Chemistry:DOV-102,677
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| Formula | C11H11Cl2N |
| Molar mass | 228.12 g·mol−1 |
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DOV-102,677 is a psychoactive drug being developed by Merck and is currently in clinical trials.[1] It is a triple reuptake inhibitor (TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).[1] It is the (−)-enantiomer of DOV-216,303, and its (+)-enantiomer is DOV-21,947 (amitifadine).
Instead of being developed for depression, DOV-102,677 is being developed for the treatment of alcoholism.[2]
IC50 values for the SERT, NET and DAT are 129 nM, 103 nM, and 133 nM.[1]
| Compound | Uptake | Binding | ||||
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| 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) increased extracellular levels of dopamine and serotonin in the prefrontal 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]
References
- ↑ 1.0 1.1 1.2 1.3 "Pharmacological profile of the "triple" monoamine neurotransmitter uptake inhibitor, DOV 102,677". Cellular and Molecular Neurobiology 26 (4–6): 857–73. 2006. doi:10.1007/s10571-006-9012-5. PMID 16636898.
- ↑ "Effect of DOV 102,677 on the volitional consumption of ethanol by Myers' high ethanol-preferring rat". Alcoholism: Clinical and Experimental Research 31 (11): 1866–71. November 2007. doi:10.1111/j.1530-0277.2007.00513.x. PMID 17908267.
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