DOV-102,677 is a

psychoactive drug A psychoactive drug, psychopharmaceutical, mind-altering drug, consciousness-altering drug, psychoactive substance, or psychotropic substance is a chemical substance that alters psychological functioning by modulating central nervous system acti ...

being developed by Merck and is currently in

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

. 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 * ...

(TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). It is the (−)-enantiomer of DOV-216,303, 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 ...

). Instead of being developed for depression, DOV-102,677 is being developed for the treatment of

alcoholism Alcoholism is the continued drinking of alcohol despite it causing problems. Some definitions require evidence of dependence and withdrawal. Problematic use of alcohol has been mentioned in the earliest historical records. The World He ...

. IC₅₀ values for the SERT,

NET NET may refer to: Broadcast media United States * National Educational Television, the predecessor of the Public Broadcasting Service (PBS) in the United States * National Empowerment Television, a politically conservative cable TV network ...

and DAT are 129 nM, 103 nM, and 133 nM. DOV stereochemistry

DOV-102,677 (20 mg/kg IP) increased

extracellular This glossary of biology terms is a list of definitions of fundamental terms and concepts used in biology, the study of life and of living organisms. It is intended as introductory material for novices; for more specific and technical definitions ...

levels of

dopamine Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic chemical of the catecholamine and phenethylamine families. It is an amine synthesized ...

and

serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

in the

prefrontal cortex In mammalian brain anatomy, the prefrontal cortex (PFC) covers the front part of the frontal lobe of the cerebral cortex. It is the association cortex in the frontal lobe. The PFC contains the Brodmann areas BA8, BA9, BA10, BA11, BA12, ...

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 Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic compound, organic chemical in the catecholamine family that functions in the brain and human body, body as a hormone, neurotransmitter and neuromodulator. The ...

levels increased linearly to a maximum of 348% at 240 min post-dosing.

References

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