Kinins—II pp 39-50 | Cite as

Preparation of Intrinsically-Labelled Kinins

  • Alfred Chung
  • James W. Ryan
  • Pierre Berryer
  • Ronald Block
Part of the Advances in Experimental Medicine and Biology book series (AEMB)

Abstract

As part of a program to prepare bradykinin (H-Arg-Pro-ProGly-Phe-Ser-Pro-Phe-Arg-OH) labelled at high specific radioactivities, we have synthesized three analogs for dehalogenation in tritium gas: [4-Br-Phe5]-bradykinin (BK), [4-Br-Phe8]-BK and [4-Br-Phe5,8]-BK. The analogs were synthesized by the Merrifield solid-phase method and were purified by molecular sieve and partition chromatography. The analogs themselves possess biological activity (as assayed for effects on mean arterial blood pressure and isolated rat uterus). [4-Br-Phe8]-BK was 1.5 to 3 times as active as bradykinin. [4-Br-Phe5,8]-BK was approx. 22% as active as BK and [4-Br-Phe5]-BK was approx. 18% as active. [4-Br-Phe5]-BK was submitted to catalytic dehalogenation with 10% Pd/C and 5% Rh/CaCO3 in H2O and DMF (1:1) plus 10 Ci of 3H2. [4-3H-Phe5]-BK was obtained at 6.7 Ci/mmole in an overall yield of 15%. [4-3HPhe8]-BK was prepared similarly to yield an intrinsically-labelled peptide with a specific radioactivity of 21 Ci/mmole.

Keywords

Angiotensin Converting Enzyme Specific Radioactivity Hydrogen Fluoride Solid Phase Peptide Synthesis Cesium Salt 
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

© Springer Science+Business Media New York 1979

Authors and Affiliations

  • Alfred Chung
    • 1
  • James W. Ryan
    • 1
  • Pierre Berryer
    • 1
  • Ronald Block
    • 2
  1. 1.Department of MedicineUniversity of Miami School of MedicineMiamiUSA
  2. 2.Papanicolaou Cancer Research InstitueMiamiUSA

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