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3′,5′-Ditritiomethotrexate as a Granulocyte Label

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Abstract

THE folic acid antagonist methotrexate (amethopterin; 4-amino-4-deoxy-10-methylpteroylglutamate), when administered to human subjects, binds tightly to the enzyme dihydrofolate reduetase., present in immature leucocytes and in developing erythrocyte forms1–3. Bioassay of bound methotrexate has shown that the compound appears to remain with the leucocyte throughout its life-span1,2. In this communication we are reporting the synthesis of tritium-labelled methotrexate (MTX-3H) of very high specific activity (15.4 c./mmole), and its use as a tag in studies of granulocyte kinetics.

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Authors and Affiliations

  1. Departments of Pharmacology and Medicine, Yale University School of Medicine, New Haven, Connecticut

    J. R. BERTINO, D. G. JOHNS, P. ALMQUIST & J. W. HOLLINGSWORTH

  2. Organic Department, Radiochemical Centre, Amersham, Buckinghamshire, England

    E. A. EVANS

Authors
  1. J. R. BERTINO
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  2. D. G. JOHNS
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  3. P. ALMQUIST
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  4. J. W. HOLLINGSWORTH
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  5. E. A. EVANS
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BERTINO, J., JOHNS, D., ALMQUIST, P. et al. 3′,5′-Ditritiomethotrexate as a Granulocyte Label. Nature 206, 1052–1053 (1965). https://doi.org/10.1038/2061052b0

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