Drug intelligence / Profile preview

BRL54443

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Not Clinically Used; In Research, Typically Administered Intraperitoneally, Orally, Or Intravenously In Animal Studies
01

Overview

BRL54443 is a **synthetic small molecule** of the piperidinylindole class that acts as a **potent and selective agonist** at the serotonin **5-HT1E and 5-HT1F receptors**. It exhibits over 30-fold selectivity for these receptors compared to other 5-HT and dopamine receptor subtypes. In preclinical studies, BRL54443 has been shown to hyperpolarize neurons by increasing steady-state, depolarization-activated potassium currents, potentially involving voltage-gated potassium channels. It is primarily used as a research tool and is not approved for medical use. Its effects have been studied in behavioral and electrophysiological assays in animal models, including reduced locomotor activity in rats and dose-dependent actions on gastrointestinal function in cats[1][3][4][8].

Other names
3-(1-methylpiperidin-4-yl)-1H-indol-5-ol5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole
02

Targets

HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)HTR2A (Serotonin receptor 5-HT2A)HTR1E (5-hydroxytryptamine receptor 1E)HTR2C (5-hydroxytryptamine 2C receptor)HTR1F (Serotonin 5-HT1F receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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