MRK-016 is a selective inverse agonist of the GABA α5 receptor. In vivo studies indicate that MRK-016 improves performance in hippocampal-dependent memory tasks and protects against LPS-induced learning and memory deficits in mice without causing seizures or anxiogenic effects at tested doses. Despite its promising cognitive-enhancing properties and favorable safety profile in young males, MRK-016’s development was halted due to poor tolerability in elderly subjects and variable human pharmacokinetics.
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| Other Names | MRK 016, MRK016 |
|---|---|
| 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 |
| CAS | 342652-67-9 |
| Molecular Weight | 368.4 |
| Molecular Formula | C17H20N8O2 |
| SMILES | CC1=CC(=NO1)C2=NN=CC3=C(C(=NN32)OCC4=NC=NN4C)C(C)(C)C |