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EGIS-12,233

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EGIS-12,233
Clinical data
ATC code
  • none
Identifiers
  • 5,7-dichloro-3-[4-[4-(4-chlorophenyl)piperazin-1-yl]butyl]-3-ethyl-indolin-2-one
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H28Cl3N3O
Molar mass480.86 g·mol−1
3D model (JSmol)
  • c3cc(Cl)ccc3N4CCN(CC4)CCCCC1(CC)c2cc(Cl)cc(Cl)c2NC1=O
  • InChI=1S/C24H28Cl3N3O/c1-2-24(20-15-18(26)16-21(27)22(20)28-23(24)31)9-3-4-10-29-11-13-30(14-12-29)19-7-5-17(25)6-8-19/h5-8,15-16H,2-4,9-14H2,1H3,(H,28,31)
  • Key:NOWFIMHNXPZVSK-UHFFFAOYSA-N
  (verify)

EGIS-12,233 is a drug with applications in scientific research, acting as a potent and selective antagonist for both the 5-HT6 and 5-HT7 serotonin receptor subtypes, with good selectivity over other receptors.[1] It has been shown to increase dopamine release in cochlear tissue, suggesting a role for the 5-HT6 and 5-HT7 receptors in regulation of the hearing system.[2]

References

[edit]
  1. ^ Volk B, Barkóczy J, Hegedus E, Udvari S, Gacsályi I, Mezei T, et al. (April 2008). "(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists". Journal of Medicinal Chemistry. 51 (8): 2522–32. doi:10.1021/jm070279v. PMID 18361484.
  2. ^ Doleviczényi Z, Vizi ES, Gacsályi I, Pallagi K, Volk B, Hársing LG, et al. (November 2008). "5-HT6/7 receptor antagonists facilitate dopamine release in the cochlea via a GABAergic disinhibitory mechanism". Neurochemical Research. 33 (11): 2364–72. doi:10.1007/s11064-008-9796-4. PMID 18663573. S2CID 11148455.
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