Inhibitory Actions of Tropeines on the α3 Glycine Receptor Function.

ABSTRACT: Glycine receptors (GlyRs) are chloride-permeable pentameric ligand-gated ion channels. The inhibitory activity of GlyRs is essential for many physiological processes, such as motor control and respiration. In addition, several pathological states, such as hyperekplexia, epilepsy, and chronic pain, are associated with abnormal glycinergic inhibition. Recent studies have pointed out that positive allosteric modulators targeting the GlyR α3 subunit (α3GlyR) displayed beneficial effects in chronic pain models. Interestingly, previous electrophysiological studies have shown that tropeines, which are a family of synthetic antagonists of the serotonin type 3 receptors (5-HT₃Rs), potentiate the activity of GlyRs conformed by α1 subunits. However, despite its importance as a pharmacologi

SUBMITTER: San Martin VP 

PROVIDER: S-EPMC6465966 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature