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Affinity and Efficacy of Oxotremorine Analogs at Ileal Muscarinic Receptors

  • B. Ringdahl
Part of the Advances in Behavioral Biology book series (ABBI, volume 30)

Abstract

The pharmacological activity of a muscarinic agonist, as measured for example by contractile responses in smooth muscle preparations, is a function of both its affinity for the receptor and its efficacy in producing a stimulus that leads to a response (26). Because of the existence in many tissues of a receptor reserve for muscarinic agonists, ED50 values for pharmacological responses often are poor estimates of affinities. More satisfactory estimates of agonist affinities may be obtained from receptor binding studies. Although the relationship between binding parameters and ED50 values of muscarinic agonists is not yet fully understood, radioligand binding techniques have given valuable information on the structural demands for agonist binding at the muscarinic receptor (3, 12). In contrast, the structural features of muscarinic agonists that cause them to activate the receptor are less readily assessed.

Keywords

Muscarinic Receptor Partial Agonist Receptor Occupancy Relative Efficacy Muscarinic Agonist 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Plenum Press, New York 1986

Authors and Affiliations

  • B. Ringdahl
    • 1
  1. 1.Department of Pharmacology School of MedicineUniversity of CaliforniaLos AngelesUSA

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