DOV-216,303

DOV-216,303
Systematic (IUPAC) name
1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
Clinical data
Legal status
  • Investigational New Medicine
Identifiers
PubChem CID 9795276
Chemical data
Formula C11H11Cl2N
Molar mass 228.117 g/mol
  (verify)

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, DOV-102,677. Its IC50 values for SERT, NET, and DAT are Ki 14 nM, 20 nM, and 78 nM, respectively.[2] All DOV compounds are being developed in collaboration with Merck.

DOV stereochemistry
DOV stereochemistry
Compound Uptake 5-HT Uptake NE Uptake DA Binding SERT Binding NET Binding DAT
DOV-216,303 14 20 78 190 380 190
Amitifadine 12 23 96 100 260 210
DOV-102,677 130 100 130 740 1000 220

The effects are not long-lasting.

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

See also

References

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