| Bioactivity | MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic[1]. | ||||||||||||
| Target | Ki: 0.22 nM (rGABAA α1), 0.4 nM (rGABAAα2) , 0.21 nM (rGABAAα3), 78 nM (rGABAAα4), 0.23 nM (rGABAAα5), 980 nM (rGABAAα6) | ||||||||||||
| In Vivo | MK0343 readily penetrates the brain in rats and occupies the benzodiazepine site of GABAA receptors, measured using an in vivo [3H]flumazenil binding assay, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL[1]. Animal Model: | ||||||||||||
| Name | MK-0343 | ||||||||||||
| CAS | 233275-76-8 | ||||||||||||
| Formula | C19H17F2N7O | ||||||||||||
| Molar Mass | 397.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Atack JR, et al. 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. 2011 Mar;25(3):314-28. |