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

Clinical Endocrinology

Volumn 59, Issue 4, 2003, Pages 526-532

  Gianotti, L ^a   Veldhuis, J D ^b   Destefanis, S ^a   Lanfranco, F ^a   Ramunni, J ^a   Arvat, E ^a   Marzetto, M ^c   Boutignon, F ^c   Deghenghi, R ^c   Ghigo, Ezio ^a,d  

^a UNIVERSITY OF TURIN   (Italy)

^b MAYO CLINIC   (United States)

^c Ardana   (France)

^d Division of Endocrinolgy   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

ESTRADIOL; FOLLITROPIN; GONADORELIN ANTAGONIST; LUTEINIZING HORMONE; TEVERELIX;

ADULT; ARTICLE; BODY MASS; CONTROLLED STUDY; ESTRADIOL BLOOD LEVEL; EVALUATION; FEMALE; FOLLICULAR PHASE; FOLLITROPIN BLOOD LEVEL; FOLLITROPIN RELEASE; GONAD; HUMAN; HUMAN EXPERIMENT; LUTEINIZING HORMONE BLOOD LEVEL; LUTEINIZING HORMONE RELEASE; NORMAL HUMAN; PRIORITY JOURNAL;

ADULT; ESTRADIOL; FEMALE; FOLLICLE STIMULATING HORMONE; FOLLICULAR PHASE; HORMONE ANTAGONISTS; HUMANS; INJECTIONS, SUBCUTANEOUS; LUTEINIZING HORMONE; OLIGOPEPTIDES; OVARY; RADIOIMMUNOASSAY; RECEPTORS, LHRH; SECRETORY RATE; TIME FACTORS;

EID: 0141839674     PISSN: 03000664     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2265.2003.01882.x     Document Type: Article

References (36)

1. Behre, H.M., Klein, B., Steinmeyer, E., McGregor, G., Voigt, K. & Nieschlag, E. (1992) Effective suppression of luteinizing hormone and testosterone by single doses of the new gonadotrophin-releasing hormone antagonist Cetrorelix (SB-75) in normal men. Journal of Clinical Endocrinology and Metabolism, 75, 393-398.
2. Blache, D., Chagas, L.M., Carty, A., Deghenghi, R., Delaleu, B., Blackberry, M.A. & Martin, G.B. (1997) GnRH secretion into CSF in rams treated with a GnRH antagonist. Journal of Neuroendocrinology, 9, 887-892.
3. Cho, S., Han, J., Sun, W., Choi, D., Bang Kwon, H., Jarry, H., Wuttke, W. & Kim, K. (1997) Evidence for autocrine inhibition of gonadotrophin-releasing hormone (GnRH) gene transcription by GnRH in hypothalamic GT1-1 neuronal cells. Molecular Brain Research, 50, 51-58.
4. Comaru-Schally, A.M., Brannan, W., Schally, A.V., Colcolough, M. & Monga, M. (1998) Efficacy and safety of luteinizing hormone-releasing antagonist cetrorelix in the treatment of symptomatic benign prostatic hyperplasia. Journal of Clinical Endocrinology and Metabolism, 83, 3826-3831.
5. Conn, P.M. & Crowley, W.F. (1994) Gonadotrophin-releasing hormone and its analogs. Annals of Review of Medicine, 49, 391-405.
6. Couzinet, B., Lahlou, N., Thomas, G., Thalabard, J.C., Bouchard, P., Roger, M. & Schaison, G. (1991) Effects of gonadotrophin releasing hormone antagonist and agonist on the pulsatile release of gonaotrophins and alpha subunit in postmenopausal women. Clinical Endocrinology, 34, 447-483.
7. Davis, M.R., Veldhuis, J.D., Rogol, A.D., Dufau, M.L. & Catt, K.J. (1987) Sustained inhibitory actions of a potent antagonist of gonadotrophin-releasing hormone in postmenopausal women. Journal of Clinical Endocrinology and Metabolism, 64, 1268-1274.
8. Deghenghi, R., Boutignon, F., Wuethrich, P. & Lenaerts, V. (1993) Antarelix (EP24332) a novel water-soluble LHRH antagonist. Biomedical Pharmacotherapy, 47, 107-110.
9. Duijkers, I.J., Klipping, C., Willemsen, W.N., Krone, D., Schneider, E., Niebch, G. & Hermann, R. (1998) Single and multiple dose-pharmacokinetics and pharmacodynamics of the gonaotrophin-releasing hormone antagonist cetrorelix in healthy female volunteers. Human Reproduction, 13, 2392-2398.
10. Erb, K., Pechstein, B., Schueler, A., Engel, J. & Hermann, R. (2000) Pituitary and gonadal endocrine effects and pharmacokinetics of the novel luteinizing homone-releasing hormone antagonist teverelix in healthy man, a first dose, in human study. Clinical Pharmacological Therapy, 67, 660-669.
11. Erb, K., Klipping, C., Duijkers, I., Pechstein, B., Achueler, A. & Hermann, R. (2001) Pharmacodynamic effects and plasma pharmacokinetics of single doses of cetrorelix acetate in healthy premenopausal women. Fertility Sterility, 75, 316-323.
12. Fox, C.R., Mulligan, T., Iranmanesh, A. & Veldhuis, J.D. (2002) A paradigm of GnRH-receptor antagonist administration followed by pulsatile I.V. recombinant human (RH) LH demonstrates equivalent acute Leydig-cell steroidogenic function in younger and older men. 84th Annual Meeting of the Endocrine Society, San Francisco, California, June 19-22, 2002, p. 476.
13. Gordon, K., Scott, R.T., Williams, R.F., Danforth, D.R., Loozen, H.J., Kloosterboer, H.J. & Hodegen, G.D. (1994) In vivo effects of a potent GnRH antagonist ORG 30850: physiologic evidence that down-regulation of GnRH receptors does not occur. Journal of Society of Gynecological Investigations, 1, 290-296.
14. Halmos, G. & Schally, A.V. (2002) Changes in subcellular distribution of pituitary receptors for luteinizing hormone-releasing hormone (LH-RH) after treatment with the LH-RH antagonist cetrorelix. Proceedings of the National Academy of Sciences of the USA, 22, 961-965.
15. Halmos, G., Schally, A.W., Pinski, J., Vadillo-Buenfil, M. & Groot, K. (1996) Downregulation of pituitary receptors for luteinizing hormone-releasing hormone (LHRH) in rats by LH-RH antagonist Cetrorelix. Medical Sciences, 93, 2398-2402.
16. Han, Y.G., Kang, S., Seong, J.Y., Geum, D., Suh, Y.H. & Kim, K. (1999) Negative regulation of gonadotrophin releasing hormone and gonadotrophin-releasing hormone receptor gene expression by a gonadotrophin-releasing homone agonist in the rat hypothalamus. Journal of Endocrinology, 11, 195-201.
17. Haviv, F., Bush, E.N., Knittle, J. & Greer, J. (1998) LHRH antagonists. Pharmacology Biotechnology, 11, 131-149.
18. Huirne, J.A.F. & Lambalk, C.B. (2001) Gonadotrophin-releasing hormone receptor antagonists. Lancet, 358, 1793-1803.
19. Kostanski, J.W., Dani, B.A., Schrier, B. & DeLuca, P.P. (2000) Effect of the concurrent LHRH antagonist administration with a LHRH superagonist in rats. Pharmacy Research, 17, 445-450.
20. Li, S. & Pelletier, G. (1994) Involvement of an autoregulatory mechanism for the regulation of gonadotrophin-releasing hormone (GnRH) gene expression in neurons in the rat preoptic area. Neuroscience Letters, 174, 61-63.
21. McCartney, C.R., Bellows, A.B., Hu, Y. et al. (2002) Heightened secretion of 17-hydroxyprogesterone in patients with polycystic ovary syndrome following sequential blockade of endogenous LH release and pulsatile IV infusions of exogenous (recombinant human) LH. 84th Annual Meeting of the Endocrine Society, San Francisco, California, June 19-22, 2002, p. 463.
22. Ortmann, O. & Diedrich, K. (1999) Pituitary and extrapituitary actions of gonadotrophin-releasing hormone and its analogues. Human Reproduction, 14, 194-206.
23. Pavlou, S.N., Veldhuis, J.D., Lindner, J., Souza, K.H., Urban, R.J., Rivier, J.E., Vale, W.W. & Stallard, D.J. (1990) Persistence of concordant LH, testosterone and alpha subunit pulses following LHRH antagonist administration in normal men. Journal of Clinical Endocrinology and Metabolism, 70, 472-1478.
24. Reissman, T., Felberbaum, R., Diedrich, K., Engel, J. & Comaru Schally, A.V. (1995) Development and applications of luteinizing hormone-releasing hormone antagonists in the treatment of infertility: on overview. Human Reproduction, 10, 1974-1981.
25. Reissman, T., Schally, A.V., Bouchard, P., Riethmüller, H. & Hengel, J. (2000) The LHRH antagonist Cetrorelix: a review. Human Reproduction Update, 6, 322-331.
26. Roth, C., Leonhardt, S., Seidel, C., Lufth, H., Wuttke, W. & Jarry, H. (2000) Comparative analysis of different puberty inhibiting mechanisms of two GnRH agonists and the GnRH antagonist cetrorelix using a female rat model. Pediatrics Research, 48, 468-474.
27. Sarkar, D.K. (1987) In vivo secretion of LHRH in ovariectomized rats is regulated by a possible autofeedback mechanism. Neuroendocrinology, 45, 510-513.
28. Schally, A.V. (1999) LHRH analogues: their impact on the control of tumorigenesis. Peptides, 20, 1247-1262.
29. Schvartz, I. & Hazum, E. (1987) Internalization and recycling of receptor-bound gonadotrophin-releasing hormone agonist in pituitary gonadotropes. Journal of Biology Chemistry, 262, 17046-17050.
30. Stojilkovic, S.S., Rojas, E., Stutzin, A., Izumi, S. & Catt, K.J. (1989) Desensitization of pituitary gonadotrophin secretion by agonist-induced inactivation of voltage-sensitive calcium channels. Journal of Biological Chemistry, 264, 10939-10942.
31. Stojilkovic, S.S., Reinhart, J. & Catt, K.J. (1994) Gonadotrophin-releasing hormone receptors: structure and signal transduction pathways. Endocrine Review, 15, 426-499.
32. Urban, R.J., Pavlou, S.N., Rivier, J.E., Vale, W.W., Dufau, M.L. & Veldhuis, J.D. (1990) Suppressive actions of a gonadotrophin-releasing hormone (GnRH) antagonist on LH, FSH, and prolactin release in estrogen-deficient postmenopausal women. American Journal of Obstetrics and Gynecology, 162, 1255-1260.
33. Valenca, M.M., Johnston, C.A., Ching, M. & Negro Vilar, A. (1987) Evidence for a negative ultrashort loop feedback mechanism operating on the luteinizing hormone-releasing hormone neural system. Endocrinology, 121, 2256-2259.
34. Veldhuis, J.D., Carlson, M.L. & Johnson, M.L. (1987) The pituitary gland secretes in bursts: appraising the nature of glandular secretory impulses by simultaneous multiple-parameter deconvolution of plasma hormone concentrations. Proceedings of the National Academy of Sciences of the USA, 84, 7686-7690.
35. Veldhuis, J.D., Johnson, M.L., Veldhuis, O.L., Straume, M. & Pincus, S.M. (2001a) Impact of pulsatility on the ensemble orderliness (approximate entropy) of neurohormone secretion. American Journal of Physiology: Regulated Integrated Computer Physiology, 281, R1975-R1985.
36. Veldhuis, J.D., Straume, M., Iranmanesh, A., Mulligan, T., Jaffe, C.A., Barkan, A., Johnson, M.L. & Pincus, S.M. (2001b) Secretory process regularity monitors neuroendocrine feedback and feedforward signaling strength in humans. American Journal of Physiology, 280, R721-R729.