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

doi:10.1016/0006-291X(81)91910-0

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-Phe^1,2, D-Trp³, D-Phe⁶,D-Ala¹⁰]-LH-RH and [N-acetyl-D-Trp^1,3,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)
Pages (from-to)	915-920
Number of pages	6
Journal	Biochemical and biophysical research communications
Volume	100
Issue number	3
DOIs	https://doi.org/10.1016/0006-291X(81)91910-0
State	Published - Jun 16 1981

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ASJC Scopus subject areas

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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Erchegyi, J., Coy, D. H., Nekola, M. V., Coy, E. J., Schally, A. V., Mezo, I., & Teplan, I. (1981). Luteinizing hormone-releasing hormone analogs with increased anti-ovulatory activity. Biochemical and biophysical research communications, 100(3), 915-920. https://doi.org/10.1016/0006-291X(81)91910-0

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title = "Luteinizing hormone-releasing hormone analogs with increased anti-ovulatory activity",

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.",

author = "J. Erchegyi and Coy, {D. H.} and Nekola, {M. V.} and Coy, {E. J.} and Schally, {A. V.} and I. Mezo and I. Teplan",

year = "1981",

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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.

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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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10.1016/0006-291X(81)91910-0