Luteinizing-follicle stimulating hormone releasing hormone - analogues with 7-leucine replaced by other amino acids

摘要

Peptides of formula (I): (where X is Ser(But), Cys(But), Asp(OBut), Glu(OBut), Orn(Boc) or Lys(Boc); Y is glycinamide or NHR; R is 1-3C alkyl opt. substd. by OH or halogen, or cyclopropyl; and Trp can be replaced by pentamethylphenylalanine, Ser can be replaced by Ala or Thr. Tyr can be replaced by Phe, Gly can be replaced by a D-amino acid corresp. to a naturally occurring L-amino acid, Arg can be replaced by Orn, and Lys can be replaced by homoarginine), are analogues of the natural luteinising hormone/follicle stimulating hormone releasing hormone (LH-RH/FSH-RH) in which X=Leu and Y=Gly-NH2, and can thus be used for treating feminine and masculine sterility of hypophysical origin and in the diagnosis of hypophysis dysfunction; they are more than twice the activity of the natural LH-RH/FSH-RH and exhibit a pronounced depot effect.