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Submit ReviewBRL 54443
说明： Potent 5-ht1E and 5-HT1F agonist
化学名： 5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole
生物活性 for BRL 54443
BRL 54443 is a potent 5-ht1E/1F receptor agonist (pEC50 values are 8.5 and 8.6 respectively). Displays > 30-fold selectivity over other 5-HT and dopamine receptors (pKi values are 8.7. 8.9, 7.2, 6.9, 7.2, 5.9, 7.0, 6.5, < 6, < 6, 6.3 and 6.2 for human 5-HT1E, 1F, 1A, 1B, 1D, 2A, 2B, 2C, 4, 7, D2 and D3 receptors respectively). Induces 5-HT2A receptor-mediated mouse aortic contraction in vitro (pEC50 = 6.52). Active in vivo.
技术数据 for BRL 54443
| 分子量 | 230.31 |
| 公式 | C14H18N2O |
| 储存 | Desiccate at +4°C |
| CAS Number | 57477-39-1 |
| PubChem ID | 2438 |
| InChI Key | WKNFADCGOAHBPG-UHFFFAOYSA-N |
| Smiles | CN1CCC(CC1)C1=CNC2=CC=C(O)C=C12 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for BRL 54443
参考文献 for BRL 54443
参考文献是支持产品生物活性的出版物。
McKune and Watt (2001) Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J.Pharmacol.Exp.Ther. 297 88 PMID: 11259531
Brown et al (1998) BRL 54443, a potent agonist with selectivity for human cloned 5-HT1E and 5-HT1F receptors. Br.J.Pharmacol. 123 233P
Lightowler et al (1998) Effect of BRL 54443 (3-(1-methylpiperidin-4-yl)-1H-indol-5-ol), a 5-HT1E/1F receptor agonist, on general behaviour and maximal electroshock seizure threshold in the rat. Br.J.Pharmacol. 123 237P
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关键词: BRL 54443, BRL 54443 supplier, Potent, 5-ht1E/F, agonists, Serotonin, 5-HT1F, Receptors, 5-HT1E, BRL54443, 5-ht1E, 1129, Tocris Bioscience
2 篇 BRL 54443 的引用文献
引用文献是使用了 Tocris 产品的出版物。 BRL 54443 的部分引用包括：
Müller et al (2009) 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One 4 e6453 PMID: 19649285
Klein et al (2011) Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. Br J Pharmacol 337 860 PMID: 21422162
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.