Langues

8 February 2019 - Neurolixis and Jagiellonian University publish novel 'biased agonist' antidepressants

Neurolixis and scientists at Jagiellonian University (Krakow, Poland) have published results from a drug discovery program aiming to identify compounds with rapid and efficacious antidepressant activity. The novel serotonin 5-HT1A receptor 'biased agonists' (patent application WO/2017/220799) activate a cellular response associated with antidepressant activity (phosphorylation of ERK enzyme), rather than other signaling pathways. 

Adrian Newman-Tancredi (CSO of Neurolixis) commented: "Depression constitutes a major healthcare challenge because current antidepressants have multiple activities, are only partially efficacious and take weeks to work. We are excited to have identified highly-selective compounds targeting a signaling pathway associated with rapid antidepressant activity. This opens the way for development of a new generation of drugs offering improved and rapid therapy of depressive disorders.”

Novel aryloxyethyl derivatives of 1-(1-benzoylpiperidin-4-yl)methanamine as the Extracellular Regulated Kinases 1/2 (ERK1/2) phosphorylation-preferring serotonin 5‑HT1A receptor biased agonists with robust antidepressant-like activity.
Sniecikowska J, Głuch-Lutwin M, Bucki A, Więckowska A, Siwek A, Jastrzębska-Więsek M, Partyka A, Wilczyńska D, Pytka K, Pociecha K, Cios A, Wyska E, Wesołowska A, Pawłowski MH, Varney M, Newman-Tancredi A, Kołaczkowski M.
Journal Medicinal Chemistry 2019 Feb 5. doi: 10.1021/acs.jmedchem.9b00062. PMID: 30721053