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.
|Storage||Desiccate at +4°C|
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.
|Solubility||Soluble to 50 mM in DMSO|
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
If you know of a relevant reference for BRL 54443, please let us know.
View Related Products by Product Action
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:
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
Do you know of a great paper that uses BRL 54443 from Tocris? Please let us know.
Reviews for BRL 54443
There are currently no reviews for this product. Be the first to review BRL 54443 and earn rewards!
Have you used BRL 54443?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.