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Benzodiazepine receptor ligands with positive and negative efficacy

1983; Elsevier BV; Volume: 22; Issue: 12 Linguagem: Inglês

10.1016/0028-3908(83)90113-2

1873-7064

C. Bræstrup, Mogens Brøndsted Nielsen, T. Honoré, Leif H. Jensen, Erling N. Petersen,

Analytical Chemistry and Chromatography

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.