3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇
- CAS号:57477-39-1
- 英文名:BRL 54443
- 中文名:3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇
- CBNumber:CB2690838
- 分子式:C14H18N2O
- 分子量:230.31
- MOL File:Mol file
- 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 :solid
- 酸度系数(pKa) :10.08±0.40(Predicted)
- 颜色 :white
3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇性质、用途与生产工艺
- 简介 3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇即BRL-54443是一种对5-HT1E和5-HT1F血清素受体亚型起选择性激动作用的药物。其制备受到越来越多医药工作者的关注。
- 生物活性 BRL 54443 是 5-HT1E/1F 受体激动剂，Ki 分别为 1.1 nM 和 0.7 nM，比对其它 5-HT 和多巴胺受体的抑制性高 30 倍以上。
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靶点
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)
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体外研究
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).
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体内研究
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：2024/11/08
- 产品编号：HY-13221
- 产品名称：BRL 54443
- CAS编号：
- 包装：5 mg
- 价格：505元
- 更新日期：2024/11/08
- 产品编号：HY-13221
- 产品名称：3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇 BRL 54443
- CAS编号：57477-39-1
- 包装：10mM * 1mLin DMSO
- 价格：555元
- 公司名称：NACALAI
- 联系电话：--
- 电子邮件：info-tech@nacalai.co.jp
- 国家：日本
- 产品数：6046
- 优势度：75
