DOV-216,303
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DOV 216,303 is an experimental
antidepressant Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathi ...
drug A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug i ...
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 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
racemic In chemistry, a racemic mixture or racemate () is a mixture that has equal amounts (50:50) of left- and right-handed enantiomers of a chiral molecule or salt. Racemic mixtures are rare in nature, but many compounds are produced industrially as r ...
mixture of
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 ...
(DOV-21,947) and its (–)-
enantiomer In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities whi ...
, DOV-102,677. Its IC50 values for SERT, NET, and DAT are Ki 14 nM, 20 nM, and 78 nM, respectively. As of March 2008, DOV had no intention to further develop DOV-216,303 because the patent on the compound had expired. In a
mouse model A model organism is a non-human species that is extensively studied to understand particular biological phenomena, with the expectation that discoveries made in the model organism will provide insight into the workings of other organisms. Mod ...
, DOV-216,303 has shown the ability to promote recovery after spinal cord
contusion A bruise, also known as a contusion, is a type of hematoma of tissue, the most common cause being capillaries damaged by trauma, causing localized bleeding that extravasates into the surrounding interstitial tissues. Most bruises occur clo ...
.


See also

* Bicifadine


References

{{Monoamine reuptake inhibitors Chloroarenes Serotonin–norepinephrine–dopamine reuptake inhibitors Abandoned drugs