The Pharmacologic Estimation of Potencies of Agonists and Antagonists in the Classification of Adenosine Receptors

  • Terry P. Kenakin
  • H. J. Leighton


This chapter outlines some of the methods used to quantitate drug effects in isolated tissues for the purposes of adenosine receptor classification. There are advantages and disadvantages to studying adenosine receptors in isolated tissues. The disadvantages are that numerous pharmacokinetic factors and reflex mechanisms make extrapolation of isolated tissue data to whole animals and man hazardous. Also, the quantitative parameters for drugs are calculated from models assuming an equilibrium between the drugs and the receptors, which is a condition often not obtained in intact tissues. However, these factors are balanced by two major advantages. If it is assumed that the independent variable in pharmacologic experiments is drug concentration and the dependent variable is tissue response, experiments in isolated tissues allow adequate control of the independent variable (under careful experimental conditions) such that meaningful dependent variables can be obtained. Also, quantitative estimates of agonist efficacy, a quantity currently inaccessible in biochemical binding studies, can be obtained from experiments in isolated tissues. Thus, drug affinity and efficacy can be quantified and used in the classification of adenosine receptors.


Tissue Factor Adenosine Receptor Partial Agonist Full Agonist Equilibrium Dissociation Constant 
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© Plenum Press, New York 1985

Authors and Affiliations

  • Terry P. Kenakin
    • 1
  • H. J. Leighton
    • 1
  1. 1.Department of Pharmacology The Wellcome Research LaboratoriesBurroughs Wellcome CompanyResearch Triangle ParkUSA

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