Allosteric Potentiating Ligand

Definition

Allosteric antagonists or agonists produce unique effects by binding to a site on the receptor to produce a bias in the receptor conformation. Allosteric modulators of nicotinergic receptors are compounds that interact with the receptor via binding sites that are distinct from those for acetylcholine and nicotinic agonists and antagonists. Consequently, modulators are not directly involved in the neurotransmission process they affect and hence usually do not induce compensatory processes, as direct agonists and antagonists may do (e.g., receptor desensitization, downregulation of expression).