Drug intelligence / Profile preview

SB-206553

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

SB-206553 is a small molecule research compound originally developed by GlaxoSmithKline (GSK). It functions as a potent and selective mixed antagonist and inverse agonist at the serotonin 5-HT2B and 5-HT2C receptors. Specifically, it shows high affinity for the human 5-HT2C receptor and rat 5-HT2B receptor, with significant selectivity over other 5-HT receptor subtypes. Additionally, SB-206553 acts as a positive allosteric modulator of the alpha-7 nicotinic acetylcholine receptor (α7 nAChR). Preclinical research has explored its potential in treating anxiety disorders and psychostimulant addiction, particularly methamphetamine-seeking behavior, as well as its role in modulating pulmonary vascular resistance. It is currently utilized primarily as a pharmacological tool in laboratory settings and is not an approved therapeutic.

Other names
5-methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole
02

Targets

HTR2C (5-hydroxytryptamine 2C receptor)CHRNA7 (α7 nicotinic receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)

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