BRL 54443

Cat. No. 1129

BRL 54443 C14H18N2O [57477-39-1]

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Chemical Name: 5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole

Biological Activity

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.

Technical Data

M.Wt:
230.31
Formula:
C14H18N2O
Solubility:
Soluble to 50 mM in DMSO
Storage:
Desiccate at +4°C
CAS No:
57477-39-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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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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Citations are publications that use Tocris products. Selected citations for BRL 54443 include:

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.

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Keywords: BRL 54443, supplier, Potent, 5-ht1E/F, agonists, Serotonin, 5-HT1F, Receptors, 5-HT1E, BRL54443, Tocris Bioscience, 5-ht1E Receptor Agonist products

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