Eplivanserin (SR-46349) hemifumarate 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 hemifumarate 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].

386.43

Solid

C₁₉H₂₁FN₂O₂.1/2C₄H₄O₄

130580-02-8

富马酸依利色林

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 25 mg/mL(64.69 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。