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MRK 016 is a gABAA receptor inverse agonist selective for the α5-subtype (EC50 = 3 nM). MRK 016 exhibits affinity at benzodiazepine binding site of recombinant human GABAA receptors (Ki values are 0.77 nM, 0.83 nM, 0.85 nM and 1.4 nM for α3-, α1-, α2-, and α5-containing respectively). MRK 016 increases long-term potentiation (LTP) in mouse hippocampal slices.
| Molecular Weight | 368.39 |
| Formula | C17H20N8O2 |
| CAS Number | 342652-67-9 |
| Solubility (25°C) | DMSO 36.84 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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