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MRK-016

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MRK-016
Names
Preferred IUPAC name 3-tert-Butyl-7-(5-methyl-1,2-oxazol-3-yl)-2-pyrazolotriazine
Identifiers
CAS Number
3D model (JSmol)
ChemSpider
PubChem CID
UNII
CompTox Dashboard (EPA)
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,8H2,1-5H3Key: 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
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). Infobox references
Chemical compound

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

See also

References

  1. 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-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.
  2. 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.
GABA receptor modulators
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
GABAA-ρTooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABABTooltip γ-Aminobutyric acid B receptor
See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators
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