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

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

Beyond the preview

Go deeper on BRL54443.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on BRL54443.

Gosset Free

Get started with Gosset.

Enter your corporate email.

Work email preferred.

Book a call