MRK-016

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

MRK-016 is a selective α₅ subunit-containing GABA_A negative allosteric modulator,[1] that has nootropic properties. It has been found to produce rapid, ketamine-like antidepressant effects in animal models of depression.[2]

References

Atack JR, Maubach KA, Wafford KA, O'Connor D, Rodrigues AD, Evans DC, et al. (November 2009). "In vitro and in vivo properties of 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 (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist". The Journal of Pharmacology and Experimental Therapeutics. 331 (2): 470–84. doi:10.1124/jpet.109.157636. PMID 19704033. S2CID 688293.
Fischell J, Van Dyke AM, Kvarta MD, LeGates TA, Thompson SM (October 2015). "Rapid Antidepressant Action and Restoration of Excitatory Synaptic Strength After Chronic Stress by Negative Modulators of Alpha5-Containing GABAA Receptors". Neuropsychopharmacology. 40 (11): 2499–509. doi:10.1038/npp.2015.112. PMC 4569955. PMID 25900119.

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