The Design of Site-Directed Radiopharmaceuticals for Use in Drug Discovery

  • William C. Eckelman
  • Raymond E. Gibson


The application of Nuclear Medicine technologies to drug discovery can be divided into two approaches: 1) the use of currently available radiopharmaceuticals to determine the presence of either a desired or unwanted physiological effect or 2) the ability to determine the interaction of the drug with a desired target (e.g., receptor or enzyme) in a specific organ. The first of these is described in Chapters 9, 15 and 16 of this book. Although drugs can be labeled with either positron emitting or single photon emitting nuclides, the selection of the drug to be labeled and the validation of the radiolabeled drug as one providing the desired information is still problematic. An entire field of basic research in Nuclear Medicine involving receptor binding radiotracers has grown since 1970, but many aspects of radioligand design remain empirical.


Positron Emission Tomography Affinity Constant Cereb Blood Flow Sigma Receptor Receptor Concentration 
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Copyright information

© Birkhäuser Boston 1993

Authors and Affiliations

  • William C. Eckelman
    • 1
  • Raymond E. Gibson
    • 2
  1. 1.PET DepartmentNational Institutes of HealthUSA
  2. 2.Radiopharmacology DepartmentMerck Research LaboratoriesUSA

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