BRL 54443

Key Product Details

Product Description

BRL 54443 is a potent 5-ht_1E/1F receptor agonist (pEC₅₀ values are 8.5 and 8.6 respectively). Displays > 30-fold selectivity over other 5-HT and dopamine receptors (pK_i 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-HT_1E, _1F, _1A, _1B, _1D, _2A, _2B, _2C, ₄, ₇, D₂ and D₃ receptors respectively). Induces 5-HT_2A receptor-mediated mouse aortic contraction in vitro (pEC₅₀ = 6.52). Active in vivo.

Product Specifications for BRL 54443

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

Solubility

Preparing Stock Solutions for BRL 54443

The following data is based on the product molecular weight 230.31.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	8.68 mL	43.42 mL	86.84 mL
2.5 mM	1.74 mL	8.68 mL	17.37 mL
5 mM	0.87 mL	4.34 mL	8.68 mL
25 mM	0.17 mL	0.87 mL	1.74 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 25 publications citing the usage of this product.

• Brown BRL 54443, a potent agonist with selectivity for human cloned 5-HT_1E and 5-HT_1F receptors. Br.J.Pharmacol.
• Lightowler Effect of BRL 54443 (3-(1-methylpiperidin-4-yl)-1H-indol-5-ol), a 5-HT_1E/1F receptor agonist, on general behaviour and maximal electroshock seizure threshold in the rat. Br.J.Pharmacol.
• McKune and Watt Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J.Pharmacol.Exp.Ther. 2001 PMID: 11259531

Product Documents for BRL 54443