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Pharmacokinetic Studies on Some Novel (2-Nitro-1-Imidazolyl) Propanolamine Radiosensitizers

  • M. R. L. Stratford
  • A. I. Minchinton
  • F. A. Stewart
  • V. S. Randhawa
Part of the NATO Advanced Study Institutes Series book series (NSSA, volume 43)

Abstract

One area of current interest in radiosensitizer development is in the use of nitroimidazoles of a more polar nature than misonida-zole, combining the benefits of a shorter half-life, and thus reduced tissue exposure, which has been correlated with the neuropathy observed with misonidazole (1), while also minimising brain penetration through the blood-brain barrier (2). In the Gray Laboratory development programme, one aim has been to attempt to combine the advantages of a highly polar compound with an increased radiosensi-tizing efficiency by including basic functions in the 2-nitroimida-zole side chain. Preliminary data for one of these, the propanol-amine Ro 03–8799, indicating favourable pharmacokinetic properties following intraperitoneal administration have already been published (3).

Keywords

Pharmacokinetic Study Polar Compound Intraperitoneal Administration Hypoxic Cell Polar Nature 
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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References

  1. 1.
    S. Disehe, M. I. Saunders, I. R. Flockhart, M. E. Lee, and P. Anderson, Misonidazole — A drug for trial in radiotherapy and oncology, Int. J. Rad. Oncol. Biol. Phys. 5:851 (1979).CrossRefGoogle Scholar
  2. 2.
    J. M. Brown, and P. Workman, Partition coefficient as a guide to the development of radiosensitizers which are less toxic than misonidazole, Radiat. Res. 82:171 (1980).PubMedCrossRefGoogle Scholar
  3. 3.
    J. Denekamp, Testing of hypoxic cell radiosensitizers in vivo, Cancer Clin. Trials 3:139 (1980).PubMedGoogle Scholar

Copyright information

© Plenum Press, New York 1982

Authors and Affiliations

  • M. R. L. Stratford
    • 1
  • A. I. Minchinton
    • 1
  • F. A. Stewart
    • 1
  • V. S. Randhawa
    • 1
  1. 1.Cancer Research Campaign Gray LaboratoryMount Vernon HospitalNorthwood, MiddlesexEngland

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