DOV-102,677 is a psychoactive drug being developed by

Merck Merck refers primarily to the German Merck family and three companies founded by the family, including: * the Merck Group, a German chemical, pharmaceutical and life sciences company founded in 1668 ** Merck Serono (known as EMD Serono in the Unite ...

and is currently in

clinical trials Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar ...

. It is a

triple reuptake inhibitor Triple is used in several contexts to mean "threefold" or a "treble": Sports * Triple (baseball), a three-base hit * A basketball three-point field goal * A figure skating jump with three rotations * In bowling terms, three strikes in a row * In ...

(TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). It is the (−)-enantiomer of

DOV-216,303 DOV 216,303 is an experimental antidepressant drug originally developed by DOV Pharmaceutical and was licensed to Merck & Co. in 2004; Merck and DOV terminated their relationship in December 2006. It is a triple reuptake inhibitor (TRI), or ...

, and its (+)-enantiomer is DOV-21,947 (

amitifadine Amitifadine (developmental code names DOV-21,947, EB-1010) is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) or so-called triple reuptake inhibitor (TRI) which is or was being developed by Euthymics Bioscience It was under de ...

). Instead of being developed for depression, DOV-102,677 is being developed for the treatment of alcoholism. IC₅₀ values for the SERT, NET and DAT are 129 nM, 103 nM, and 133 nM. DOV stereochemistry

DOV-102,677 (20 mg/kg IP) increased extracellular levels of dopamine and serotonin in the prefrontal cortex to 320 and 280% above baseline 100 min after administration. Dopamine levels were stably increased for the duration (240 min) of the study, but serotonin levels declined to baseline by 200 min after administration. Norepinephrine levels increased linearly to a maximum of 348% at 240 min post-dosing.

References

Chloroarenes Cyclopropanes Serotonin–norepinephrine–dopamine reuptake inhibitors {{psychoactive-stub