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Eplivanserin: Wikis

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Eplivanserin
Systematic (IUPAC) name
(Z,E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime
Identifiers
CAS number 130579-75-8
130580-02-8 (fumarate)
ATC code none
PubChem 5493160
Chemical data
Formula C 19H21FN2O2  
Mol. mass 328.381 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

Eplivanserin (expected trade name Ciltyri) is an experimental drug for the treatment of insomnia, developed by Sanofi Aventis. As of March 2008, it is undergoing Phase III clinical trials.

Mechanism of action

Eplivanserin is an inverse agonist on the serotonin receptor subtype 5-HT2A. In contrast to older sedating drugs acting on 5-HT2A receptors (e. g. haloperidol, clozapine, risperidone), eplivanserin has practically no affinity to dopamine, histamine and adrenergic receptors.[1]

Study results

In a placebo controlled Phase II clinical trial with 351 subjects, eplivanserin reduced the sleep latency by 39 minutes (versus 26 minutes under placebo).[1]

References

  1. ^ a b Teergarden, BR; Al Shamma, H, Xiong, Y (2008). "5-HT2A Inverse-Agonists for the Treatment of Insomnia". Current Topics in Medicinal Chemistry 8 (11): 969–976. doi:10.2174/156802608784936700.  
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