Kinetics of Drug—Receptor Interaction: Interpreting Dose—Response Data

  • Ronald J. Tallarida
  • Leonard S. Jacob


The concept of the pharmacological receptor was introduced by Langley28 and by Ehrlich.11 Langley’s formulation was based on experiments in which he applied nicotine to small regions of a muscle surface. He observed that a muscle twitch occurred only when the nicotine was applied to certain small areas of the muscle surface and, hence, he postulated the existence of a receptive substance at those small areas. Ehrlich, on the other hand, worked with various dyes, observing that some cells were stained more deeply or in a different way from other cells. These observations suggested to Ehrlich that a general theory could be developed that would explain the selective action of drugs. Much study since then, particularly studies that showed that other substances could inhibit or block the specific action of a drug, have given general acceptance to the receptor concept. The most general definition of a receptor is that it is that component of the cell that combines chemically with a drug in order to produce an effect. For the most part we know little about the chemical or physicochemical makeup of the receptor. In that respect, the receptor has been described as a measure of our ignorance by Gero20; yet the concept has proved most helpful in pharmacology.


Dissociation Constant Partial Agonist Receptor Occupancy Rate Theory Full Agonist 
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Copyright information

© Springer-Verlag New York Inc. 1979

Authors and Affiliations

  • Ronald J. Tallarida
    • 1
  • Leonard S. Jacob
    • 2
    • 3
    • 4
  1. 1.Temple University School of MedicinePhiladelphiaUSA
  2. 2.Department of AnesthesiologyUniversity of Pennsylvania School of MedicinePhiladelphiaUSA
  3. 3.Department of PharmacologyUniversity of Pennsylvania School of MedicinePhiladelphiaUSA
  4. 4.Medical College of PennsylvaniaPhiladelphiaUSA

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