Luteinizing hormone-releasing hormone analogs with increased anti-ovulatory activity |
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Authors: | J. Erchegyi D.H. Coy M.V. Nekola E.J. Coy A.V. Schally I. Mezo I. Teplan |
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Affiliation: | 1. Department of Medicine, Tulane University School of Medicine, New Orleans, Louisiana 70112 USA;2. VA Medical Center, New Orleans, Louisiana 70112 USA |
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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. |
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Keywords: | t-BOC t-butyloxycarbonyl TFA trifluoroacetic acid TLC thin layer chromatography HPLC high pressure liquid chromatography |
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