Shortly after the discovery of GnRH by Nobel laureatesGuillemin and Schally, researchers tried to modify the GnRH decapeptide with the intent to create analogues that could activate or block the receptor. Subsequent to the development and introduction of GnRH analogues, non-peptide or small-molecule GnRH modulators were developed and introduced.
A gonadotropin-releasing hormone agonist (GnRH agonist) is a GnRH modulator that activates the GnRH receptor resulting in increased secretion of FSH and LH. Initially it was thought that GnRH agonists could be used as potent and prolonged stimulators of pituitary gonadotropin release, but it was soon recognized that GnRH agonists, after their initial stimulating action – termed a "flare" effect – eventually caused a paradoxical and sustained drop in gonadotropin secretion. This second effect was termed "downregulation" and can be observed after about 10 days. While this phase is reversible upon stopping the medication, it can be maintained when GnRH agonists use is continued for a long time. GnRH agonists can also be administered in a pulsatile manner through the use of a pump to produce a long-term stimulation of gonadotropin secretion, for instance to induce puberty.
A gonadotropin-releasing hormone antagonist (GnRH antagonist) is a GnRH modulator that blocks the GnRH receptor resulting in an immediate drop in gonadotropin (FSH, LH) secretion. GnRH antagonists are primarily used in IVF treatments to block natural ovulation.
^Riggs MM, Bennetts M, van der Graaf PH, Martin SW (2012). "Integrated pharmacometrics and systems pharmacology model-based analyses to guide GnRH receptor modulator development for management of endometriosis". CPT: Pharmacometrics & Systems Pharmacology. 1 (9): 1–9. doi:10.1038/psp.2012.10. PMC3606940. PMID 23887363.
^Catherine Racowsky, Peter N. Schlegel, Bart C.J.M. Fauser, Douglas Carrell (7 June 2011). Biennial Review of Infertility. Springer Science & Business Media. pp. 80–. ISBN978-1-4419-8456-2.
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May 02, 2024
gonadotropin, releasing, hormone, modulator, gnrh, modulator, gnrh, receptor, modulator, also, known, lhrh, modulator, lhrh, receptor, modulator, type, medication, which, modulates, gnrh, receptor, biological, target, hypothalamic, hormone, gonadotropin, relea. A GnRH modulator or GnRH receptor modulator also known as an LHRH modulator or LHRH receptor modulator is a type of medication which modulates the GnRH receptor the biological target of the hypothalamic hormone gonadotropin releasing hormone GnRH also known as luteinizing releasing hormone or LHRH 1 2 They include GnRH agonists and GnRH antagonists These medications may be GnRH analogues like leuprorelin and cetrorelix peptides that are structurally related to GnRH or small molecules like elagolix and relugolix which are structurally distinct from and unrelated to GnRH analogues Gonadotropin releasing hormone modulatorDrug classLeuprorelin a GnRH agonist and GnRH analogue and a prototypical GnRH modulator Class identifiersSynonymsGnRH receptor modulator GnRH analogue GnRH agonist GnRH antagonist GnRH blocker LHRH modulator LHRH receptor modulator LHRH analogue LHRH agonist LHRH antagonist LHRH blockerUseInfertility prostate cancer precocious puberty breast cancer endometriosis uterine fibroids transgender peopleBiological targetGnRH receptorChemical classPeptide small molecule non peptide Legal statusIn Wikidata GnRH modulators affect the secretion of the gonadotropins luteinizing hormone LH and follicle stimulating hormone FSH which in turn affects the gonads influencing their function and hence fertility as well as the production of sex steroids including that of estradiol and progesterone in women and of testosterone in men As such GnRH modulators can also be described as progonadotropic or antigonadotropic depending on whether they act to increase or decrease gonadotropins Shortly after the discovery of GnRH by Nobel laureates Guillemin and Schally researchers tried to modify the GnRH decapeptide with the intent to create analogues that could activate or block the receptor Subsequent to the development and introduction of GnRH analogues non peptide or small molecule GnRH modulators were developed and introduced All GnRH modulators are contraindicated in pregnancy pregnancy category X Contents 1 GnRH agonists 1 1 Peptides analogues 2 GnRH antagonists 2 1 Peptides analogues 2 2 Non peptides small molecules 3 See also 4 References 5 External linksGnRH agonists editMain article Gonadotropin releasing hormone agonist A gonadotropin releasing hormone agonist GnRH agonist is a GnRH modulator that activates the GnRH receptor resulting in increased secretion of FSH and LH Initially it was thought that GnRH agonists could be used as potent and prolonged stimulators of pituitary gonadotropin release but it was soon recognized that GnRH agonists after their initial stimulating action termed a flare effect eventually caused a paradoxical and sustained drop in gonadotropin secretion This second effect was termed downregulation and can be observed after about 10 days While this phase is reversible upon stopping the medication it can be maintained when GnRH agonists use is continued for a long time GnRH agonists can also be administered in a pulsatile manner through the use of a pump to produce a long term stimulation of gonadotropin secretion for instance to induce puberty Peptides analogues edit Buserelin Deslorelin Fertirelin Gonadorelin Goserelin Histrelin Lecirelin Leuprorelin Nafarelin Peforelin TriptorelinGnRH antagonists editMain article Gonadotropin releasing hormone antagonist A gonadotropin releasing hormone antagonist GnRH antagonist is a GnRH modulator that blocks the GnRH receptor resulting in an immediate drop in gonadotropin FSH LH secretion GnRH antagonists are primarily used in IVF treatments to block natural ovulation Peptides analogues edit Abarelix Cetrorelix Degarelix Ganirelix Non peptides small molecules edit Elagolix Linzagolixa Relugolix a Under development not yet marketed See also editSteroidogenesis inhibitor List of investigational sex hormonal agents GnRH gonadotropinsReferences edit Riggs MM Bennetts M van der Graaf PH Martin SW 2012 Integrated pharmacometrics and systems pharmacology model based analyses to guide GnRH receptor modulator development for management of endometriosis CPT Pharmacometrics amp Systems Pharmacology 1 9 1 9 doi 10 1038 psp 2012 10 PMC 3606940 PMID 23887363 Catherine Racowsky Peter N Schlegel Bart C J M Fauser Douglas Carrell 7 June 2011 Biennial Review of Infertility Springer Science amp Business Media pp 80 ISBN 978 1 4419 8456 2 External links editHistory of GnRH agonist and antagonist development Retrieved from https en wikipedia org w index php title Gonadotropin releasing hormone modulator amp oldid 1215895327, wikipedia, wiki, book, books, library,
