Partial agonist

[1] 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.

[2] Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine.

Examples of ligands activating peroxisome proliferator-activated receptor gamma as partial agonists are honokiol and falcarindiol.

[3][4] Delta 9-tetrahydrocannabivarin (THCV) is a partial agonist at CB2 receptors and this activity might be implicated in ∆9-THCV-mediated anti-inflammatory effects.

[5] Additionally, Delta-9-Tetrahydrocannabinol (THC) is a partial agonist at both the CB1 and CB2 receptors, with the former being responsible for its psychoactive effects.

Relationship between percentage activity and concentration of full agonists and partial agonists