Synthesis and biological activity of peptide antagonists of luliberin (luteinizing hormone-releasing hormone)

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Abstract
A series of des-His2 octa- and nonapeptide analogs of luliberin (luteinizing hormone-releasing hormone) with modifications in the 1 and 6 positions, and in some instances the 10 position, was prepared. Some analogs are potent inhibitors of luliberin in vitro and in vivo in rats. The use of UV absorption measurements for evaluating peptides containing tyrosine and tryptophan is described. An efficient synthesis of O-methyl-D-tyrosine is reported.