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Chemical Structure| 233275-76-8 Chemical Structure| 233275-76-8

Structure of MK-0343
CAS No.: 233275-76-8

Chemical Structure| 233275-76-8

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MK 0343 is a selective partial agonist of GABAAα3, α1, α5 and α2 with Ki values of 0.21 nM-0.40 nM. It displays anxiolytic activity in rodent and primate models.

Synonyms: MRK-409

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Product Details of MK-0343

CAS No. :233275-76-8
Formula : C19H17F2N7O
M.W : 397.38
SMILES Code : CN1N=CN=C1COC2=NN3C(C=C2C4CCC4)=NN=C3C5=C(C=CC=C5F)F
Synonyms :
MRK-409
MDL No. :MFCD22683821
InChI Key :GOIFCXRIFSYPFG-UHFFFAOYSA-N
Pubchem ID :22609888

Safety of MK-0343

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.16mL

5.03mL

2.52mL

References

[1]Atack JR, Wafford KA, 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.

[2]de Haas SL, de Visser SJ, et al. Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABA(A) alpha2,3 subtype selective agonist, compared to lorazepam and placebo in healthy male volunteers. J Psychopharmacol. 2008 Jan;22(1):24-32.

[3]Brohan J, Goudra BG. The Role of GABA Receptor Agonists in Anesthesia and Sedation. CNS Drugs. 2017 Oct;31(10):845-856. doi: 10.1007/s40263-017-0463-7. PMID: 29039138.

[4]Atack JR, Wafford KA, Street LJ, Dawson GR, Tye S, Van Laere K, Bormans G, Sanabria-Bohórquez SM, De Lepeleire I, de Hoon JN, Van Hecken A, Burns HD, McKernan RM, Murphy MG, Hargreaves RJ. 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. doi: 10.1177/0269881109354927. Epub 2010 Feb 10. PMID: 20147571.

[5]de Haas SL, de Visser SJ, van der Post JP, Schoemaker RC, van Dyck K, Murphy MG, de Smet M, Vessey LK, Ramakrishnan R, Xue L, Cohen AF, van Gerven JM. Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABA(A) alpha2,3 subtype selective agonist, compared to lorazepam and placebo in healthy male volunteers. J Psychopharmacol. 2008 Jan;22(1):24-32. doi: 10.1177/0269881107082108. PMID: 18187530.

 

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