130579-75-8
130579-75-8 結(jié)構(gòu)式
基本信息
(Z,E)-1-(2-氟苯基)-3-(4-羥基苯基)-2-丙烯-1-酮 O-[2-(二甲基氨基)乙基]肟
VAIOZOCLKVMIMN-PRJWTAEASA-N
(Z,E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
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5-HT 2 Receptor 5.8 nM (IC 50 , in rat cortical membrane) |
5-HT 2 Receptor 1.14 nM (Ki) |
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.
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.