product name BRL-54443
Description: BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. In studies using rat brain cortical membranes, BRL-54443 causes biphasic inhibition of total [3H]-5-HT. In C57BL/6J mouse aortae, BRL 54443 leads to a contraction in the presence of Ketanserin (an antagonist of 5-HT2A and 5-HT2C receptors).
References: Eur J Pharmacol. 2004 May 25;492(2-3):259-67; J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.
230.31
Formula
C14H18N2O
CAS No.
57477-39-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 46 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (8.7 mM)
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: BRL 54443 has also measurable affinity for the 5-HT2A receptor. BRL 54443 induces contraction with a −logEC50 of 6.52. Contraction caused by BRL 54443 is likely mediated through stimulation of 5-HT5-HT2A receptors. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. |
| Animal model | Adult male cats |
| Formulation & Dosage | Dissolved in distilled water containing 1 equivalent 2,3-dihydroxybutanedioic acid+0.9% NaCl; 3 μg/kg-30 mg/kg; s.c.injection |
| References | Eur J Pharmacol. 2004 May 25;492(2-3):259-67; J Pharmacol Exp Ther. 2001 Apr;297(1):88-95. |
