In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects - when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present.
Some currently common drugs that have been classed as partial agonists at particular receptors include: buspirone, aripiprazole, buprenorphine, and norclozapine.
Famous quotes containing the word partial:
“Both the man of science and the man of art live always at the edge of mystery, surrounded by it. Both, as a measure of their creation, have always had to do with the harmonization of what is new with what is familiar, with the balance between novelty and synthesis, with the struggle to make partial order in total chaos.... This cannot be an easy life.”
—J. Robert Oppenheimer (1904–1967)