title: Increased potency and sustained suppressive actions of a new gonadotropin-releasing hormone (GnRH) antagonist peptide in man.
abstract: We have used a new potent GnRH antagonist to assess the efficacy of suppression of gonadotropin secretion in healthy postmenopausal women at three different doses. The Nal-Glu antagonist produced significant suppression of immunoactive and bioactive LH at a 300 micrograms/kg dose throughout the 30-hr sampling interval with only minimal local (skin) histamine release. This increased potency and decreased skin reactivity of the Nal-Glu antagonist make it a drug with potential clinical use similar to the GnRH agonist, but with the advantage of immediate gonadotropin suppression.
authors.affiliation: Department of Internal Medicine, University of Virginia School of Medicine, Charlottesville 22908.
authors.forename: R J
authors.initials: RJ
authors.lastname: Urban
authors.forename: S N
authors.initials: SN
authors.lastname: Pavlou
authors.forename: J E
authors.initials: JE
authors.lastname: Rivier
authors.forename: W W
authors.initials: WW
authors.lastname: Vale
authors.forename: M L
authors.initials: ML
authors.lastname: Dufau
authors.forename: J D
authors.initials: JD
authors.lastname: Veldhuis
mesh_terms: D005260:Female; D005640:Follicle Stimulating Hormone / Q000097:blood; D007987:Gonadotropin-Releasing Hormone / Q000008:administration & dosage / Q000276:immunology / Q000494:pharmacology / Q000031:analogs & derivatives; D006801:Humans; D007700:Kinetics; D007986:Luteinizing Hormone / Q000097:blood; D008593:Menopause / Q000097:blood*; D008875:Middle Aged; D012882:Skin Tests
chemical_list: C055688:LHRH, Ac-2-Nal(1)-4-Cl-Phe(2)-3-Pal(3)-Arg(5)-4-methoxybenzoyl-2-ABA(6)-Ala(10)-; D007987:Gonadotropin-Releasing Hormone; D007986:Luteinizing Hormone; D005640:Follicle Stimulating Hormone