BRL 54443

• CAT Number: I004143
• CAS Number: 57477-39-1
• Molecular Formula: C14H18N2O
• Molecular Weight: 230.31
• Purity: ≥95%
• Synonyms: 3-(1-methylpiperidin-4-yl)-1H-indol-5-ol
• Target: Neuronal Signaling
• Solubility: DMSO: ≥ 51 mg/mL
• Storage: 2-8°C
• IC50: 8.7(pKi, 5-HT1E); 8.9 (pKi, 5-HT1F)
• InChI: InChI=1S/C14H18N2O/c1-16-6-4-10(5-7-16)13-9-15-14-3-2-11(17)8-12(13)14/h2-3,8-10,15,17H,4-7H2,1H3
• InChIKey: WKNFADCGOAHBPG-UHFFFAOYSA-N
• SMILES: CN1CCC(CC1)C2=CNC3=C2C=C(C=C3)O

BRL 54443（Cat No.:I004143） is a potent agonist of the 5-HT1E and 5-HT1F receptors, with pKi values of 8.7 and 8.9, respectively. It exhibits high selectivity for these receptors, with more than 30-fold selectivity over other 5-HT (serotonin) and dopamine receptors. The activation of 5-HT1E and 5-HT1F receptors can have various effects, including the modulation of neurotransmitter release and the regulation of vascular tone. BRL 54443’s selectivity profile makes it a valuable tool for studying the specific functions of the 5-HT1E and 5-HT1F receptors in biological systems.

Reference

[1]. 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.
[2]. 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.
[3]. 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.