Abstract
Following elucidation of the structure of gonadotropin-releasing hormones (GnRH) by the laboratories of Schally [1] and Guilleman [2] in 1971, hundreds of analogs, both agonists and antagonists of GnRH, were synthesized and tested. Early success in increasing the potency of agonists and recognition of the ability of GnRH agonists paradoxically to inhibit the pituitary-gonadal axis quickly brought GnRH agonists to the forefront of investigation. It is now known that chronic administration of GnRH agonists effectively inhibits the reproductive/ endocrine systems and is useful in the treatment of conditions such as precocious puberty, prostatic carcinoma and uterine fibroids.
This is a preview of subscription content, log in via an institution to check access.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
Matsuo H, Balea Y, Nair RM, Arimura A, Schally AV (1971) Structure of the porcine LH- and FSH-releasing hormone. I. The proposed amino acid sequence. Biochem Bio- phys Res Commun 43:1334
Burgus R, Butcher M, Amoss M, Ling N, Monahan MW, Rivier J, Fellows R, Black- well R, Yale W, Guilleman R (1972) Primary structure of the ovine hypothalamic luteinizing hormone releasing factor (LRF). Proc Natl Acad Sci USA 69:278
Karten MJ, Rivier JE (1986) Gonadotropin-releasing hormone analog design, rationale and perspective. Endocr Rev 7(1):44
Rivier J, Rivier C, Perrin M, Porter J, Vale W (1984) LHRH analogs as antiovulatory agents. In: Vickery BH, Nestor JJ Jr, Hafez ESE (eds) LHRH and its analogs. MTP, Boston, p 11
Nekola MV, Coy DH (1984) LHRH antagonists in females. In: Vickery BH, Nestor JJ Jr, Hafez ESE (eds) LHRH and its analogs. MTP, Boston, p 125
Schmidt F, Sundaram K, Thau RB, Bardin CW (1984) [Ac-D-Nal(2)1, 4FD-Phe2, D- Trp3D-Arg6]-LHRH, a potent antagonist of LHRH, produces transient edema and behavioral changes in rats. Contraception 29:283
Phillips A, Hahn DW, Capetola RJ, McGuire JL (1986) The antiovulatory and anaphylactoid activities of two potent LHRH antagonists. Pharmacologist 28 Abs:#689
Hahn DW, McGuire JL, Vale WW, Rivier J (1985) Reproductive/endocrine and anaphylactoid properties of an LHRH antagonist, ORF 18260 [Ac- DNAL1(2), 4FDPhe2, D-Trp3, D-Arg6]-GnRH. Life Sci 37:505
Schally AV, Arimura A, Coy DH (1980) Recent approaches to fertility control based on derivatives of LH-RH. Vitam Horm 38:257
Kenigsberg D, Littman BA, Hodgen GD (1984) Medical hypophysectomy: I. Dose-response using a gonadotropin-releasing hormone antagonist. Fertil Steril 42:112
Schriock ED, Monroe SE, Martin MC, Henzel MR, Jaffe RB (1985) Effect on corpus luteum function of luteal phase administration of a potent gonadotropin-releasing hormone analog (nafareline). Fertil Steril 43:844
Kenigsberg D, Hodgen GD (1986) Ovulation-inhibition by administration of weekly gonadotropin-releasing hormone antagonist. J Clin Endocrinol Metab 62:734
Werlin LB, Hodgen GD (1983) Gonadotropin-releasing hormone agonist suppresses ovulation, menses and endometriosis in monkeys: an individualized intermittent regimen. J Clin Endocrinol Metab 56:844
Kenigsberg D, Littman BA, Hodgen GD (1984) Medical hypophysectomy: I. Dose-response using a gonadotropin-releasing hormone antagonist. Fertil Steril 42:112
Goodman AL, Hodgen GD (1979) Between ovary interaction in the regulation of follicle’s growth, corpus luteum function, and gonadotropin secretion in the primary ovarian cycle. I. Effects of follicle cautery and hemiovariectomy during the follicular phase in cynomolgus monkeys. Endocrinology 104:1304
diZerega GS, Nixon WE, Hodgen GD (1980) Intercycle serum FSH elevations: significance in recruitment and selection of the dominant follicle and assessment of corpus luteum normalcy. J Clin Endocrinol Metab 50:1046
Nilsson L, Wikland M, Hamberg L (1982) Recruitment of an ovulatory follicle in the human following follicle-ectomy and luteectomy. Fertil Steril 37:30
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1988 Springer-Verlag Berlin Heidelberg
About this paper
Cite this paper
Hahn, D.W. et al. (1988). Contraceptive Potential of GnRH Antagonists. In: Runnebaum, B., Rabe, T., Kiesel, L. (eds) Female Contraception. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-73790-9_16
Download citation
DOI: https://doi.org/10.1007/978-3-642-73790-9_16
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-642-73792-3
Online ISBN: 978-3-642-73790-9
eBook Packages: Springer Book Archive