Draft:CE-103
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 CE-103 | |
| Legal status | |
|---|---|
| Legal status |
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| Identifiers | |
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| Chemical and physical data | |
| Formula | C17H15NOS2 |
| Molar mass | 313.43 g·mol−1 |
| 3D model (JSmol) | |
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CE-103 is an analog of modafinil, a member of a series of structurally related heterocyclic derivatives.[1]
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.[2]
It is closely related to CE-123, being a positional isomer.
See also
[edit]References
[edit]- ↑ 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.
- ↑ Sase A, Aher YD, Saroja SR, Ganesan MK, Sase S, Holy M, Höger H, Bakulev V, Ecker GF, Langer T, Sitte HH, Leban J, Lubec G (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.