BRL 54443

Discontinued Product

BRL 54443 (Cat. No. 1129) has been withdrawn from sale for commercial reasons.
Description: Potent 5-ht1E and 5-HT1F agonist
Chemical Name: 5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole
Citations (2)
Literature (1)

Biological Activity 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.

Technical Data for BRL 54443

M. Wt 230.31
Formula C14H18N2O
Storage Desiccate at +4°C
CAS Number 57477-39-1
PubChem ID 2438
Smiles CN1CCC(CC1)C1=CNC2=CC=C(O)C=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets for BRL 54443

Certificate of Analysis / Product Datasheet
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References for BRL 54443

References are publications that support the biological activity of the product.

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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Keywords: BRL 54443, BRL 54443 supplier, Potent, 5-ht1E/F, agonists, Serotonin, 5-HT1F, Receptors, 5-HT1E, BRL54443, 5-ht1E, 1129, Tocris Bioscience

2 Citations for BRL 54443

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

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

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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

5-HT Receptors Scientific Review

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.