Új potenciális oxitocin antagonisták szintézise és in vitro receptoranalitikai vizsgálata

Translated title of the contribution: Synthesis and in vitro receptor analysis of new potential oxytocin antagonists

J. Havass, K. Bakos, G. Tóth, F. Fülöp, G. Falkay

Research output: Contribution to journalArticle

Abstract

Oxytocin (OT) itself and the sensitivity of the uterus to OT play a crucial role in the initiation of both normal and pathologically early delivery. It recognition of the complex mechanism of action suggests that specific OT antagonists are of therapeutic value in postponing early contractions. In this study neurohypophyseal hormone analogues containing Sar in position 7, Arg in position 8, and various conformationally restricted or bulky derivatives of phenilalanine and tryptophan amino acids in position 2 were prepared to design more potent and selective OT antagonists. We determined the ligand-receptor binding characteristics of these newly synthetized peptides in the presence of [3H]oxytocin and [3H]vasopressin on isolated guinea-pig uterus, rat liver and kidney inner medulla plasma membranes. In the case of each peptides we calculated the Ki values and the selectivity ratio. The binding to the OT receptor was dramatically decreased for the Trp-derivatives containing analogues, while the Phe-derivatives containing analogues diplayed a relatively high receptor affinity and have a relatively high OT/VP1 receptor selectivity.

Translated title of the contributionSynthesis and in vitro receptor analysis of new potential oxytocin antagonists
Original languageHungarian
Pages (from-to)168-174
Number of pages7
JournalActa pharmaceutica Hungarica
Volume70
Issue number3-6
Publication statusPublished - Jan 1 2000

ASJC Scopus subject areas

  • Pharmaceutical Science

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