Suppressive actions of a gonadotropin-releasing hormone antagonist on luteinizing hormone, follicle-stimulating hormone, and prolactin release in estrogen-deficient postmenopausal women

Randall Urban, Spyros N. Pavlou, Jean E. Rivier, Wylie W. Vale, Maria L. Dufau, Johannes D. Veldhuis

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

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antagonist, the "Nal-Glu" peptide [Ac-D2Nal1, 4ClDPhe2, D3Pal3, Arg5, DGlu6(AA), DAla10], in nine healthy estrogen-withdrawn postmenopausal women.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.

Original languageEnglish (US)
Pages (from-to)1255-1260
Number of pages6
JournalAmerican Journal of Obstetrics and Gynecology
Volume162
Issue number5
DOIs
StatePublished - 1990
Externally publishedYes

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Hormone Antagonists
Follicle Stimulating Hormone
Luteinizing Hormone
Gonadotropin-Releasing Hormone
Prolactin
Estrogens
Peptides

Keywords

  • bioactive luteinizing hormone
  • gonadotropin secretion
  • gonadotropin-releasing hormone
  • Gonadotropin-releasing hormone antagonist
  • prolactin secretion

ASJC Scopus subject areas

  • Medicine(all)
  • Obstetrics and Gynecology

Cite this

Suppressive actions of a gonadotropin-releasing hormone antagonist on luteinizing hormone, follicle-stimulating hormone, and prolactin release in estrogen-deficient postmenopausal women. / Urban, Randall; Pavlou, Spyros N.; Rivier, Jean E.; Vale, Wylie W.; Dufau, Maria L.; Veldhuis, Johannes D.

In: American Journal of Obstetrics and Gynecology, Vol. 162, No. 5, 1990, p. 1255-1260.

Research output: Contribution to journalArticle

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abstract = "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.",
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