The Neurolixis R&D pipeline is based on novel compounds that activate serotonin 5-HT1A receptors in the brain: NLX-112, NLX-101 and NLX-204. These compounds are exceptionally selective and have been extensively tested in vitro and in vivo. A review just published in Pharmacology & Therapeutics provides a thorough overview of their differential properties, with particular focus on their preferential activity in models of motor disorders (for NLX-112), of cognition and respiratory dysfunction (for NLX-101) and of mood deficits (for NLX-204). The distinctive properties of the compounds arise from their 'biased agonism', which enables them to preferentially target specific brain regions associated with different 5-HT1A receptor functions. The phenomenon of biased agonism (also known as 'functional selectivity') is attracting increasing attention because it offers the possibility of developing safer and more efficacious treatments for brain diseases.
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Translating biased agonists from molecules to medications: Serotonin 5-HT1A receptor functional selectivity for CNS disorders
Pharmacology & Therapeutics. 2021 Jun 24:107937. doi: 10.1016/j.pharmthera.2021.107937. Online ahead of print. PMID: 34174274