Modulation of glycine receptor function: A novel approach for therapeutic intervention at inhibitory synapses?

Bodo Laube, Gábor Maksay, Rudolf Schemm, Heinrich Betz

Research output: Contribution to journalReview article

197 Citations (Scopus)

Abstract

Transmitter-gated ion channels mediate rapid synaptic transmission in the CNS and constitute important targets for many neuroactive drugs. Inhibitory glycine receptors (GlyRs) are members of the nicotinic acetylcholine receptor superfamily and inhibit neuronal firing by opening Cl- channels following agonist binding. In this article, we discuss recent developments in GlyR pharmacology, delineate the receptor domains that are involved in binding of agonists and allosteric modulators, and present a molecular model of the extracellular architecture of the receptor. The recent discovery of compounds that act preferentially on specific GlyR isoforms and the differential expression of these isoforms in distinct regions of the developing and adult CNS show considerable promise towards the development of drugs that act in defined glycine-mediated pathways. In particular, compounds that can potentiate GlyR function should provide leads for novel muscle relaxants in addition to sedative and analgesic agents.

Original languageEnglish
Pages (from-to)519-527
Number of pages9
JournalTrends in Pharmacological Sciences
Volume23
Issue number11
DOIs
Publication statusPublished - Nov 1 2002

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ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

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