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Four analogs of luteinizing hormone-releasing hormone (LH-RH), [des-His2,D-Ala6]-LH-RH, [des-His2,D-Ala6, des-Gly-NH2(10)1-LH-RH ethylamide, [des-His2,D-Leu6]-LH-RH, and [D-Phe2,D-Leu6]-LH-RH, at 300-fold molar ratios (analog/LH-RH) led to an almost complete inhibition of LH response to LH-RH in anesthetized 4-day cycling rats on the afternoon of proestrus. At a 75-fold molar ratio, [des-His2,D-Ala6]-LH-RH still inhibited the LH-RH-induced LH release by 50%. The ethylamide substitution at the COOH terminus of [des-His2,D-Ala6]-LH-RH did not significantly improve the inhibitory activity of the molecule.
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