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DOV-216,303

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Chemical compound
Pharmaceutical compound
DOV-216,303
Legal status
Legal status
Identifiers
  • 1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C11H11Cl2N
Molar mass 228.12 g·mol−1
3D model (JSmol)
  • C1C2C1(CNC2)C3=CC(=C(C=C3)Cl)Cl
  • 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
 NcheckY (what is this?)   (verify)

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]

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

[edit ]

References

[edit ]
  1. ^ McCoy M (August 12, 2004). "Merck and DOV Pharmaceutical In Drug Pact". Chemical & Engineering News.
  2. ^ a b "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. ^ a b 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年03月05日0. PMID 29578004. S2CID 5007186.
SSRIs Tooltip Selective serotonin reuptake inhibitors
SNRIs Tooltip Serotonin–norepinephrine reuptake inhibitors
NRIs Tooltip Norepinephrine reuptake inhibitors
NDRIs Tooltip Norepinephrine–dopamine reuptake inhibitors
NaSSAs Tooltip Noradrenergic and specific serotonergic antidepressants
SARIs Tooltip Serotonin antagonist and reuptake inhibitors
SMS Tooltip Serotonin modulator and stimulators
Others
TCAs Tooltip Tricyclic antidepressants
TeCAs Tooltip Tetracyclic antidepressants
Others
Non-selective
MAOA Tooltip Monoamine oxidase A-selective
MAOB Tooltip Monoamine oxidase B-selective
Miscellaneous
DAT Tooltip Dopamine transporter
(DRIs Tooltip Dopamine reuptake inhibitors)
NET Tooltip Norepinephrine transporter
(NRIs Tooltip Norepinephrine reuptake inhibitors)
SERT Tooltip Serotonin transporter
(SRIs Tooltip Serotonin reuptake inhibitors)
VMATs Tooltip Vesicular monoamine transporters
Others

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