LUSAPERIDONE
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- CAS号:
- 214548-46-6
- 英文名:
- LUSAPERIDONE
- 英文别名:
- R107474;LUSAPERIDONE;Lusaperidone [inn];4H-Pyrido[1,2-a]pyrimidin-4-one, 3-[2-(3,4-dihydrobenzofuro[3,2-c]pyridin-2(1H)-yl)ethyl]-2-methyl-;2-Methyl-3-[2-(1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridin-2-yl)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one
- 中文名:
- LUSAPERIDONE
- 中文别名:
- 芦沙哌酮;化合物 T11894
- CBNumber:
- CB42451309
- 分子式:
- C22H21N3O2
- 分子量:
- 359.42
- MOL File:
- 214548-46-6.mol
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LUSAPERIDONE化学性质
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沸点:
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538.3±60.0 °C(Predicted)
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密度:
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1.31±0.1 g/cm3(Predicted)
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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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6.93±0.20(Predicted)
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LUSAPERIDONE性质、用途与生产工艺
Lusaperidone (R107474) 是一种α2肾上腺素受体 (adrenergic receptor) 拮抗剂,对α2A和α2C的 Ki 值分别为0.13和0.15 nM。
Ki: 0.13 nM (α2A adrenergic receptor), 0.15 nM (α2C adrenergic receptor)
Lusaperidone has subnanomolar affinity for α2A and α2C adrenergic receptor (K
i
=0.13 and 0.15 nM, respectively) and shows nanomolar affinity for the hα2B adrenergic receptor and h5-HT7 receptors (K
i
=1 and 5 nM, respectively). Lusaperidone interacts weakly (K
i
values ranging between 81 and 920 nM) with dopamine-hD2L, -hD3 and -hD4, h5-HT1D-, h5-HT1F-, h5-HT2A-, h5-HT2C-, and h5-HT5A receptors. Lusaperidone, tested up to 10 μM, interacts only at micromolar concentrations or not at all with any of the other receptor or transporter binding sites tested in this study. Lusaperidone has been shown to reverse the clonidine-induced inhibition of cyclic AMP production mediated by human α2A and α2C adrenoceptors expressed in cell lines (K
b
is 2.8 and 4.4 nM, respectively) and is a full antagonist on both receptor subtypes.
Lusaperidone occupies the α2A and α2C adrenergic receptor with an ED
50
of 0.014 mg/kg sc (0.009-0.019) and 0.026 mg/kg sc (0.022-0.030), respectively. The uptake of R107474 after
in vivo
intravenous administration is very rapid; in most tissues (including the brain) it reaches maximum concentration at 5 min after tracer injection.
LUSAPERIDONE
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-U00117 | Lusaperidone | | 1 mg | 1818元 |
2024/04/30 | HY-U00117 | LUSAPERIDONE Lusaperidone | 214548-46-6 | 5mg | 4000元 |
214548-46-6, LUSAPERIDONE 相关搜索:
- 芦沙哌酮
- 化合物 T11894
- 214548-46-6
- 4H-Pyrido[1,2-a]pyrimidin-4-one, 3-[2-(3,4-dihydrobenzofuro[3,2-c]pyridin-2(1H)-yl)ethyl]-2-methyl-
- R107474
- 2-Methyl-3-[2-(1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridin-2-yl)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one
- Lusaperidone [inn]
- LUSAPERIDONE