EMD-386088 explained

EMD-386088 is an indole derivative which is used in scientific research. It acts as a potent 5-HT₆ receptor partial agonist, with a K_i of 1 nM, a significantly higher affinity than older 5-HT₆ agonists such as EMDT, although it possesses moderate affinity for the 5-HT₃ receptor as well.^[1] Subsequent research has determined that EMD-386088 is also a dopamine reuptake inhibitor and that this action is involved in the antidepressant-like effects of the drug in rodents.^[2]

EMD-386088 can be further reacted with a butyrophenone sidechain.^[3]

See also

• EMDT
• ST-1936
• Tepirindole

Notes and References

1. Mattsson C, Sonesson C, Sandahl A, Greiner HE, Gassen M, Plaschke J, Leibrock J, Böttcher H . 6 . 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists . Bioorganic & Medicinal Chemistry Letters . 15 . 19 . 4230–4234 . October 2005 . 16055331 . 10.1016/j.bmcl.2005.06.067 .
2. Jastrzębska-Więsek M, Siwek A, Partyka A, Antkiewicz-Michaluk L, Michaluk J, Romańska I, Kołaczkowski M, Wesołowska A . 6 . Study of a mechanism responsible for potential antidepressant activity of EMD 386088, a 5-HT6 partial agonist in rats . Naunyn-Schmiedeberg's Archives of Pharmacology . 389 . 8 . 839–849 . August 2016 . 27106213 . 4939156 . 10.1007/s00210-016-1245-3 .
3. Genus Possanza, Kurt Freter, & Sven Luttke, (1976 to Boehringer Ingelheim GmbH).