Benzodiazepine receptor ligands with positive and negative efficacy

Recent studies have shown that benzodiazepine receptors can be affected not only by benzodiazepine agonists and antagonists but also by a new class of ligands which produce effects opposite to those of benzodiazepines, that is they produce convulsions and anxiety. These ligands can be described as h...

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Veröffentlicht in:Neuropharmacology 1983-12, Vol.22 (12), p.1451-1457
Hauptverfasser: Braestrup, C., Nielsen, M., Honoré, T., Jensen, L.H., Petersen, E.N.
Format: Artikel
Sprache:eng
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Zusammenfassung:Recent studies have shown that benzodiazepine receptors can be affected not only by benzodiazepine agonists and antagonists but also by a new class of ligands which produce effects opposite to those of benzodiazepines, that is they produce convulsions and anxiety. These ligands can be described as having a negative efficacy at the receptor; tentatively they are named “inverse agonists”. Pharmacological experiments indicate that agonists, antagonists and inverse agonists comprise a whole continuum of agents with a graduated variety of efficacy at the receptor. Biochemical studies, supported by published electrophysiological data, indicate that the benzodiazepine receptor allosterically up- or down-regulates the gain in the GABAergic system depending on the nature of the ligand.
ISSN:0028-3908
1873-7064
DOI:10.1016/0028-3908(83)90113-2