Eplivanserin (SR-46349) is a potent, selective and orally active5-HT_2Areceptorantagonist, with anIC₅₀of 5.8 nM in rat cortical membrane, and aK_dof 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for5-HT_2Athan 5-HT_2Band 5-HT_2C^[1][2].

Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, with IC₅₀s of 0.12 μM (Pig cortex 5-HT_1C), 14 μM (Rat hippocampus 5-HT_1A), and 16 μM (Rat stnatum 5-HT_1B, Ox caudate nucleus 5-HT_1D). Eplivanserin also has inhibitory effects on rat cortex adrenergic α₁and α₂, rat whole brain histammine H₁, Na⁺channel, and rat striatum dopamine D₁and D₂, with IC₅₀s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively^[1].

Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT₂receptor binding of [³H]ketanserin with an ED₅₀of 0.087 mg/kg after i.p. injection, and 0.097 mg/kg after p.o administration in mice^[1].
SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment in rats^[2].

328.38

C₁₉H₂₁FN₂O₂

130579-75-8

依利色林

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