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Updated: Apr 29, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
A pharmacological paradox: may a neutral antagonist shift an agonist concentration-response curve to the left?
1Freiburg Institute for Advanced Studies (FRIAS), University of Freiburg, 79104, Freiburg, Germany, thomas.feuerstein@uniklinik-freiburg.de.
Abstract:
It is generally accepted that the presence of a competitive antagonist shifts an agonist concentration-response curve to the right. However, this may not always be the case: The concentration-response curve of an inverse receptor agonist may be shifted to the left by a neutral antagonist; a condition, which can be hypothetically explained by the assumption of both negative cooperativity of dimeric receptors plus a receptor reserve.
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