Synthesis and receptor binding of Cys-endomorphin

M. Szücs, Lajos Baláspiri, Géza Tóth, Noboru Yanaihara

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

This paper describes the synthesis and binding profile of a new analog of endomorphin, Cys-endomorphin (C-Y-P-W-F-NH2), to μ- and δ-opioid receptors in rat brain. The new derivative displayed an IC50 of 16 ± 4.7 and > 10,000 nM against the μ-selective [3H] endomorphin-2 and the highly δ-specific [3H] Ile(5,6)-deltorphin II, respectively. Thus, Cys-endomorphin also favors μ- versus δ-opioid binding sites similarly to the parent peptide. The new ligand displayed weak potency with an IC50 of 3,800 nM for [3H] naloxone binding. Even in 10-5 M, the highest concentration tested, Cys-endomorphin was not able to produce 50% inhibition of [3H] naloxone binding in the presence of 100 mM Na+. The data, however, indicated that the agonistic character of endomorphins was retained for the new analog. The difference in the affinity of Cys-endomorphin for peptides versus naloxone supports previous observations with other μ-opioid ligands, namely that disctinct domains of the receptor might participate in the binding of these structurally different compounds.

Original languageEnglish
Pages (from-to)253-258
Number of pages6
JournalBiomedical Research
Volume20
Issue number5
Publication statusPublished - 1999

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Naloxone
Opioid Analgesics
Inhibitory Concentration 50
Ligands
Peptides
Opioid Receptors
Rats
Brain
Binding Sites
Derivatives

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)

Cite this

Szücs, M., Baláspiri, L., Tóth, G., & Yanaihara, N. (1999). Synthesis and receptor binding of Cys-endomorphin. Biomedical Research, 20(5), 253-258.

Synthesis and receptor binding of Cys-endomorphin. / Szücs, M.; Baláspiri, Lajos; Tóth, Géza; Yanaihara, Noboru.

In: Biomedical Research, Vol. 20, No. 5, 1999, p. 253-258.

Research output: Contribution to journalArticle

Szücs, M, Baláspiri, L, Tóth, G & Yanaihara, N 1999, 'Synthesis and receptor binding of Cys-endomorphin', Biomedical Research, vol. 20, no. 5, pp. 253-258.
Szücs M, Baláspiri L, Tóth G, Yanaihara N. Synthesis and receptor binding of Cys-endomorphin. Biomedical Research. 1999;20(5):253-258.
Szücs, M. ; Baláspiri, Lajos ; Tóth, Géza ; Yanaihara, Noboru. / Synthesis and receptor binding of Cys-endomorphin. In: Biomedical Research. 1999 ; Vol. 20, No. 5. pp. 253-258.
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