Catalog Number: 1129
Chemical Name: 5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole
Biological Activity
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. All Tocris products are intended for laboratory research use only.
Background References
  1. 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
  2. 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
Citations:

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

2 Citations: Showing 1 - 2
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  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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