依利色林
- CAS号:130579-75-8
- 英文名:Eplivanserin
- 中文名:依利色林
- CBNumber:CB51011732
- 分子式:C19H21FN2O2
- 分子量:328.38
- MOL File:130579-75-8.mol
- 沸点 :453.4±55.0 °C(Predicted)
- 密度 :1.08
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :9.60±0.15(Predicted)
依利色林性质、用途与生产工艺
- 生物活性 Eplivanserin 是一种有效的，选择性的，可口服的 5-HT2 receptor 拮抗剂，在大鼠皮层膜中，IC50 值为 5.8 nM，同时对 5-HT2 receptor 的 Kd 值为 1.14 nM。
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靶点
5-HT 2 Receptor
5.8 nM (IC 50 , in rat cortical membrane)
5-HT 2 Receptor
1.14 nM (Ki)
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体外研究
Eplivanserin is a potent, selective and orally available 5-HT 2 antagonist, with an IC 50 of 5.8 nM in rat cortical membrane, and a K d of 1.14 nM. Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, with IC 50 s 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 α 1 and α 2 , rat whole brain histammine H 1 , Na + channel, and rat striatum dopamine D 1 and D 2 , with IC 50 s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively.
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体内研究
Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT 2 receptor binding of [ 3 H]ketanserin with an ED 50 of 0.087 mg/kg after i.p. injection, and 0.097 mg/kg after p.o administration in mice.
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