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Drug Binding and Drug Effect

  • Chapter
The Dose—Response Relation in Pharmacology

Abstract

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.

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Author information

Authors and Affiliations

  1. Temple University School of Medicine, 19140, Philadelphia, Pennsylvania, USA

    Ronald J. Tallarida Ph.D. (Professor of Pharmacology)

  2. Department of Anesthesiology, University of Pennsylvania School of Medicine, 19104, Philadelphia, Pennsylvania, USA

    Leonard S. Jacob M.D., Ph.D. (Faculty, Visiting Assistant Professor of Pharmacology)

  3. Department of Pharmacology, University of Pennsylvania School of Medicine, 19104, Philadelphia, Pennsylvania, USA

    Leonard S. Jacob M.D., Ph.D. (Faculty, Visiting Assistant Professor of Pharmacology)

  4. Medical College of Pennsylvania, 19129, Philadelphia, Pennsylvania, USA

    Leonard S. Jacob M.D., Ph.D. (Faculty, Visiting Assistant Professor of Pharmacology)

Authors
  1. Ronald J. Tallarida Ph.D.
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  2. Leonard S. Jacob M.D., Ph.D.
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© 1979 Springer-Verlag New York Inc.

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Tallarida, R.J., Jacob, L.S. (1979). Drug Binding and Drug Effect. In: The Dose—Response Relation in Pharmacology. Springer, New York, NY. https://doi.org/10.1007/978-1-4684-6265-4_5

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  • DOI: https://doi.org/10.1007/978-1-4684-6265-4_5

  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-1-4684-6267-8

  • Online ISBN: 978-1-4684-6265-4

  • eBook Packages: Springer Book Archive

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