Full agonists, partial agonists and inverse agonists

An agonist is a ligand that binds to a receptor and alters the receptor state resulting in a biological response. A full agonist reaches the maximal response capability of the system, and a partial agonist does not (even at full receptor occupancy). A partial agonist acts as an antagonist in the presence of a full agonist (if they compete for the same receptors). An inverse agonist is a ligand that by binding to receptors reduces the fraction of them in an active conformation. Spare receptors are said to exist wherever a full agonist can cause a maximum response when occupying only a fraction of the total receptor population.

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Agonists, partial agonists

E.g., Phenylephrine Is Full Agonist at Alpha-Adrenoceptors. E.g., Aripipraxole Is Partial Antagonist at Selected Dopamine Receptors, PDF, Receptor Antagonist

Agonist, Partial Agonist, Antagonist and Inverse Agonist: Difference Explained

Cii: To define and explain dose-effect relationships of drugs, including dose-response curves – Jenny's Jam Jar