MK-0343

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MK-0343 (MRK-409) 是一种有效的 α2/3 亚型选择性部分 GABAA 受体激动剂。

MK-0343 (MRK-409) is a potent, α2/3 subtype selective, partial GABAA receptor agonist, shows greater agonist efficacy at the α3 over α1 subtypes; readily penetrates the brain in rats and occupies the benzodiazepine site of GABA(A) receptors with an Occ(50) of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL; produces anxiolytic-like activity in rodent and primate unconditioned and conditioned models of anxiety.

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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. Animal Model:Male Sprague-Dawley rats (approximately 250–300g) (pharmacokinetics)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.

MRK-409 | MK0343

Membrane Transporter/Ion Channel

GAT

GAT

Other Indications

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233275-76-8

397.39

C19H17F2N7O

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (629.12 mM)

CN1N=CN=C1COC2=NN3C(C=C2C4CCC4)=NN=C3C5=C(F)C=CC=C5F

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

(-20℃)

With Ice Pack

≥ 2 years