Preparation of specifically tritiated endomorphins

C. Tömböly, Rajiv Dixit, Imre Lengyel, A. Borsodi, Géza Tóth

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

Endomorphin-1 (EM1, Tyr-Pro-Trp-Phe-NH2) and endomorphin-2 (EM2, Tyr-Pro-Phe-Phe-NH2) are natural tetrapeptide ligands of μ-opioid receptors involved in the modulation and attenuation of pain. For a detailed examination of their receptor-binding properties and their metabolic stability, tritium-labelled EM1 and EM2 radioisotopomers were synthesized by catalytic dehalogenation or saturation of the precursor peptides with tritium gas. Amino acid analysis revealed that the tritium labelling was specific and the specifically labelled radioligands possessed high specific activity, ranging from 0.77 TBq/mmol to 2.35 TBq/mmol. The biological half-lives of the peptides in the biological matrix (295 min and 230 min for EM1 and EM2, respectively) indicate that these radioligands are appropriate for binding assays in rat brain membrane preparations. The radioisotopomers of EM2 are not statistically different in the receptor-ligand interaction, and they are excellent tools for further comparative biochemical studies.

Original languageEnglish
Pages (from-to)355-363
Number of pages9
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume44
Issue number5
DOIs
Publication statusPublished - 2001

Fingerprint

Tritium
Dehalogenation
Ligands
Peptides
Opioid Receptors
Labeling
Rats
Assays
Brain
Gases
Modulation
Membranes
Amino Acids
Pain
endomorphin 2

Keywords

  • Endogenous opioid peptides
  • Endomorphins
  • Metabolism
  • Radioisotopomers
  • Specific labelling
  • Tritium

ASJC Scopus subject areas

  • Analytical Chemistry
  • Drug Discovery
  • Organic Chemistry
  • Clinical Biochemistry
  • Molecular Medicine
  • Pharmacology

Cite this

Preparation of specifically tritiated endomorphins. / Tömböly, C.; Dixit, Rajiv; Lengyel, Imre; Borsodi, A.; Tóth, Géza.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 44, No. 5, 2001, p. 355-363.

Research output: Contribution to journalArticle

Tömböly, C. ; Dixit, Rajiv ; Lengyel, Imre ; Borsodi, A. ; Tóth, Géza. / Preparation of specifically tritiated endomorphins. In: Journal of Labelled Compounds and Radiopharmaceuticals. 2001 ; Vol. 44, No. 5. pp. 355-363.
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