Date published: 2026-1-24

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BRL 54443 (CAS 57477-39-1)

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Alternate Names:
5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole; 3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol
Application:
BRL 54443 is a potent agonist at SR-1E and SR-1F
CAS Number:
57477-39-1
Purity:
≥98%
Molecular Weight:
230.31
Molecular Formula:
C14H18N2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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BRL 54443 is a potent 5-HT1E/1F receptor agonist (pEC50 values are 8.5 and 8.6 respectively). Induces 5-HT2A receptor-mediated mouse aortic contraction in vitro (pEC50 = 6.52). 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-HT1E1F, 1A, 1B, 1D, 2A, 2B, 2C, 4, 7, D2 and D3 receptors respectively).


BRL 54443 (CAS 57477-39-1) References

  1. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling.  |  McKune, CM. and Watts, SW. 2001. J Pharmacol Exp Ther. 297: 88-95. PMID: 11259531
  2. Serotonin-induced contraction in mesenteric resistance arteries: signaling and changes in deoxycorticosterone acetate-salt hypertension.  |  Watts, SW. 2002. Hypertension. 39: 825-9. PMID: 11897772
  3. 5-Hydroxytryptamine modulates cytokine and chemokine production in LPS-primed human monocytes via stimulation of different 5-HTR subtypes.  |  Dürk, T., et al. 2005. Int Immunol. 17: 599-606. PMID: 15802305
  4. Non-invasive optical biosensor for assaying endogenous G protein-coupled receptors in adherent cells.  |  Fang, Y., et al. 2007. J Pharmacol Toxicol Methods. 55: 314-22. PMID: 17207642
  5. Overview on 5-HT receptors and their role in physiology and pathology of the central nervous system.  |  Filip, M. and Bader, M. 2009. Pharmacol Rep. 61: 761-77. PMID: 19903999
  6. 5-Hydroxytryptamine induces cyclooxygenase-2 in rat vascular smooth muscle cells: Mechanisms involving Src, PKC and MAPK activation [corrected].  |  Machida, T., et al. 2011. Eur J Pharmacol. 656: 19-26. PMID: 21262218
  7. Serotonergic Modulation as Effective Treatment for Dravet Syndrome in a Zebrafish Mutant Model.  |  Sourbron, J., et al. 2016. ACS Chem Neurosci. 7: 588-98. PMID: 26822114
  8. 5-HT modulates the rat mesenteric vasopressor outflow by 5-HT1D sympatholytic receptors.  |  García-Pedraza, JÁ., et al. 2017. Clin Exp Pharmacol Physiol. 44: 1224-1231. PMID: 28771848
  9. Structural insights into the lipid and ligand regulation of serotonin receptors.  |  Xu, P., et al. 2021. Nature. 592: 469-473. PMID: 33762731
  10. Structure of serotonin receptors: molecular underpinning of receptor activation and modulation.  |  Zweckstetter, M., et al. 2021. Signal Transduct Target Ther. 6: 243. PMID: 34145221
  11. Molecular Cloning and Functional Characterization of Three 5-HT Receptor Genes (HTR1B, HTR1E, and HTR1F) in Chickens.  |  Sun, C., et al. 2021. Genes (Basel). 12: PMID: 34207786

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

BRL 54443, 10 mg

sc-203855
10 mg
$118.00

BRL 54443, 50 mg

sc-203855A
50 mg
$465.00