New insights in insurmountable antagonism

  title={New insights in insurmountable antagonism},
  author={G. Vauquelin and I. Van Liefde and B. B. Birzbier and P. Vanderheyden},
  journal={Fundamental & Clinical Pharmacology},
  • G. Vauquelin, I. Van Liefde, +1 author P. Vanderheyden
  • Published 2002
  • Biology, Medicine
  • Fundamental & Clinical Pharmacology
  • Antagonists that produce parallel rightward shifts of agonist dose–response curves with no alteration of the maximal response are traditionally classified as surmountable, while insurmountable antagonists also depress the maximal response. Although the longevity of the antagonist–receptor complex is quoted in many studies to explain insurmountable antagonism, slowly interconverting receptor conformations, allosteric binding sites, and receptor internalization have been evoked as alternative… CONTINUE READING
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