1-(1-甲基-1H-吲哚-5-基)-3-(吡啶-3-基)脲
| 中文名称 | 1-(1-甲基-1H-吲哚-5-基)-3-(吡啶-3-基)脲 |
|---|---|
| 中文同义词 | 1-(1-甲基-1H-吲哚-5-基)-3-(吡啶-3-基)脲;化合物SB-200646 |
| 英文名称 | SB 200646 HYDROCHLORIDE |
| 英文同义词 | SB 200646;SB 200646 HYDROCHLORIDE;N-(1-METHYL-1H-5-INDOLYL)-N'-(3-PYRIDINYL)UREA HYDROCHLORIDE;N-(1-METHYL-1H-INDOL-5-YL)-N'-3-PYRIDINYLUREA HYDROCHLORIDE;SB200646HCl;N-(1-methyl-5-indolyl)-N'-(3-pyridyl)urea;N-(1-Methyl-1H-indol-5-yl)-N'-3-pyridinylurea;1-(1-Methyl-1H-indol-5-yl)-3-pyridin-3-yl-urea |
| CAS号 | 143797-63-1 |
| 分子式 | C15H14N4O |
| 分子量 | 266.3 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 143797-63-1.mol |
| 结构式 |  |
1-(1-甲基-1H-吲哚-5-基)-3-(吡啶-3-基)脲 性质
| 储存条件 | 2-8°C |
|---|---|
| 溶解度 | DMSO：可溶26 mg/mL， |
| 形态 | 固体 |
| 颜色 | 淡黄色低 |
| 水溶解性 | Water: 1 mg/mL (NaN mM) |
SB 200646 (SB 200646A) 是一种强效的、选择性的 5-HT2B/2C 口服活性拮抗剂，比对5-HT2A受体的选择性高出50倍。SB 200646 对大鼠 5-HT2C 受体、大鼠 5-HT2B 受体和大鼠 5-HT2A 受体的pKi值分别为6.9、7.5和5.2。SB 200646 在体内具有电生理作用和抗焦虑的特性。
| Target | Value |
|
5-HT2B (rat)
(Cell-free assay) | 7.5(pKi) |
|
5-HT2C (Rat)
(Cell-free assay) | 6.9(pKi) |
|
5-HT2A (rat)
(Cell-free assay) | 5.2(pKi) |
SB-200646A (4 μM) abolishes the ethanol-induced increase in miniature inhibitory postsynaptic current (mIPSC) frequency and had no effect on basal mIPSC frequency.
SB-200646A (20 mg/kg; intravenous injection; daily; for 21 days; male albino Sprague-Dawley rats) treatment significantly decreases the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons.
The i.v. administration of 4-16 mg/kg of SB-200646A significantly increases the firing rate and % events as bursts in spontaneously active VTA dopaminergic neurons and significantly increases the % events as burst in substantia nigra pars compacta (SNC) dopaminergic neurons.
| Animal Model: | Male albino Sprague-Dawley rats (200-225 g at the beginning of treatment and 300-350 g at the time of the experiment) |
| Dosage: | 20 mg/kg |
| Administration: | Intravenous injection; daily; for 21 days |
| Result: | Significantly decreased the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons. |
| 提供商 | 语言 |
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英文
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | S2649 | 1-(1-甲基-1H-吲哚-5-基)-3-(吡啶-3-基)脲 SB 200646 | 143797-63-1 | 5mg | 2246.13元 |
| 2024/04/30 | S2649 | 1-(1-甲基-1H-吲哚-5-基)-3-(吡啶-3-基)脲 SB 200646 | 143797-63-1 | 25mg | 7366.54元 |