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 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.
D000161:Acoustic Stimulation; D000818:Animals; D002243:Carbolines / Q000378:metabolism; D002712:Chlorides / Q000378:metabolism; D006801:Humans; D008024:Ligands; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000378:metabolism; D011963:Receptors, GABA-A; D012640:Seizures / Q000378:metabolism; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D002243:Carbolines; D002712:Chlorides; D008024:Ligands; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; C034818:methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate; D005680:gamma-Aminobutyric Acid; C024915:beta-carboline-3-carboxylic acid ethyl ester