Seproxetine
 | |
| Clinical data | |
|---|---|
| ATC code |
|
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Elimination half-life | 4–16 days |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C16H16F3NO |
| Molar mass | 295.305 g·mol−1 |
Seproxetine, also known as (S)-norfluoxetine, is a selective serotonin reuptake inhibitor (SSRI).[1][2] It is the S enantiomer of norfluoxetine, the main active metabolite of the widely used antidepressant fluoxetine;[3] it is nearly 4 times more selective for stimulating neurosteroid synthesis relative to serotonin reuptake inhibition than fluoxetine.[4] It is formed through the demethylation, or removal of a methyl group, of norfluoxetine.[5] Seproxetine is both an inhibitor of serotonin and dopamine transporters, 5-HT2A and 5-HT2C receptors.[6] It was being investigated by Eli Lilly and Company as an antidepressant; however, it inhibited the KvLQT1 protein, which is responsible for the management of the QT interval. This is the time it takes for the heart to contract and recover. Due to the inhibition, the QT interval was prolonged, which could lead to significant cardiac side complications.[7] Due to this, development of the medication was discontinued.[1] Tests on its efficacy found that it was equivalent to fluoxetine, but sixteen times more powerful than the R enantiomer of norfluoxetine.[8]
References
- ^ a b "Seproxetine". DrugBank. University of Alberta. Archived from the original on 31 October 2020. Retrieved 10 August 2016.
- S2CID 25958396.
- ISSN 1355-5146.
- PMID 19157982.
- ^ Alvén Fimmerstad T (2022). Could fluorinated pharmaceuticals have an impact on the EOF amount in human blood? (degree of Bachelor thesis). Örebro University.
- S2CID 233773168.
- ^ "Seproxetine". Inxight Drugs. National Center for Advancing Translational Sciences (NCATS). Archived from the original on 20 April 2023. Retrieved 20 April 2023.
- .