BRL 54443 Chemical Properties

Boiling point:

431.5±45.0 °C(Predicted)

Density 

1.196

storage temp. 

Inert atmosphere,2-8°C

solubility 

H₂O: 50 mg/mL

form 

solid

pka

10.08±0.40(Predicted)

color 

white

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36

WGK Germany 

3

BRL 54443 Usage And Synthesis

Uses

BRL-53443 is a potent 5-HT and dopamine receptor agonist. Neuroresearch product.

Definition

ChEBI: 3-(1-methyl-4-piperidinyl)-1H-indol-5-ol is a member of hydroxyindoles.

Biological Activity

A potent 5-ht 1E/1F receptor agonist (pEC 50 values are 8.5 and 8.6 respectively). Displays > 30-fold selectivity over other 5-HT and dopamine receptors (pK i 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-HT 1E , 1F , 1A , 1B , 1D , 2A , 2B , 2C , 4 , 7 , D 2 and D 3 receptors respectively). Induces 5-HT 2A receptor-mediated mouse aortic contraction in vitro (pEC 50 = 6.52). Active in vivo .

storage

+4°C (desiccate)

References

1. a.m. brown, k. avenell, t j. young et al. brl 54443, a potent agonist with selectivity for human cloned 5-ht1e and 5-ht1f receptors. 1998. br.j.pharmacol. 123 233p.2. s. lightowler, t. stean, n. upton et al. 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. 1998. br.j.pharmacol. 123 237p.3. mckune cm, watts sw. characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. j pharmacol exp ther. 2001 apr;297(1):88-95.4. janssen p, tack j, sifrim d et al. influence of 5-ht1 receptor agonists on feline stomach relaxation. eur j pharmacol. 2004 may 25;492(2-3):259-67.

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