Increased potency and sustained suppressive actions of a new gonadotropin-releasing hormone (GnRH) antagonist peptide in man.
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.
Urban
R J
RJ
Department of Internal Medicine, University of Virginia School of Medicine, Charlottesville 22908.
Pavlou
S N
SN
Rivier
J E
JE
Vale
W W
WW
Dufau
M L
ML
Veldhuis
J D
JD
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
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