3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇
| 中文名称 | 3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇 |
|---|---|
| 中文同义词 | 3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇;3-(1-甲基哌啶-4-基)-1H-吲哚-5-醇;化合物BRL54443;BRL-54443,5-HT 1E和5-HT 1F受体激动剂 |
| 英文名称 | BRL 54443 |
| 英文同义词 | BRL 54443;5-HYDROXY-3-(1-METHYLPIPERIDIN-4-YL)-1H-INDOLE;3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol;3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol BRL 54443;3-(1-methylpiperidin-4-yl)-1H-indol-5-ol;1H-Indol-5-ol, 3-(1-Methyl-4-piperidinyl)-;BRL 54443 HCl;BRL-54443;BRL54443 |
| CAS号 | 57477-39-1 |
| 分子式 | C14H18N2O |
| 分子量 | 230.31 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;抑制剂;神经信号;小分子抑制剂，天然产物;Inhibitors |
| Mol文件 | Mol File |
| 结构式 |  |
3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇 性质
| 沸点 | 431.5±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.196 |
| 储存条件 | Inert atmosphere,2-8°C |
| 溶解度 | H2O:50 mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 10.08±0.40(Predicted) |
| 颜色 | 白色 |
|
5-HT 1E Receptor 1.1 nM (Ki) |
5-HT 1F Receptor 0.7 nM (Ki) |
5-HT 1A Receptor 63 nM (Ki) |
5-HT 1B Receptor 126 nM (Ki) |
5-HT 1D Receptor 63 nM (Ki) |
5-HT 2A Receptor 1259 nM (Ki) |
5-HT 2B Receptor 100 nM (Ki) |
5-HT 2C Receptor 316 nM (Ki) |
5-HT 6 Receptor >10,000 nM (Ki) |
5-HT 7 Receptor >10,000 nM (Ki) |
Despite its low affinity for other receptors [5-HT
1A
(63 nM), 5-HT
1B
(126 nM), 5-HT
1D
(63 nM), 5-HT
2A
(1259 nM), 5-HT
2B
(100 nM), 5-HT
2C
(316 nM), 5-HT
6
(>10,000 nM), 5-HT
7
(>10,000 nM), D
2
(501 nM), D
3
(631 nM), and α
1B
-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT
1F
receptors.
In DG membranes, BRL54443 selectively stimulates 5-HT
1E
receptors and potently inhibits forskolin-dependent cAMP production (IC
50
=14 nM). BRL 54443 also induces contraction (-log EC
50
=6.52).
Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-13221 | BRL 54443 | 5 mg | 505元 | |
| 2024/11/08 | HY-13221 | 3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇 BRL 54443 | 57477-39-1 | 10mM * 1mLin DMSO | 555元 |