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    BRL-54443
    BRL-54443

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0999
    CAS #: 57477-39-1Purity ≥98%

    Description: BRL 54443 (BRL54443; BRL-54443) is a potent agonist of 5-HT1E and 5-HT1F receptor with important biological activity. It inhibits 5-HT1E and 5-HT1F with pKi values of 8.7 and 9.25, respectively.

    References: Eur J Pharmacol. 2004 May 25;492(2-3):259-67; J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.

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    Molecular Weight (MW)230.31 
    FormulaC14H18N2O 
    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 
    SynonymsBRL 54443; BRL54443; BRL-54443


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    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.

    In VivoBRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. 
    Animal modelAdult male cats 
    Formulation & DosageDissolved 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. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    BRL-54443
    Top, comparison of contraction elicited by 5-HT, 5-CT, α-methyl-5-HT, 5-HT2 receptor agonist DOI, BRL 54443, and nonselective 5-HT receptor agonist 5-methoxytryptamine. Bottom, comparison of contraction elicited by 5-HT, 2-methyl-5-hydroxytryptamine maleate, sumatriptan, PAPP, dipropyl-5CT, BW 723C86, and 8-OH-DPAT.  J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.
     
    BRL-54443
    Effect of 5-HT2A receptor antagonist ketanserin on BRL 54443-induced contraction in the C57BL/6J aortae. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95. 


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