DOV-102,677
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| Clinical data | |
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| ATC code |
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| Identifiers | |
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| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C11H11Cl2N |
| Molar mass | 228.118 g/mol g·mol−1 |
| 3D model (JSmol) | |
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DOV 102,677 is a psychoactive drug being developed by Merck as an antidepressant and is currently in clinical trials.[1] It is a so-called triple (re)uptake inhibitor (TUI), 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 | ||||
|---|---|---|---|---|---|---|
| 5-HT | NE | DA | SERT | NET | DAT | |
| 216,303 | 14 | 20 | 78 | 190 | 380 | 190 |
| 21,947 | 12 | 23 | 96 | 100 | 260 | 210 |
| 102,677 | 130 | 100 | 130 | 740 | 1000 | 220 |
"DOV 102,677 (20 mg/kg IP) increased extracellular levels of DA and 5-HT in the prefrontal cortex to 320 and 280% above baseline 100 min after administration. DA levels were stably increased for the duration (240 min) of the study, but serotonin levels declined to baseline by 200 min after administration. NE levels increased linearly to a maximum of 348% at 240 min post-dosing."[1]
See also
- N.B. Milnacipran also uses epichlorohydrin and phenylacetonitrile in most of the syntheses for this compound.
References
- ^ a b c d Attention: This template ({{cite pmid}}) is deprecated. To cite the publication identified by PMID 16636898, please use {{cite journal}} with
|pmid=16636898instead. - ^ Attention: This template ({{cite pmid}}) is deprecated. To cite the publication identified by PMID 17908267, please use {{cite journal}} with
|pmid=17908267instead.
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