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Radiolabeled Atrial Natriuretic Peptide and Somatostatin for in Vivo Imaging of Receptors

  • Richard J. Flanagan

Abstract

For many years peptides and proteins labeled with Iodine-125 on tyrosine residues have been standard tools of biochemistry for the in vitro mapping of receptors. Such methods provide microscopic information on a cellular level but little overall information about the in vivo biodistribution of the receptors and their dynamic relationship with their endogenous ligands. The gathering of this in vivo information by techniques such as Nuclear Imaging has been limited by the rapid catabolism of radiolabeled peptides in circulation. This is not as a result of labeling but is due to the extremely short half-life of peptides in vivo. The normal fate of peptides in circulation is to be partitioned between a large pool of low affinity non-specific peptidases and a small quantity of specific, high affinity receptors. Under such circumstances the labeled peptide will preferentially bind to the high affinity receptors but injection of amounts greater than the capacity of the receptors will cause overflow into the non-specific peptidase pool, with corresponding loss of information. Furthermore, it is important that receptor occupancy by the labeled peptide be limited, perhaps to less than 10% of receptor mass, in order that the ligand/receptor interactions observed are true tracer phenomena and not due to perturbation of the natural equilibrium by the injected material.

Keywords

Atrial Natriuretic Peptide Guanylate Cyclase Atrial Natriuretic Factor Receptor Mediate Uptake Minute Post Injection 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Birkhäuser Boston 1993

Authors and Affiliations

  • Richard J. Flanagan
    • 1
  1. 1.Merck FrosstCanada

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