TY - JOUR
T1 - Suppressive actions of a gonadotropin-releasing hormone antagonist on luteinizing hormone, follicle-stimulating hormone, and prolactin release in estrogen-deficient postmenopausal women
AU - Urban, Randall J.
AU - Pavlou, Spyros N.
AU - Rivier, Jean E.
AU - Vale, Wylie W.
AU - Dufau, Maria L.
AU - Veldhuis, Johannes D.
N1 - Funding Information:
Supported in part by National Institutes of Health (NIH) Grant no. RR 00847 to the Clinical Research Center of the University of Virginia, Research Career Development Award No. 1 K04 HD 00634 (j. D. V.), National Institutes of Health Clinical Associate Physician Award no. 3 MOl RR00847-1491 (R.]. U.), Biomed-icalResearch Support Grant No. 5-S07-RR 05431-26 (R..f. U.), Diabetes and Research Training Center Grant no. 5 P60 AM 22125-05, National Institutes of Health-supported Clinfo Data Reduction Systems, and National Institutes of Health Grant no. HD 13527 (j. R., W. V.).
PY - 1990/5
Y1 - 1990/5
N2 - We investigated time- and dose-dependent actions of a gonadotropin-releasing hormone antagonist, the "Nal-Glu" peptide [Ac-D2Nal1, 4ClDPhe2, D3Pal3, Arg5, DGlu6(AA), DAla10], in nine healthy estrogen-withdrawn postmenopausal women. Gonadotropin-releasing hormone antagonist was administered subcutaneously at doses of 10, 30, 100, and 300 μg/kg. Suppression of immunoactive luteinizing hormone concentrations was achieved with a 30 μg/kg dose of antagonist. Suppression of immunoactive follicle-stimulating hormone levels was less (40%) even at the highest antagonist dose (300 μg/kg). Bioactive luteinizing hormone concentrations also significantly decreased (60%) at the two antagonist doses tested (30 and 300 μg/kg). However, the lower antagonist dose showed an "escape" of bioactive luteinizing hormone values after 18 hours. No suppressive effects of the antagonist on prolactin secretion occurred at any dose tested. We conclude that this gonadotropin-releasing hormone antagonist can achieve effective, potent, and long-lasting suppression of pituitary secretion of biologically active luteinizing hormone at higher doses, but secretion of biologically active luteinizing hormone may escape" at lower doses.
AB - We investigated time- and dose-dependent actions of a gonadotropin-releasing hormone antagonist, the "Nal-Glu" peptide [Ac-D2Nal1, 4ClDPhe2, D3Pal3, Arg5, DGlu6(AA), DAla10], in nine healthy estrogen-withdrawn postmenopausal women. Gonadotropin-releasing hormone antagonist was administered subcutaneously at doses of 10, 30, 100, and 300 μg/kg. Suppression of immunoactive luteinizing hormone concentrations was achieved with a 30 μg/kg dose of antagonist. Suppression of immunoactive follicle-stimulating hormone levels was less (40%) even at the highest antagonist dose (300 μg/kg). Bioactive luteinizing hormone concentrations also significantly decreased (60%) at the two antagonist doses tested (30 and 300 μg/kg). However, the lower antagonist dose showed an "escape" of bioactive luteinizing hormone values after 18 hours. No suppressive effects of the antagonist on prolactin secretion occurred at any dose tested. We conclude that this gonadotropin-releasing hormone antagonist can achieve effective, potent, and long-lasting suppression of pituitary secretion of biologically active luteinizing hormone at higher doses, but secretion of biologically active luteinizing hormone may escape" at lower doses.
KW - Gonadotropin-releasing hormone antagonist
KW - bioactive luteinizing hormone
KW - gonadotropin secretion
KW - gonadotropin-releasing hormone
KW - prolactin secretion
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U2 - 10.1016/0002-9378(90)90030-B
DO - 10.1016/0002-9378(90)90030-B
M3 - Article
C2 - 2111095
AN - SCOPUS:0025367725
SN - 0002-9378
VL - 162
SP - 1255
EP - 1260
JO - American journal of obstetrics and gynecology
JF - American journal of obstetrics and gynecology
IS - 5
ER -