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BRL 54443

Catalog #: 1129
2 Citations Datasheet / COA / SDS

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1129 has been discontinued.
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BRL 54443 | CAS No. 57477-39-1 | 5-HT1E Receptor Agonists
1 Image
Description: Potent 5-ht1E and 5-HT1F agonist

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

Product Details
Citations (2)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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

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

Background References

  1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  2. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling.
    McKune and Watt
    J.Pharmacol.Exp.Ther., 2001;297:88
  3. BRL 54443, a potent agonist with selectivity for human cloned 5-HT1E and 5-HT1F receptors.
    Brown et al.
    Br.J.Pharmacol., 1998;123:233P
  4. 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.
    Lightowler et al.
    Br.J.Pharmacol., 1998;123:237P

Product Datasheets

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Citations for BRL 54443

The citations listed below are publications that use Tocris products. Selected citations for BRL 54443 include:

2 Citations: Showing 1 - 2

  1. Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships.
    Authors: Klein Et al.
    Br J Pharmacol  2011;337:860
  2. 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo.
    Authors: M&#252;ller Et al.
    PLoS One  2009;4:e6453

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