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Neurosteroids as selective inhibitors of glycine receptor activity

18 April 2020
Neurosteroids as selective inhibitors of glycine receptor activity

Eva Kudová from IOCB Prague collaborates with Julia V. Bukanova from the Research Center of Neurology in Moscow on research targetting the ability of neurosteroids to influence the functional activity of inhibitory glycine and γ-aminobutyric acid receptors (GlyRs and GABAARs). 

Disturbance of functional activity of GlyRs and GABAARs underlies many neurological disorders (e.g. pain, epilepsy). Interestingly, four neurosteroids – testosterone, epitestosterone, dihydroandrostenedione, and etiocholanedione – did not modulate GABA-induced chloride currents, while strongly inhibiting glycine-induced chloride currents. 

Such selective modulation is rare and novel among the known neurosteroids and offers new avenues of investigation in the field of drug-like selective modulators for potential neuropharmacological applications.

Read the paper:

  • Bukanova, J. V.; Solntseva, E. I.; Kudova, E. Neurosteroids as Selective Inhibitors of Glycine Receptor Activity: Structure-Activity Relationship Study on Endogenous Androstanes and Androstenes. Frontiers in Molecular Neuroscience 2020, 13, 44. https://doi.org/10.3389/fnmol.2020.00044
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