BRL 54443 (maleate)

BRL 54443 (MALEATE) is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively) ; displays > 30-fold selectivity over other 5-HT and dopamine receptors[1].

Product Specifications

CAS Number

[1197333-54-2]

UNSPSC

12352005

Hazard Statement

H315-H319-H335

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/brl-54443-maleate.html

Smiles

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

Molecular Formula

C18H22N2O5

Molecular Weight

346.38

Precautions

P261-P264-P271-P280-P302+P352-P304+P340-P362+P364-P405-P501

References & Citations

[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.|[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.|[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.|[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.