DOV-216,303

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DOV-216,303
DOV-216,303.svg
Legal status
Legal status
  • Investigational New Medicine
Identifiers
CAS Number 410074-75-8
PubChem (CID) 9795276
ChemSpider 7971043
ChEMBL CHEMBL528995
Chemical and physical data
Formula C11H11Cl2N
Molar mass 228.117 g/mol
3D model (Jmol) Interactive image
  (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
  • Doses of up to 100 mg 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[edit]

References[edit]

  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. doi:10.1111/j.1527-3458.2006.00123.x. PMID 16958986.