Partial agonist

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Agonists

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.[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, and norclozapine. Examples of ligands activating peroxisome proliferator-activated receptor gamma as partial agonists are honokiol and falcarindiol.[3][4]

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References[edit]

  1. ^ Calvey, Norman; Williams, Norton (2009). "Partial agonists". Principles and Practice of Pharmacology for Anaesthetists. p. 62. ISBN 978-1-4051-9484-6. 
  2. ^ Zhu, Bao Ting (2005). "Mechanistic explanation for the unique pharmacologic properties of receptor partial agonists". Biomedicine & Pharmacotherapy 59 (3): 76–89. doi:10.1016/j.biopha.2005.01.010. PMID 15795100. 
  3. ^ Atanasov, Atanas G.; Wang, Jian N.; Gu, Shi P.; Bu, Jing; Kramer, Matthias P.; Baumgartner, Lisa; Fakhrudin, Nanang; Ladurner, Angela; Malainer, Clemens; Vuorinen, Anna; Noha, Stefan M.; Schwaiger, Stefan; Rollinger, Judith M.; Schuster, Daniela; Stuppner, Hermann; Dirsch, Verena M.; Heiss, Elke H. (2013). "Honokiol: A non-adipogenic PPARγ agonist from nature". Biochimica et Biophysica Acta 1830 (10): 4813–9. doi:10.1016/j.bbagen.2013.06.021. PMC 3790966. PMID 23811337. 
  4. ^ Atanasov, Atanas G.; Blunder, Martina; Fakhrudin, Nanang; Liu, Xin; Noha, Stefan M.; Malainer, Clemens; Kramer, Matthias P.; Cocic, Amina; Kunert, Olaf; Schinkovitz, Andreas; Heiss, Elke H.; Schuster, Daniela; Dirsch, Verena M.; Bauer, Rudolf (2013). "Polyacetylenes from Notopterygium incisum–New Selective Partial Agonists of Peroxisome Proliferator-Activated Receptor-Gamma". PLoS ONE 8 (4): e61755. Bibcode:2013PLoSO...861755A. doi:10.1371/journal.pone.0061755. PMC 3632601. PMID 23630612.