Eplivanserin hemifumarate
Chemical Name: (1Z,2E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime hemifumarate
Purity: ≥98%
Biological Activity
Eplivanserin hemifumarate is a potent and selective 5-HT2A antagonist (IC50 values are 5.8 and 120 and >100 nM for 5-HT2A, 5-HT2B and 5-HT2C, respectively). Attenuates cocaine-induced hyperactivity. Increases dopamine (DA) release in rat medial prefrontal cortex (mPFC); potentiates haloperidol-induced DA release in the mPFC and nucleus accumbens.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo.
Yadav et al.
J.Pharmacol.Exp.Ther., 2011;339:99 -
Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses.
Filip et al.
J.Pharmacol.Exp.Ther., 2004;310:1246 -
SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced DA release in rat medial prefrontal cortex and nucleus accumbens.
Bonaccorso et al.
Neuropsychopharmacology., 2002;27:430
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