Structure-activity relationships in luteinizing hormone-releasing hormone

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Abstract
Three analogs of luteinizing hormone-releasing hormone (LH-RH) of the structure less than Glu-His-Trp-Ser-Tyr-Gly-Gly-Leu-Arg-Pro-Gly-NH2, involving substitutions inpositions 1, 3, and 8 with nonprotein amino acids, have been synthesized by the solid-phase method. They are [pyro-L-alpha-(1-aminoadipic)]-LH-RH, [3-(2-naphthyl)-L-Ala3]-LH-RH, and [delta-N-i-Pr-L-Orn8]-LH-RH. Their LH-RH activities in vivo were 12.5, 51.8, and 3.7% that of LH-RH, respectively, in the assay using ovariectomized, estrogen- and progesterone-treated rats. In a test based upon subcutaneous injection into immature male rats, [3-(2-naphthyl)-Ala3]-LH-RH released 1.2 times as much LH and 0.8 times as much FSH as synthetic LH-RH.

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