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LH-releasing activity of potent LH-RH analogs in vitro
Authors:DH Coy  FLabrieM Savary  EJ Coy  AV Schally
Institution:1. Medical Research Council Group in Molecular Endocrinology, Centre Hospitalier de l''Université Laval, Québec, G1V 4G2, Canada;2. Polypeptide Laboratories, V.A. Hospital and Tulane University School of Medicine, New Orleans, La., U.S.A.
Abstract:The LH-releasing activity of eight superactive analogs of LH-RH was measured in pituitary cells in primary culture. Introduction of the C-terminal ethylamide modification into D-Ala6]- and D-Leu6]-LH-RH (two peptides already 3 times more active than LH-RH) increases their activities 10-fold. D-Phe6]- and D-Trp6]-LH-RH are 90 and 100 times more active than LH-RH, respectively. The ethylamide derivatives of these two compounds are however approximately six times less active than the parent peptides.
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