inverse agonist
A drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
Full Definition
An inverse agonist is a type of receptor ligand that not only lacks the ability to activate a receptor but actually reduces the receptor's basal activity below its normal unstimulated level. This differs from a competitive antagonist, which simply blocks receptor activation without affecting basal activity. In psychopharmacology, some benzodiazepine receptor ligands can act as inverse agonists, producing anxiogenic and proconvulsant effects opposite to those of benzodiazepine agonists. Understanding inverse agonism is crucial for predicting drug interactions and side effects.
Usage
Usage note: Reserve for advanced pharmacological discussions; ensure clear distinction from antagonists.
In Context
- "Some benzodiazepine receptor ligands act as inverse agonists, producing anxiety rather than sedation." — Pharmacology textbook
- "The inverse agonist properties of certain compounds explain their paradoxical effects in clinical trials." — Drug development report