MRK-016
Chemical compound
Names | |
---|---|
Preferred IUPAC name
3-
tert
-Butyl-7-(5-methyl-1,2-oxazol-3-yl)-2-[(1
H
-1,2,4-triazol-5-yl)methoxy]pyrazolo[1,5-
d
][1,2,4]triazine
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Identifiers | |
3D model (
JSmol
)
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ChemSpider | |
PubChem
CID
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UNII | |
CompTox Dashboard
(
EPA
)
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Properties | |
C 17 H 20 N 8 O 2 | |
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).
|
MRK-016 is a selective α 5 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]
See also
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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