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Systematic (IUPAC) name | |
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1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
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Identifiers | |
ATC code | None |
PubChem | CID: 9795276 |
Chemical data | |
Formula | C11H11Cl2N |
Molecular mass | 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.
Compound | Uptake 5-HT | Uptake NE | Uptake DA | Binding SERT | Binding NET | Binding DAT |
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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 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
References
- ^ a b Mitchell, S. (2006-03-04). "SSRIs face next-generation replacement". United Press International.
- ^ 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.