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DOV-102,677

Chemical compound

DOV-102,677

Chemical compound

| elimination_half-life =

DOV-102,677 is a psychoactive drug being developed by Merck and is currently in clinical trials. It is a triple reuptake inhibitor (TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). It is the (−)-enantiomer of DOV-216,303, and its (+)-enantiomer is DOV-21,947 (amitifadine).

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 stereochemistry
CompoundUptakeBinding5-HTNEDASERTNETDAT
DOV-216,303142078190380190
Amitifadine122396100260210
DOV-102,6771301001307401000220

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

References

  1. (2006). "Pharmacological profile of the "triple" monoamine neurotransmitter uptake inhibitor, DOV 102,677". Cellular and Molecular Neurobiology.
  2. (November 2007). "Effect of DOV 102,677 on the volitional consumption of ethanol by Myers' high ethanol-preferring rat". Alcoholism: Clinical and Experimental Research.
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chloroarenes cyclopropanes serotonin–norepinephrine–dopamine-reuptake-inhibitors
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