CE-125

CE-125
CE-125
Legal status
Legal status
Identifiers
  • 4-((benzhydrylsulfinyl)methyl)-2-cyclopropylthiazole
PubChem CID
Chemical and physical data
FormulaC20H19NOS2
Molar mass353.50 g·mol−1
3D model (JSmol)
  • O=S(CC1=CSC(C2CC2)=N1)C(C3=CC=CC=C3)C4=CC=CC=C4
  • InChI=1S/C20H19NOS2/c22-24(14-18-13-23-20(21-18)17-11-12-17)19(15-7-3-1-4-8-15)16-9-5-2-6-10-16/h1-10,13,17,19H,11-12,14H2
  • Key:USSBQUDPPUTTQY-UHFFFAOYSA-N

CE-125 is an analog of modafinil, a member of a series of structurally related heterocyclic derivatives.

CE-125 is a selective dopamine reuptake inhibitor, with IC50 of the monoamine transporters being 4.1 ± 0.8 μM at the dopamine transporter (DAT), 687.2 ± 152.8 μM at the norepinephrine transporter (NET), and 436.1 ± 129 μM at the serotonin transporter (SERT). Rats given CE-125 at doses 1 and 10 mg/kg increased the working memory index in a radial arm maze. The compound also altered dopaminergic signaling in rat frontal cortex. D1 receptor protein levels were significantly reduced in trained and treated animals, while D2 receptor levels remained unchanged.

CE-125 and related compounds are studied as potential treatment of motivational disorders and Alzheimer's disease.

See also

References

  1. 1 2 Shaikh A, Ahmad F, Teoh SL, Kumar J, Yahaya MF (2023). "Targeting dopamine transporter to ameliorate cognitive deficits in Alzheimer's disease". Frontiers in Cellular Neuroscience. 17 1292858. doi:10.3389/fncel.2023.1292858. PMC 10679733. PMID 38026688.
  2. ↑ Kalaba P, Ilić M, Aher NY, Dragačević V, Wieder M, Zehl M, Wackerlig J, Beyl S, Sartori SB, Ebner K, Roller A, Lukic N, Beryozkina T, Gonzalez ER, Neill P, Khan JA, Bakulev V, Leban JJ, Hering S, Pifl C, Singewald N, Lubec J, Urban E, Sitte HH, Langer T, Lubec G (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.
  3. ↑ Hussein AM, Aher YD, Kalaba P, Aher NY, Dragačević V, Radoman B, Ilić M, Leban J, Beryozkina T, Ahmed AB, Urban E, Langer T, Lubec G (August 2017). "A novel heterocyclic compound improves working memory in the radial arm maze and modulates the dopamine receptor D1R in frontal cortex of the Sprague-Dawley rat". Behavioural Brain Research. 332: 308–315. doi:10.1016/j.bbr.2017.06.023. PMID 28629964.