Suppression and recovery of LH secretion by a potent and selective GnRH-receptor antagonist peptide in healthy early follicular-phase women are mediated via selective control of LH secretory burst mass

Summary aim  GnRH antagonists are competitive inhibitors of GnRH receptors. Their administration induces prompt suppression of the gonadal axis. In animals, GnRH antagonists upregulate the activity of GnRH‐secreting neurones, which could cause gonadotrophin rebound following inhibition. The aim of t...

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Bibliographic Details
Published in:Clinical endocrinology (Oxford) 2003-10, Vol.59 (4), p.526-532
Main Authors: Gianotti, L., Veldhuis, J. D., Destefanis, S., Lanfranco, F., Ramunni, J., Arvat, E., Marzetto, M., Boutignon, F., Deghenghi, R., Ghigo, E.
Format: Article
Language:English
Subjects:
Adult
Biological and medical sciences
Endocrinopathies
Estradiol - blood
Female
Follicle Stimulating Hormone - blood
Follicle Stimulating Hormone - metabolism
Follicular Phase - physiology
Fundamental and applied biological sciences. Psychology
Hormone Antagonists - pharmacology
Humans
Injections, Subcutaneous
Luteinizing Hormone - blood
Luteinizing Hormone - metabolism
Medical sciences
Oligopeptides - pharmacology
Ovary - drug effects
Radioimmunoassay - methods
Receptors, LHRH - antagonists & inhibitors
Secretory Rate - drug effects
Time Factors
Vertebrates: endocrinology
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Summary:Summary aim  GnRH antagonists are competitive inhibitors of GnRH receptors. Their administration induces prompt suppression of the gonadal axis. In animals, GnRH antagonists upregulate the activity of GnRH‐secreting neurones, which could cause gonadotrophin rebound following inhibition. The aim of this study was to evaluate the effects of a potent GnRH antagonist, Teverelix (TEV), on the gonadal axis in healthy young women. subjects and measurements  In nine women [20–35 years old, body mass index (BMI) 19–25 kg/m2] in the early follicular phase, serum LH and FSH levels were evaluated every 10 min from 08·00 to 12·00 h before, and 24 h and 96 h after TEV injection (2·5 mg in 1 ml subcutaneusly on day 0). Serum gonadotrophin and oestradiol levels were also evaluated at baseline and at 6, 8, 12, 48, 72 h after TEV. results  The antagonist reduced both serum LH and FSH concentrations; LH levels were significantly and promptly reduced at +6 h (nadir at +8 h) until +48 h and recovered at +72 h, while FSH levels were reduced (P 
ISSN:0300-0664
1365-2265
DOI:10.1046/j.1365-2265.2003.01882.x