233275-76-8

233275-76-8 structure

Name: MK 0343
Chemical Name: 7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol -5-yl)methoxy][1,2,4]triazolo[4,3-b]pyridazine
CAS Number: 233275-76-8
Molecular Formula: C₁₉H₁₇F₂N₇O
Molecular Weight: 397.38100
Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
Create Date: 2016-07-23 04:54:12
Modify Date: 2025-08-25 13:10:19
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic[1].

Name	7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol -5-yl)methoxy][1,2,4]triazolo[4,3-b]pyridazine
Synonyms	7-cyclobutyl-3-(2,6-difluorophenyl)-6-(2-methyl-2H-1,2,4-triazol-3-ylmethoxy)-1,2,4-triazolo[4,3-b]pyridazine (6-OXO-5,6,7,8-TETRAHYDROPTERIDIN-7-YL)ACETONITRILE 7-Cyanomethyl-7.8-dihydro-6-hydroxy-pteridin 7-cyclobutyl-6-(2-methyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2,6-difluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine 7-Cyanmethyl-7,8-dihydro-6-hydroxy-pteridin

Description	MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic[1].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor Research Areas >> Neurological Disease Signaling Pathways >> Neuronal Signaling >> GABA Receptor
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)[1]
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: Male Sprague-Dawley rats (approximately 250–300g) (pharmacokinetics)[1] Dosage: 1, 2 or 3 mg/kg Administration: Oral administration Result: Readily penetrated the brain in rats and occupies the benzodiazepine site of GABAA receptors, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL.
References	[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.

RIDADR	NONH for all modes of transport