CE-103

CE-103
CE-103
Legal status
Legal status
Identifiers
  • 2-(benzhydrylsulfinylmethyl)-1,3-thiazole
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC17H15NOS2
Molar mass313.43 g·mol−1
3D model (JSmol)
  • O=S(CC1=NC=CS1)C(C2=CC=CC=C2)C3=CC=CC=C3
  • InChI=InChI=1S/C17H15NOS2/c19-21(13-16-18-11-12-20-16)17(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-12,17H,13H2
  • Key:MMCRZMXHSNGINW-UHFFFAOYSA-N

CE-103 is an analog of modafinil, a member of a series of structurally related heterocyclic derivatives.

CE-103 inhibits dopamine reuptake with an IC50 of 14.73 μM, an IC50 of 420.1 μM at the norepinephrine transporter (NET), while its effect on serotonin transporter (SERT) is negligible, therefore it is a modestly selective dopamine reuptake inhibitor. Sprague Dawley rats given CE-103 at doses 1 and 10 mg/kg showed an increased working memory index in a radial arm maze. Administration of the compound also decreased levels of complexes containing phosphorylated dopamine transporter (pDAT) and D1 receptor, while significantly increasing levels of complexes containing D2 receptor and D3 receptor.

It is closely related to CE-123, being a positional isomer.

See also

References

  1. ↑ Kalaba P, Ilić M, Aher NY, Dragačević V, Wieder M, Zehl M, et al. (January 2020). "Structure-Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters". Journal of Medicinal Chemistry. 63 (1): 391–417. doi:10.1021/acs.jmedchem.9b01938. PMID 31841637.
  2. ↑ Sase A, Aher YD, Saroja SR, Ganesan MK, Sase S, Holy M, et al. (March 2016). "A heterocyclic compound CE-103 inhibits dopamine reuptake and modulates dopamine transporter and dopamine D1-D3 containing receptor complexes". Neuropharmacology. 102: 186–196. doi:10.1016/j.neuropharm.2015.07.039. PMID 26407764.