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Glossary of Pharmacology 

Inverse Agonist

Definition: 
An agonist that binds to the receptor and reduces its constitutive activity leading to a biological response that is opposite to the response elicited by a full or partial agonist. Constitutively active agonist receptors are responsible for a certain biological effect and binding of inverse agonist to the receptor abolishes the spontaneous receptor activity and therefore translates into a biological effect in the opposite direction. 

Example:

Olmesartan is an inverse agonist of the spontaneously active angiotensin II type 1 (AT1) receptor in the heart and blood vessels, and it inhibits such spontaneous activity leading to a reduction in blood pressure.

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