers. J.Psychopharmacol. 22 24. PMID: 18187530.
Atack et al (2010) 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, primates, and humans. J.Pharmacol.Exp.Ther. 332 17.
Atack et al (2011) MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. J.Psychopharmacol. 25 314. PMID: 20147571.
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Keywords: MK 0343, supplier, MK0343, gabaa, subtype-selective, partial, agonists, α3, alpha3, a3, anxiolytics, brain, penetrant
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