Inhibition of LH-release by synthetic analogues of LH-RH in rat pituitary cell culture

Károly Nikolics, Christian Bieglmayer, Jürgen Spona, J. Seprődi, István Teplán

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Conditions for testing the inhibitory activity of synthetic analogues of LH-RH in monolayer cultures of rat pituitary cells were optimized. Nine synthetic derivatives of LH-RH were tested to evaluate their inhibitory dose50 (ID50) values. The peptide antagonists tested included linear, branched-chain, dimeric and tetrameric derivatives of LH-RH. Ac-D-Phe1, D-Cpa2, D-Trp3.6-LH-RH (analogue V) was found to be the most effective competitive inhibitor of the series with an ID50 value of 6×10-9M in the presence of 10-9 M LH-RH. The kinetics of the LH-RH-blocking action of two inhibitors were also studied. Both the linear (analogue I) and the dimeric (analogue VI) peptide showed immediate inhibition of LH-release. Prolonged inhibitory activity of the same two peptides was observed when cells were incubated with LH-RH subsequent to preincubation with the inhibitors.

Original languageEnglish
Pages (from-to)65-73
Number of pages9
JournalPeptides
Volume2
Issue number1
DOIs
Publication statusPublished - 1981

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Cell culture
Gonadotropin-Releasing Hormone
Rats
Cell Culture Techniques
Peptides
Derivatives
Monolayers
Kinetics
Testing

Keywords

  • Inhibition of LH-release
  • LH-RH analogues
  • Pituitary cell culture

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

Cite this

Inhibition of LH-release by synthetic analogues of LH-RH in rat pituitary cell culture. / Nikolics, Károly; Bieglmayer, Christian; Spona, Jürgen; Seprődi, J.; Teplán, István.

In: Peptides, Vol. 2, No. 1, 1981, p. 65-73.

Research output: Contribution to journalArticle

Nikolics, Károly ; Bieglmayer, Christian ; Spona, Jürgen ; Seprődi, J. ; Teplán, István. / Inhibition of LH-release by synthetic analogues of LH-RH in rat pituitary cell culture. In: Peptides. 1981 ; Vol. 2, No. 1. pp. 65-73.
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