Abstract

The anti-LH-releasing activity of several analogues of LH-RH was tested by 2-hour infusion in ovariectomized, estrogen-progesterone-pretreated rats and in immature male rats. [Leu3]LH-RH, [Leu3, desGly10]-LH-RH ethylamide, [desHis2, Leu3,desGly10]-LH-RH ethylamide, [Gly2, Leu3,desGly10]-LH-RH ethylamide, [Leu1, desGly10]-LH-RH ethylamides, [desHis2,D-Ala6,desGly10]-LH-RH ethylamide, [desHis2,Leu3,D-Ala6, desGly10]-LH-RH ethylamide, and [D-pGlu1,desGly10]-LH-RH ethylamide, and and [D-pGlu1,desHis2,desGly10]-LH-RH ethylamide showed some anti-LH-releasing activity, but never completely inhibited the increase in serum LH in response to LH-RH. No significant differences were found among the analogues tested and [desHis2,desGly10]-LH-RH ethylamide, and inhibitory potency was not improved with those peptides containing D-alanine in position 6 of the chain. None of the analogues tested, including [desHis2,desGly10]-LH-RH ethylamide, was able to block the LH-RH-induced FSH release in these systems.

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