DOV-216,303

DOV 216,303 is an experimental antidepressant drug originally developed by DOV Pharmaceutical and was licensed to Merck & Co. in 2004;[1] Merck and DOV terminated their relationship in December 2006.[2]: 12 [3]

DOV-216,303
Legal status
Legal status
Identifiers
IUPAC name
  • 1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC11H11Cl2N
Molar mass228.12 g·mol−1
3D model (JSmol)
SMILES
  • C1C2C1(CNC2)C3=CC(=C(C=C3)Cl)Cl
InChI
  • InChI=1S/C11H11Cl2N/c12-9-2-1-7(3-10(9)13)11-4-8(11)5-14-6-11/h1-3,8,14H,4-6H2 N
  • Key:BSMNRYCSBFHEMQ-UHFFFAOYSA-N N
 NY (what is this?)  (verify)

It is a triple reuptake inhibitor (TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).[4] It is the racemic mixture of amitifadine (DOV-21,947) and its (–)-enantiomer, DOV-102,677. Its IC50 values for SERT, NET, and DAT are Ki 14 nM, 20 nM, and 78 nM, respectively.[4]

As of March 2008, DOV had no intention to further develop DOV-216,303 because the patent on the compound had expired.[2]: 6 

In a mouse model, DOV-216,303 has shown the ability to promote recovery after spinal cord contusion.[5]

See also

References
  1. McCoy M (August 12, 2004). "Merck and DOV Pharmaceutical In Drug Pact". Chemical & Engineering News.
  2. "10-K For the fiscal year ended December 31, 2007". Dov Pharmaceutical via SEC Edgar. March 31, 2008. DOV 216,303 was originally in development for depression; however as the patented composition of matter claim has expired, there are no ongoing clinical trials of DOV 216,303 and none are planned.
  3. "DOV 216303". Adis Insight. Springer Nature Switzerland AG. Retrieved 26 February 2017.
  4. Skolnick P, Krieter P, Tizzano J, Basile A, Popik P, Czobor P, Lippa A (2006). "Preclinical and clinical pharmacology of DOV 216,303, a "triple" reuptake inhibitor". CNS Drug Reviews. 12 (2): 123–34. doi:10.1111/j.1527-3458.2006.00123.x. PMC 6494125. PMID 16958986.
  5. Chu TH, Cummins K, Stys PK (May 2018). "The triple monoamine re-uptake inhibitor DOV 216,303 promotes functional recovery after spinal cord contusion injury in mice". Neuroscience Letters. 675: 1–6. doi:10.1016/j.neulet.2018.03.050. PMID 29578004. S2CID 5007186.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.