TY - JOUR
T1 - Luteinizing hormone-releasing hormone analogs with increased anti-ovulatory activity
AU - Erchegyi, J.
AU - Coy, D. H.
AU - Nekola, M. V.
AU - Coy, E. J.
AU - Schally, A. V.
AU - Mezo, I.
AU - Teplan, I.
PY - 1981/6/16
Y1 - 1981/6/16
N2 - 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.
AB - 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.
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U2 - 10.1016/0006-291X(81)91910-0
DO - 10.1016/0006-291X(81)91910-0
M3 - Article
C2 - 7023483
AN - SCOPUS:0019841525
VL - 100
SP - 915
EP - 920
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
SN - 0006-291X
IS - 3
ER -