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Open Access Articles- Top Results for DOV-216,303

DOV-216,303

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DOV-216,303
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Systematic (IUPAC) name
1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
Clinical data
Identifiers
None
PubChem CID 9795276
Chemical data
Formula C11H11Cl2N
228.117 g/mol
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DOV 216,303 is an antidepressant drug originally developed by DOV Pharmaceutical and now licensed to the larger pharmaceutical company Merck & Co., which is currently in clinical trials.[1] It is a so-called triple reuptake inhibitor (TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).[1][2] It is the racemic mixture of amitifadine (DOV 21,947) and its (–)-enantiomer. Its IC50 values for SERT, NET, and DAT are Ki 14 nM, 20 nM, and 78 nM, respectively.[2] It is closely related to DOV 102,677 and amitifadine, both of which are also being developed in collaboration with Merck.

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Compound Uptake 5-HT Uptake NE Uptake DA Binding SERT Binding NET Binding DAT
DOV 216,303 14 20 78 190 380 190
DOV 21,947 12 23 96 100 260 210
DOV 102,677 130 100 130 740 1000 220
  • Doses of up to 100mg per day are well tolerated with only nausea, and GI disturbances reported as side effects.
  • This compound does not cause notable shifts in LMA, and is not psychostimulant.

The effects are not long-lasting.

More recently (see attachment), it appears that the DOV compound may also be useful at increasing weight loss.

  • DOV causes a decrease in circulating triglycerides.
  • The reason for weightloss is not going to be thermogenic or psychostimulant, or chronic decrease appetite. Read article for details.

See also

References

  1. ^ a b Mitchell, S. (2006-03-04). "SSRIs face next-generation replacement". United Press International. 
  2. ^ 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): 123–134. PMID 16958986. doi:10.1111/j.1527-3458.2006.00123.x. 



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