CAS 342652-67-9: 3-(1,1-Dimethylethyl)-7-(5-methyl-3-isoxazolyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazine

MRK 016 is an antidepressant drug that acts by potentiating the effect of serotonin and norepinephrine. It has been shown to be effective in treating depression in animals by increasing the production of growth factor and chloride, which are necessary for neuronal function. MRK 016 is a racemic mixture of two enantiomers, with the S-enantiomer being more potent than the R-enantiomer. MRK 016 binds to the benzodiazepine binding site on GABA receptors at nanomolar concentrations, but does not act as an antagonist or agonist. This drug also binds to alpha-1 adrenergic receptors with high affinity, inhibiting receptor activity and reducing anxiety. The pharmacokinetic properties of MRK 016 have been studied in both rats and wild-type mice. In rats, MRK 016 has a short plasma half-life and a low volume of distribution. In mice, this drug has a longer plasma half-life and higher volume of

MRK-016 is a selective GABAA α5 receptor inverse agonist/ negative allosteric modulator, orally available and penetrating the BBB. MRK-016 is antidepressant.