BRL 54443 maleate 

BRL 54443 (MALEATE) is a potent 5-HT_1E/1F receptor agonist (K_i values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors^[1].

Despite its low affinity for other receptors [5-HT_1A (63 nM), 5-HT_1B (126 nM), 5-HT_1D (63 nM), 5-HT_2A (1259 nM), 5-HT_2B (100 nM), 5-HT_2C (316 nM), 5-HT₆ (>10,000 nM), 5-HT₇ (>10,000 nM), D₂ (501 nM), D₃ (631 nM), and α_1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT_1F receptors^[1].
In DG membranes, BRL54443 selectively stimulates 5-HT_1E receptors and potently inhibits forskolin-dependent cAMP production (IC₅₀=14 nM). BRL 54443 (MALEATE) (MALEATE) also induces contraction (-log EC₅₀=6.52)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

346.38

C₁₈H₂₂N₂O₅

1197333-54-2

OC1=CC2=C(NC=C2C3CCN(C)CC3)C=C1.O=C(O)/C=C\C(O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Klein MT, et al. Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther. 2011 Jun;337(3):860-867.  [Content Brief]

  [2]. McKune CM, et al. 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.  [Content Brief]

  [3]. Klein MT, et al. Distribution of 5-ht(1E) receptors in the mammalian brain and cerebral vasculature: an immunohistochemical and pharmacological study. Br J Pharmacol. 2012 Jun;166(4):1290-302.  [Content Brief]

  [4]. Granados-Soto V, et al. The role of peripheral 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F serotonergic receptors in the reduction of nociception in rats. Neuroscience. 2010 Jan 20;165(2):561-8.  [Content Brief]