Laube, Bodo ; Maksay, Gábor ; Schemm, Rudolf ; Betz, Heinrich (2002)
Modulation of glycine receptor function: a novel approach for therapeutic intervention at inhibitory synapses?
In: Trends in pharmacological sciences, 23 (11)
Artikel, Bibliographie
Kurzbeschreibung (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.
| Typ des Eintrags: | Artikel |
|---|---|
| Erschienen: | 2002 |
| Autor(en): | Laube, Bodo ; Maksay, Gábor ; Schemm, Rudolf ; Betz, Heinrich |
| Art des Eintrags: | Bibliographie |
| Titel: | Modulation of glycine receptor function: a novel approach for therapeutic intervention at inhibitory synapses? |
| Sprache: | Englisch |
| Publikationsjahr: | 2002 |
| Titel der Zeitschrift, Zeitung oder Schriftenreihe: | Trends in pharmacological sciences |
| Jahrgang/Volume einer Zeitschrift: | 23 |
| (Heft-)Nummer: | 11 |
| Kurzbeschreibung (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. |
| Fachbereich(e)/-gebiet(e): | 10 Fachbereich Biologie 10 Fachbereich Biologie > Neurophysiologie und neurosensorische Systeme ?? fb10_zoologie ?? |
| Hinterlegungsdatum: | 11 Apr 2011 09:48 |
| Letzte Änderung: | 05 Mär 2019 06:48 |
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