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| Formula | C11H11Cl2N |
| Molar mass | 228.12 g·mol−1 |
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DOV-102,677 is apsychoactive drug beingdeveloped byMerck and is currently inclinical trials.[1] It is atriple reuptake inhibitor (TRI), orserotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).[1] It is the (−)-enantiomer ofDOV-216,303, and its (+)-enantiomer is DOV-21,947 (amitifadine).
Instead of being developed fordepression, DOV-102,677 is being developed for the treatment ofalcoholism.[2]
IC50 values for theSERT,NET andDAT are 129 nM, 103 nM, and 133 nM.[1]
| Compound | Uptake | Binding | ||||
|---|---|---|---|---|---|---|
| 5-HT | NE | DA | SERT | NET | 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 |
DOV-102,677 (20 mg/kg IP) increasedextracellular levels ofdopamine andserotonin in theprefrontal cortex to 320% and 280% above baseline 100 min after administration. Dopamine levels were stably increased for the duration (240 min) of the study, but serotonin levels declined to baseline by 200 min after administration.Norepinephrine levels increased linearly to a maximum of 348% at 240 min post-dosing.[1]
