依利色林
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- CAS号:
- 130579-75-8
- 英文名:
- Eplivanserin
- 英文别名:
- EPLIVANSERIN;VAIOZOCLKVMIMN-PRJWTAEASA-N;(Z,E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime;2-Propen-1-one, 1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-, O-[2-(dimethylamino)ethyl]oxime, (1Z,2E)-;5-hydroxytryptamine Receptor,Serotonin Receptor,5-HT2A,5-HT Receptor,Eplivanserin,SR46349,oral,dopamine,SR 46349,Inhibitor,inhibit,release
- 中文名:
- 依利色林
- 中文别名:
- 依利色林;化合物 T11217;(Z,E)-1-(2-氟苯基)-3-(4-羟基苯基)-2-丙烯-1-酮 O-[2-(二甲基氨基)乙基]肟
- CBNumber:
- CB51011732
- 分子式:
- C19H21FN2O2
- 分子量:
- 328.38
- MOL File:
- 130579-75-8.mol
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依利色林化学性质
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沸点:
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453.4±55.0 °C(Predicted)
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密度:
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1.08
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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9.60±0.15(Predicted)
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依利色林性质、用途与生产工艺
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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5-HT
2
Receptor
5.8 nM (IC
50
, in rat cortical membrane)
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5-HT
2
Receptor
1.14 nM (Ki)
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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.
依利色林
上下游产品信息
上游原料
下游产品
130579-75-8, 依利色林 相关搜索:
- 化合物 T11217
- 依利色林
- (Z,E)-1-(2-氟苯基)-3-(4-羟基苯基)-2-丙烯-1-酮 O-[2-(二甲基氨基)乙基]肟
- 130579-75-8
- 2-Propen-1-one, 1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-, O-[2-(dimethylamino)ethyl]oxime, (1Z,2E)-
- 5-hydroxytryptamine Receptor,Serotonin Receptor,5-HT2A,5-HT Receptor,Eplivanserin,SR46349,oral,dopamine,SR 46349,Inhibitor,inhibit,release
- VAIOZOCLKVMIMN-PRJWTAEASA-N
- (Z,E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime
- EPLIVANSERIN