[The molecular biology mechanism of action of benzodiazepine].
The central GABAA synapses contain specific benzodiazepine binding sites thought to modulate the receptor allosterically for the transmitter. The benzodiazepine receptor represents a modulating site which is located on the GABA-A receptor/chloride channel complex and mediates both positive and negative modulation of the chloride channel. The effects of the benzodiazepines lie in an increase in the receptor-coupled conductivity of chlorides. Different stressors induce changes in the benzodiazepine receptor complex regarding hypersensitivity. There are indications that these stress-induced changes are mediated by an endogenous peptide. The modulation on these receptors is of functional significance in stress-relevant behavioural reactions and in conflict situations. The research results have led to new concepts of the receptor function and of the effects of compounds which are the basis of potential pharmaceuticals. The neuro-pharmacology of the future promises new pharmaceutical targets on the mechanisms of the allosteric modulation of the receptor function.
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Klinik für Anästhesiologie und Intensivtherapie, Medizinische Fakultät (Charité), Humboldt-Universität zu Berlin.
D000818:Animals; D058787:GABA-A Receptor Antagonists; D006801:Humans; D051381:Rats; D011963:Receptors, GABA-A / Q000502:physiology*; D013312:Stress, Physiological / Q000503:physiopathology
D058787:GABA-A Receptor Antagonists; D011963:Receptors, GABA-A