BRL 54443

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Cat.No. 1129 - BRL 54443 | C14H18N2O | CAS No. 57477-39-1
Description: Potent 5-ht1E/F agonist
Chemical Name: 5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole
Datasheet
Citations (2)
Reviews
Literature

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
Storage Desiccate at +4°C
CAS Number 57477-39-1
PubChem ID 2438
InChI Key WKNFADCGOAHBPG-UHFFFAOYSA-N
Smiles CN1CCC(CC1)C1=CNC2=CC=C(O)C=C12

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.

Solubility Data

SolubilitySoluble to 50 mM in DMSO

Preparing Stock Solutions

The following data is based on the product molecular weight 230.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.34 mL 21.71 mL 43.42 mL
5 mM 0.87 mL 4.34 mL 8.68 mL
10 mM 0.43 mL 2.17 mL 4.34 mL
50 mM 0.09 mL 0.43 mL 0.87 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:

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 PMID:


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Keywords: BRL 54443, supplier, Potent, 5-ht1E/F, agonists, Serotonin, 5-HT1F, Receptors, 5-HT1E, BRL54443, 5-ht1E, Receptors, 5-ht1E, Receptors, 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


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Literature in this Area

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5-HT Receptors

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.