Binding characteristics of novel delta receptor selective opioid peptides

A. Borsodi, M. Spelea, I. Szatmari, Z. Darula, I. Kertesz, G. Toth

Research output: Contribution to journalArticle

Abstract

New opioid agonists and antagonists have been developed in normal and in tritiated forms. The compounds have been tested uy in vitro binding assays in various systems. The agonist deltorphins ..' aitous derivatives of the antagonist TIPP (H-Tyr-Tic-Phe-Phe- OH) have ueen synthezised The pseudopeptide TIPPT (H-Tyr-TicTICHv-NHlPhe-Phe-OH) and TICPT (H-TyrTicT[CH2-NH]Cha-Phe-OH) not only display very exceptional selectivity but show high stability against enzymatic degradation All of the radioligands exhibit ingh affinity (Kj values in the nanomolar range) and label single class uf binding site. Displacement studies indicated the following and order of potencies. delta"kappa>mu for the agonists; delta>>mu>kappa for the antagonists and the high specific radioactivity and selectivity.

Original languageEnglish
JournalFASEB Journal
Volume11
Issue number9
Publication statusPublished - 1997

Fingerprint

opioid peptides
delta Opioid Receptor
Opioid Peptides
agonists
antagonists
receptors
Narcotic Antagonists
Radioactivity
Opioid Analgesics
enzyme stability
Labels
Assays
Binding Sites
narcotics
Derivatives
Degradation
binding sites
chemical derivatives
degradation
assays

ASJC Scopus subject areas

  • Agricultural and Biological Sciences (miscellaneous)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Biochemistry
  • Cell Biology

Cite this

Binding characteristics of novel delta receptor selective opioid peptides. / Borsodi, A.; Spelea, M.; Szatmari, I.; Darula, Z.; Kertesz, I.; Toth, G.

In: FASEB Journal, Vol. 11, No. 9, 1997.

Research output: Contribution to journalArticle

Borsodi, A, Spelea, M, Szatmari, I, Darula, Z, Kertesz, I & Toth, G 1997, 'Binding characteristics of novel delta receptor selective opioid peptides', FASEB Journal, vol. 11, no. 9.
Borsodi, A. ; Spelea, M. ; Szatmari, I. ; Darula, Z. ; Kertesz, I. ; Toth, G. / Binding characteristics of novel delta receptor selective opioid peptides. In: FASEB Journal. 1997 ; Vol. 11, No. 9.
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