Eplivanserin 是一种有效和特异性的 5-HT2A 受体拮抗剂，Kd 值为 1.14 nM，在大鼠皮质膜中 IC50 值为 5.8 nM。

Eplivanserin is an effective and selective antagonist of 5-HT2A receptor with a Kd of 1.14 nM and an IC50 value of 5.8 nM in rat cortical membrane.

Eplivanserin has inhibitory effects on rat cortex adrenergic α1 and α2, rat whole brain histammine H1, Na+ channel, and rat striatum dopamine D1 and D2, with IC50s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C with IC50s of 0.12 μM (Pig cortex 5-HT1C), 14 μM (Rat hippocampus 5-HT1A), and 16 μM (Rat stnatum 5-HT1B, Ox caudate nucleus 5-HT1D)[1].

In mice, Eplivanserin(0.097 mg/kg; i.p.) inhibits 5-HT2 receptor binding of [3H]ketanserin with an ED50 of 0.087 mg/kg[1]. In rats, SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment[2].

130579-75-8

C19H21FN2O2

328.38

依利色林;SR-46349;Eplivanserin

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years