Allosteric modulation and direct activation of glycine receptors by a tricyclic sulfonamide

Allosteric modulation and direct activation of glycine receptors by a tricyclic sulfonamide

Abstract Ionotropic glycine receptors (GlyRs) are chloride-permeable ligand-gated ion channels expressed in the nervous system. Alterations to glycinergic inhibition and the generation of dysfunctional GlyRs have been linked to chronic pain, a widely prevalent disease. Positive allosteric modulators...

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Main Authors: César O. Lara, Carlos F. Burgos, Katherine Fariña-Oliva, Ana M. Marileo, Victoria P. San Martín, David Flaig, Paul Soto-Ortega, Omayra V. Contreras, Anggelo Sazo, Krishna Gaete-Riquelme, Jeremías Corradi, Carola Muñoz-Montesino, Jorge Fuentealba, Patricio A. Castro, Luis G. Aguayo, Cecilia Bouzat, Gustavo Moraga-Cid, Gonzalo E. Yévenes
Format: Article
Language:English
Published: Nature Portfolio 2025-02-01
Series:Scientific Reports
Subjects:
Glycine receptors
Allosteric modulation
Electrophysiology
Molecular modelling
Pharmacology
Chronic pain
Online Access:https://doi.org/10.1038/s41598-025-90209-7
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https://doi.org/10.1038/s41598-025-90209-7

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