Determining the potency and molecular mechanism of action of insurmountable antagonists.

@article{Kenakin2006DeterminingTP,
  title={Determining the potency and molecular mechanism of action of insurmountable antagonists.},
  author={Terry Kenakin and Stephen Jenkinson and Christian A Watson},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2006},
  volume={319 2},
  pages={710-23}
}
Insurmountable antagonism (maximal response to the agonist depressed) can result from a temporal inequilibrium involving a slow offset orthosteric antagonist or be the result of an allosteric modulation of the receptor. The former mechanism is operative when the antagonist, agonist, and receptors cannot come to proper equilibrium during the time allotted for collection of agonist response (hemi-equilibrium conditions). Allosteric effects (changes in the conformation of the receptor through… CONTINUE READING
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