EMD-386088

EMD-386088
Clinical data
ATC code none
Identifiers
CAS Number 54635-62-0 YesY
PubChem (CID) 10131112
Chemical and physical data
Formula C14H14ClN2
Molar mass 245.727 g/mol
3D model (Jmol) Interactive image
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EMD-386088 is an indole derivative which is used in scientific research. It acts as a potent 5-HT6 receptor partial agonist, with a Ki 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]

See also

References

  1. Mattsson, C; Sonesson, C; Sandahl, A; Greiner, HE; Gassen, M; Plaschke, J; Leibrock, J; Böttcher, H (2005). "2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists". Bioorganic & Medicinal Chemistry Letters. 15 (19): 4230–4. doi:10.1016/j.bmcl.2005.06.067. PMID 16055331.
  2. Jastrzębska-Więsek M, Siwek A, Partyka A, Antkiewicz-Michaluk L, Michaluk J, Romańska I, Kołaczkowski M, Wesołowska A (2016). "Study of a mechanism responsible for potential antidepressant activity of EMD 386088, a 5-HT6 partial agonist in rats". Naunyn Schmiedebergs Arch. Pharmacol. 389: 839–49. doi:10.1007/s00210-016-1245-3. PMC 4939156Freely accessible. PMID 27106213.


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