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 language||English (US)|
|Number of pages||6|
|Journal||Biochemical and biophysical research communications|
|State||Published - Jun 16 1981|
ASJC Scopus subject areas
- Molecular Biology
- Cell Biology