A transient state concept of drug receptor interaction

  • Heinz Lüllmann
  • Albrecht Ziegler
Article

Summary

  1. 1.

    Experimental results obtained with muscarine-like drugs cannot be explained satisfactorily by existing drug receptor theories.

     
  2. 2.

    The time courses and extents of the negative inotropic effects and that of the desensitization caused by cholinomimetic drugs were recorded in guinea-pig isolated, electrically driven atria. The uptake of 3H-carbachol by the tissue was measured under identical experimental conditions.

     
  3. 3.

    A concept of drug receptor interaction is proposed based upon these experimental results. It differs from the existing theories by including both the disposal of the drug molecules in the biophase (drug transport) and the existence of an inactivated drug receptor complex. The active drug receptor complex is regarded as a transient state.

     
  4. 4.

    The transient state concept makes it possible to use only one set of constants to describe uptake curves and effect curves over the entire dose range.

     

Key words

Muscarinic Drugs Drug-Receptor-Interaction Kinetic Model Desensitization Fading 

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Copyright information

© Springer-Verlag 1973

Authors and Affiliations

  • Heinz Lüllmann
    • 1
  • Albrecht Ziegler
    • 1
  1. 1.Institut für PharmakologieChristian Albrechts-UniversitätKielGermany

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