Much of the conceptual framework regarding how to study receptor function evolved from pharmacological investigation of drug action. Consequently, the historical account of the development of receptor theory in this chapter, as well as the outline of how to characterize receptors in intact tissues in chapter 2, will emphasize early investigations of drug action rather than (for example) physiological studies of hormone action. However, the reader must keep in mind that drug can be defined as any agent that affects living processes. Drugs presumably bind to receptors designed for interaction with endogenous hormones and neurotransmitters or other regulatory agents. By way of definition, agonist drugs are analogous to endogenous hormones and neurotransmitters in the sense that they elicit a biological effect, although the effect elicited may be stimulatory or inhibitory. In contrast, antagonist drugs are defined as agents that block receptor-mediated effects elicited by hormones, neurotransmitters, or agonist drugs by competing for receptor occupancy. Most often, antagonists do not appear to have an endogenous counterpart in the strict sense of a competitive inhibitor of receptor occupancy.


Historical Perspective Receptor Occupancy Rate Theory Rectangular Hyperbola Agonist Drug 
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© kluwer Academic Publishers 1996

Authors and Affiliations

  • Lee E. Limbird
    • 1
  1. 1.Vanderbilt UniversityNashvilleUSA

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