TU Darmstadt / ULB / TUbiblio

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

Laube, Bodo and Maksay, Gábor and Schemm, Rudolf and Betz, Heinrich (2002):
Modulation of glycine receptor function: a novel approach for therapeutic intervention at inhibitory synapses?
In: Trends in pharmacological sciences, pp. 519-27, 23, (11), ISSN 0165-6147, [Article]

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.

Item Type: Article
Erschienen: 2002
Creators: Laube, Bodo and Maksay, Gábor and Schemm, Rudolf and Betz, Heinrich
Title: Modulation of glycine receptor function: a novel approach for therapeutic intervention at inhibitory synapses?
Language: English
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.

Journal or Publication Title: Trends in pharmacological sciences
Volume: 23
Number: 11
Divisions: 10 Department of Biology
10 Department of Biology > Neurophysiology and Neurosensory Systems
?? fb10_zoologie ??
Date Deposited: 11 Apr 2011 09:48
Export:

Optionen (nur für Redakteure)

View Item View Item