MRK-016 (Cat.No:I008016) 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.
| Catalog Number | I008016 |
| CAS Number | 783331-24-8 |
| Synonyms | MRK-016; MRK 016; MRK016.;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 |
| Molecular Formula | C17H20N8O2 |
| Purity | 95% |
| Target | GABA Receptor |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at +4C |
| IUPAC Name | 3-[3-tert-butyl-2-[(2-methyl-1,2,4-triazol-3-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazin-7-yl]-5-methyl-1,2-oxazole |
| 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 |
| InChIKey | QYSYOGCIDRANAR-UHFFFAOYSA-N |
| SMILES | CC1=CC(=NO1)C2=NN=CC3=C(C(=NN32)OCC4=NC=NN4C)C(C)(C)C |
| Reference | </br>1:Administration of the inverse benzodiazepine agonist MRK-016 rescues acquisition and memory consolidation following peripheral administration of bacterial endotoxin. Eimerbrink MJ, White JD, Pendry RJ, Hodges SL, Sadler LN, Wiles JD, Weintraub MK, Chumley MJ, Boehm GW.Behav Brain Res. 2015 Jul 15;288:50-3. doi: 10.1016/j.bbr.2015.03.048. Epub 2015 Mar 28. PMID: 25823763 </br>2: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. Atack JR, Maubach KA, Wafford KA, O/’Connor D, Rodrigues AD, Evans DC, Tattersall FD, Chambers MS, MacLeod AM, Eng WS, Ryan C, Hostetler E, Sanabria SM, Gibson RE, Krause S, Burns HD, Hargreaves RJ, Agrawal NG, McKernan RM, Murphy MG, Gingrich K, Dawson GR, Musson DG, Petty KJ.J Pharmacol Exp Ther. 2009 Nov;331(2):470-84. doi: 10.1124/jpet.109.157636. Epub 2009 Aug 24. PMID: 19704033 Free Article |
