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
| Solubility | Soluble 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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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:
Keywords: BRL 54443, supplier, Potent, 5-ht1E/F, agonists, Serotonin, 5-HT1F, Receptors, 5-HT1E, BRL54443, 5-ht1E, Receptors, 5-ht1E, Receptors, Tocris Bioscience
