Chemistry:EMD-386088

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Short description: Chemical compound
EMD-386088
EMD-386088.svg
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC14H14ClN2
Molar mass245.73 g·mol−1
3D model (JSmol)
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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]

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

See also

References

  1. "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. doi:10.1016/j.bmcl.2005.06.067. PMID 16055331. 
  2. "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. doi:10.1007/s00210-016-1245-3. PMID 27106213. 
  3. Genus Possanza, Kurt Freter, & Sven Luttke, U.S. Patent 3,980,658 (1976 to Boehringer Ingelheim GmbH).