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
Molecular mass	228.117 g/mol
SMILES C3C2CNCC23c(cc1Cl)ccc1Cl
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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. It is a so-called triple reuptake inhibitor (TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). 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 K_i 14 nM, 20 nM, and 78 nM, respectively. All DOV compounds are being developed in collaboration with Merck.

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

• Bicifadine