Tritiated deltorphin analogues with high specific radioactivity and high affinity and selectivity for delta opioid receptors

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8 Citations (Scopus)

Abstract

New conformationally constrained deltorphin I and II analogues were designed and synthesized, using a more lipophilic amino acid (Ile) instead of Val at positions 5 and 6, and 2-aminotetralin-2-carboxylic acid (Atc) at position 3. Two analogues (Tyr-D-Ala-(S)-Atc-Asp-Ile-Ile-Gly-NH2 and Tyr-D-Ala-(R)-Atc-Glu-Ile-Ile-Gly-NH2) with high potency and selectivity for δ opioid receptors were chosen for tritiation, with 3,5-I2-Tyr1-deltorphin analogues as precursors. Catalytic dehalotritiation of these precursors resulted in tritiated peptides with high specific radioactivity (1.28 TBq/mmol (34.5 Ci/mmol) and 1.33 TBq/mmol (36.0 Ci/mmol), respectively).

Original languageEnglish
Pages (from-to)817-826
Number of pages10
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume39
Issue number10
DOIs
Publication statusPublished - Oct 1 1997

Keywords

  • Dehalogenation
  • Deltorphins
  • Iodination
  • Opioid receptors

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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