Drug Binding and Drug Effect

  • Ronald J. Tallarida
  • Leonard S. Jacob


Drugs that bind readily to a tissue may differ markedly in their ability to produce an effect. In other words, they differ in efficacy or in intrinsic activity. We do not know the reason for these differences; in fact, we do not know very much about the sequence of events between binding and effect. A reasonable explanation would seem to be access to the receptor. Clearly, if the drug molecule cannot arrive at the receptor, then no effect is possible. However, even when access to the receptor is not limited, the effect may not temporally follow the binding. For example, if acetylcholine is administered to a tissue, the effect can rise to a peak and then fall to some lower level, even though the concentration at the receptor is still apparently rising. As a specific example, we mention the work of Lullman and Ziegler,33 who studied the time course of uptake of carbachol by the guinea pig atria and the time course of the effect, decreased contractile force. The time courses of effect and concentration were very different. The effect reached its final value in 2–3 min, whereas the uptake was still in progress even after 30 min. These are just two examples, but there are numerous others which suggest a temporal dependence in the concentration-effect relationship. Thus, access to the receptors is not a general explanation for differences in the efficacy. Furthermore, binding to the tissue may bear no relation to a drug’s ability to produce an effect.


Dissociation Constant Drug Binding Pharmacological Method Renal Tubular Secretion Quinuclidinyl Benzilate 
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© 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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