MRK-016

MRK-016 is a selective α₅ subunit-containing GABA_A negative allosteric modulator that has nootropic properties. It has been found to produce rapid, ketamine-like antidepressant effects in animal models of depression.[1]

MRK-016

Names
IUPAC name 3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo(1,5-d)(1,2,4)triazine
Identifiers
CAS Number	783331-24-8
3D model (JSmol)	Interactive image
ChemSpider	5293780
PubChem CID	6918583
CompTox Dashboard (EPA)	DTXSID60426080
InChI InChI=1S/C17H20N8O2/c1-10-6-11(23-27-10)15-21-19-7-12-14(17(2,3)4)16(22-25(12)15)26-8-13-18-9-20-24(13)5/h6-7,9H,8H2,1-5H3 Key: QYSYOGCIDRANAR-UHFFFAOYSA-N
SMILES CN1N=CN=C1COC1=NN2C(C=NN=C2C2=NOC(C)=C2)=C1C(C)(C)C
Properties
Chemical formula	C17H20N8O2
Molar mass	368.401 g·mol^−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

See also

• GABA_A receptor negative allosteric modulator
• GABA_A receptor § Ligands

References

1. Fischell, Jonathan; Van Dyke, Adam M; Kvarta, Mark D; LeGates, Tara A; Thompson, Scott M (2015). "Rapid Antidepressant Action and Restoration of Excitatory Synaptic Strength After Chronic Stress by Negative Modulators of Alpha5-Containing GABAA Receptors". Neuropsychopharmacology. 40: 2499–2509. doi:10.1038/npp.2015.112. ISSN 0893-133X. PMC 4569955. PMID 25900119.