Luteinizing hormone-releasing hormone analogs with increased anti-ovulatory activity

J. Erchegyi, D. H. Coy, M. V. Nekola, E. J. Coy, A. V. Schally, I. Mezo, I. Teplan

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Abstract

A series of LH-RH antagonist analogs has been developed in which inhibitory activities have been increased to a potentially clinically useful level. The new peptides, which are typified by [N-acetyl-D-p-Cl-Phe1,2, D-Trp3, D-Phe6,D-Ala10]-LH-RH and [N-acetyl-D-Trp1,3,D-p-Cl-Phe2,D-Phe6, D-Ala10]-LH-RH, most importantly contain new modification to positions 1, 2 and 10, and induce full blockade of ovulation at single doses as low as 10 μg per rat (50 μg/kg). Various ring substituents on D-Trp or D-Phe in position 1 or other D-amino acid replacements in position 10 did not significantly improve anti-ovulatory activity. Incorporation of N-Me-Leu in position 7 was slightly detrimental to activity.

Original languageEnglish (US)
Pages (from-to)915-920
Number of pages6
JournalBiochemical and biophysical research communications
Volume100
Issue number3
DOIs
StatePublished - Jun 16 1981

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ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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