Modification of Membrane Function by Drugs

  • James W. PutneyJr.
  • Amir Askari


The importance of the surface membrane of cells as the primary site of action of many drugs has been obvious since the earliest conceptions of membranes as regulatory barriers. As soon as the permeability characteristics of cells became apparent, investigators reasoned that polar and highly water-soluble agents were unlikely to gain access to the inner plasma of cells. The rapid action of many of these compounds similarly argued for the cell surface as a probable site of action. Ingenious quantitative analyses by A. J. Clarkw(1) showed that most drugs are maximally effective when occupying only a small fraction of the total surface area available. Thus the concept of specific recognition sites or receptors in (or on) the membrane was introduced. With very little modificatión, this concept remains today as a cornerstone principle of the basic mechanisms of drug action. Even agents that do not act through “classical” receptor mechanisms (e.g., the anesthetics discussed herein) produce their pharmacological actions by modifying membrane funtion. The effects of pharmacological agents on membrane functions have, therefore, a dual importance. First, such knowledge may obviously yield concepts useful in the alleviation or management of diseases that directly involve disorders of membrane function. Second, it is becoming increasingly apparent that the mode of actions of most (if not all) pharmacological agents involves modification of membrane functions either directly or indirectly. Thus the action of drugs on membrane functions can be considered a fundamental aspect of drug action important in virtually all areas of pharmacology.


Smooth Muscle Local Anesthetic Adenylate Cyclase Parotid Gland Cholera Toxin 
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Copyright information

© Springer Science+Business Media New York 1980

Authors and Affiliations

  • James W. PutneyJr.
    • 1
  • Amir Askari
    • 2
  1. 1.Department of PharmacologyWayne State University School of MedicineDetroitUSA
  2. 2.Department of Pharmacology and TherapeuticsMedical College of OhioToledoUSA

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