The sticky issue of neurosteroids and GABAA receptors

Research output: Contribution to journalArticle

71 Scopus citations

Abstract

Endogenous neurosteroids and their synthetic analogs (neuroactive steroids) are potent modulators of GABAA receptors. Thus, they are of physiological and clinical relevance for their ability to modulate inhibitory function in the CNS. Despite their importance, fundamental issues of neurosteroid actions remain unresolved. Recent evidence suggests that glutamatergic principal neurons, rather than glia, are the major sources of neurosteroid synthesis. Other recent studies have identified putative neurosteroid binding sites on GABAA receptors. In this Opinion, we argue that neurosteroids require a membranous route of access to transmembrane-domain binding sites within GABAA receptors. This has implications for the design of future neuroactive steroids because the lipid solubility and related accessibility properties of the ligand are likely to be key determinants of receptor modulation.

Original languageEnglish
Pages (from-to)299-306
Number of pages8
JournalTrends in Neurosciences
Volume33
Issue number7
DOIs
StatePublished - Jul 1 2010

Fingerprint Dive into the research topics of 'The sticky issue of neurosteroids and GABA<sub>A</sub> receptors'. Together they form a unique fingerprint.

  • Cite this