A ligand that binds to allosteric site of the receptor and induces conformational changes that alter the efficacy and/or affinity of the agonists bound to the orthosteric site of the receptor. They can either enhance (positive allosteric modulator) or reduce (negative allosteric modulator) the efficacy and/or affinity of the orthosteric agonists. Silent/neutral allosteric modulator can bind to the allosteric site and prevents the binding of other allosteric ligands without triggering any changes in the affinity or efficacy of the orthosteric agonists.
Benzodiazepines are positive allosteric modulators of the inhibitory neurotransmitterγ-aminobutyric acid (GABA) receptors type A in the CNS and therefore are used for management of anxiety and seizures.
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