Gonadotropin-releasing hormone modulator

Gonadotropin-releasing hormone modulator
Drug class
Leuprorelin, a GnRH agonist and GnRH analogue and a prototypical GnRH modulator.
Class identifiers
SynonymsGnRH receptor modulator; GnRH analogue; GnRH agonist; GnRH antagonist; GnRH blocker; LHRH modulator; LHRH receptor modulator; LHRH analogue; LHRH agonist; LHRH antagonist; LHRH blocker
UseInfertility; prostate cancer; precocious puberty; breast cancer; endometriosis; uterine fibroids; transgender people
Biological targetGnRH receptor
Chemical classPeptide; small-molecule (non-peptide)
Legal status
In Wikidata

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.

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).

GnRH agonists

Main 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)

GnRH antagonists

Main 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)

Non-peptides (small-molecules)

a = Under development; not yet marketed.

See also

References

  1. ^ 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. PMC 3606940. PMID 23887363.
  2. ^ 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–. ISBN 978-1-4419-8456-2.



Read other articles:

Delusi Cotard

Artikel ini sebatang kara, artinya tidak ada artikel lain yang memiliki pranala balik ke halaman ini.Bantulah menambah pranala ke artikel ini dari artikel yang berhubungan atau coba peralatan pencari pranala.Tag ini diberikan pada Oktober 2022. Delusi CotardAhli saraf Jules Cotard (1840-1889) menggambarkan The Delirium of Negation sebagai penyakit mental dengan tingkat keparahan yang bervariasi.Informasi umumNama lainSindrom Cotard, Sindrom mayat hidupSpesialisasiPsikiatri Delusi Cotard alias...

 

 

Carl von Clausewitz

Prussian general and military theorist (1780–1831) Clausewitz redirects here. For the part of defence of Berlin during World War II, see Operation Clausewitz. For the Paradox computer strategy games engine, see Clausewitz Engine. Carl von ClausewitzCarl von Clausewitz, while in Prussian service, painted by Wilhelm Wach in early 1830s.Birth nameCarl Philipp Gottfried von ClausewitzBorn(1780-07-01)1 July 1780Burg bei Magdeburg, Kingdom of Prussia, Holy Roman EmpireDied16 November 1831(1831-11...

 

 

Religion in Japan

Religious practices in Japan Religious believers in Japan (CIA World Factbook)[3] Shinto   70.5% Buddhism   67.2% Christianity   1.5% Other religions   5.9% Total adherents exceeds 100% because many Japanese people practice both Shinto and Buddhism. Religion in Japan (2018 NHK research)[4] No religion   62% Buddhism   31% Shinto   3% Christianity   1% Others   1% No answer   2% A ritual at the Takachiho-gawara, the sa...

Maharaja Piedmont

Lambang kemaharajaan dan kepangeranan Piedmont. Maharaja, kemudian kepangeranan Piedmont (bahasa Italia: Piemonte, bahasa Prancis: Piémont) aslinya adalah wilayah kadipaten Savoyard oleh karena itu para maharajanya adalah anggota-anggota Cabang Savoy-Achaea dari istana terkemuka tersebut. Gelar tersebut diwariskan oleh cabang-cabang yang lebih tua dari dinasti itu pada tahun 1418, pada saat di mana Savoy ditingkatkan ke status adipati dan Piedmont ke status pangeran. Ketika Istana Savoy dibe...

 

 

Mazmur 119

Mazmur 119Naskah Gulungan Mazmur 11Q5 di antara Naskah Laut Mati memuat salinan sejumlah besar mazmur Alkitab yang diperkirakan dibuat pada abad ke-2 SM.KitabKitab MazmurKategoriKetuvimBagian Alkitab KristenPerjanjian LamaUrutan dalamKitab Kristen19← Mazmur 118 Mazmur 120 → Mazmur 119 (disingkat Maz 119, Mzm 119 atau Mz 119; penomoran Septuaginta: Mazmur 118) adalah sebuah mazmur dalam bagian ke-5 Kitab Mazmur di Alkitab Ibrani dan Perjanjian Lama dalam Alkitab Kristen. Tidak ditu...

 

 

Looney Tunes (video game)

1992 video gameLooney TunesDeveloper(s)SunsoftPublisher(s)SunsoftDirector(s)Akito TakeuchiProducer(s)Kiharu YoshidaProgrammer(s)Michio OkasakaArtist(s)Shigeyuki AsaHiroshi ItoComposer(s)Manami MatsumaeSeriesLooney TunesPlatform(s)Game Boy, Game Boy ColorReleaseGame BoyNA: October 2, 1992[1]JP: December 22, 1992EU: 1992Game Boy ColorNA: September 1999EU: September 1999Genre(s)PlatformerMode(s)Single player Looney Tunes is a platform video game developed and published by Sunsoft release...

Pakistan at the 2006 Asian Games

Sporting event delegationPakistan at the2006 Asian GamesIOC codePAKNOCPakistan Olympic Associationin DohaCompetitors387MedalsRanked 31st Gold 0 Silver 1 Bronze 3 Total 4 Asian Games appearances (overview)195419581962196619701974197819821986199019941998200220062010201420182022 Pakistan competed in the 2006 Asian Games held in Doha, Qatar. Medalists [1] Medal Name Sport Event Date  Silver Muhammad AkramNasir AliBadshah GulWajid AliWaseem SajjadMuhammad ArshadMaqsood AliRahat Maqsoo...

 

 

Ancre

AncreCiri-ciri fisikMuara sungaiSungai SommePanjang38 kmLuas DASDAS: 327 km² Ancre merupakan sebuah sungai di Picardie, Prancis. Bermuara di Miraumont, sebuah desa dekat kota Albert, sungai ini mengalir ke Sungai Somme di Corbie. Sungai tersebut tidak melintasi departemen apapun selain Somme. Lihat pula Pertempuran Dataran Tinggi Ancre (Oktober 1916) Pertempuran Ancre (November 1916) Catatan kaki http://www.geoportail.fr Diarsipkan 2010-12-15 di Wayback Machine. The Ancre at the Sandre datab...

 

 

Denias, Senandung di Atas Awan

Artikel ini tidak memiliki referensi atau sumber tepercaya sehingga isinya tidak bisa dipastikan. Tolong bantu perbaiki artikel ini dengan menambahkan referensi yang layak. Tulisan tanpa sumber dapat dipertanyakan dan dihapus sewaktu-waktu.Cari sumber: Denias, Senandung di Atas Awan – berita · surat kabar · buku · cendekiawan · JSTOR Topik artikel ini mungkin tidak memenuhi kriteria kelayakan umum. Harap penuhi kelayakan artikel dengan: menyertakan sum...

Julie Newmar

Julie NewmarNewmar, 1965LahirJulia Chalene Newmeyer16 Agustus 1933 (umur 90)Los Angeles, California, A.S.PekerjaanAktrispenaripenyanyipebisnispenulisTahun aktif1952–sekarangTinggi5 kaki 11 inci (1,80 m)[1]Suami/istriJ. Holt Smith ​ ​(m. 1977; c. 1984)​Anak1PenghargaanInkpot Award (2014)[2]Situs webjulienewmar.com Julie Newmar (nee Julia Chalene Newmeyer, lahir 16 Agustus 1933) adalah seorang aktris, pe...

 

 

Trikromasi

Tiga pigmen sel kerucut pada mata manusia menyebapkan penglihatan trikromatik. Trikromasi atau trikromatisme adalah keadaan yang membuat mata mampu membedakan tiga kanal warna yang berbeda, atau keadaan adanya tiga jenis sel kerucut yang berbeda pada matanya.[1] Teori trikromatik ini dicetuskan pada abad ke 18 oleh Thomas Young yang mengatakan bahwa penglihatan warna adalah hasil dari tiga jenis sel fotoreseptor yang berbeda. Teori ini dikembangkan oleh Hermann von Helmholtz dengan me...

 

 

Open-design movement

Movement for product development with publicly shared designs RepRap general-purpose 3D printer that not only could be used to make structures and functional components for open-design projects but is an open-source project itself Uzebox is an open-design video game console.[1] Bug Labs open source hardware[2][3] Zoybar open source guitar kit with 3-D printed body[4] The open-design movement involves the development of physical products, machines and systems th...

Denmark–Norway

Political union in Northern Europe between 1524 and 1814 This article is about the former union. For modern bilateral relations, see Denmark–Norway relations. Denmark–NorwayDanmark–Norge (Danish)1524–15331537–1814 Royal Standard of Denmark-Norway(1731–1819) Coat of arms(1699–1814) Motto: Fromhed styrker rigerne (Piety strengthens the realms)[1] Used from 1588–1648Anthem: Kong Christian stod ved højen mastKing Christian stood by the lofty mast Used from ...

 

 

Witwatersrand Gold Rush

Gold rush in Johannesburg, South Africa This article's tone or style may not reflect the encyclopedic tone used on Wikipedia. See Wikipedia's guide to writing better articles for suggestions. (February 2018) (Learn how and when to remove this template message) Witwatersrand Gold RushWitwatersrand Basin and major goldfieldsDate1886LocationWitwatersrand Basin, Johannesburg, South AfricaOutcomeThe largest gold rush ever led to the eventual Boer defeat in the Second Boer War (1899-1902), the loss...

 

 

Elliott W. Sproul

American politician Elliott W. SproulMember of the U.S. House of Representativesfrom Illinois's 3rd districtIn officeMarch 4, 1921 – March 3, 1931Preceded byWilliam Warfield WilsonSucceeded byEdward A. Kelly Personal detailsBorn(1856-12-28)December 28, 1856Apohaqui, Kings County, New Brunswick, CanadaDiedJune 22, 1935(1935-06-22) (aged 78)Chicago, Illinois, U.S.Political partyRepublican Elliott Wilford Sproul (December 28, 1856 – June 22, 1935) was a U.S. Represe...

Шаблон:Мифология

МифологияРитуально-мифологическийкомплекс Система ценностей Сакральное Миф Мономиф Теория основного мифа Ритуал Обряд Праздник Жречество Мифологическое сознание Магическое мышление Низшая мифология Модель мира Цикличность Сотворение мира Мировое яйцо Мифическое �...

 

 

Ilmu formal

Artikel ini bukan mengenai Ilmu budaya. Bagian dari seriIlmu Pengetahuan Formal Logika Matematika Logika matematika Statistika matematika Ilmu komputer teoretis Teori permainan Teori keputusan Ilmu aktuaria Teori informasi Teori sistem FisikalFisika Fisika klasik Fisika modern Fisika terapan Fisika komputasi Fisika atom Fisika nuklir Fisika partikel Fisika eksperimental Fisika teori Fisika benda terkondensasi Mekanika Mekanika klasik Mekanika kuantum Mekanika kontinuum Rheologi Mekanika benda...

 

 

大字 (数字)

この項目には、一部のコンピュータや閲覧ソフトで表示できない文字が含まれています（詳細）。 数字の大字（だいじ）は、漢数字の一種。通常用いる単純な字形の漢数字（小字）の代わりに同じ音の別の漢字を用いるものである。 概要 壱万円日本銀行券（「壱」が大字） 弐千円日本銀行券（「弐」が大字） 漢数字には「一」「二」「三」と続く小字と、「壱」「�...

2022年肯塔基州聯邦參議員選舉

2022年肯塔基州聯邦參議員選舉 ← 2016年 2022年11月8日 (2022-11-08) 2028年 →   获提名人 蘭德·保羅 查爾斯·布克 政党 共和黨 民主党 民選得票 913,326 564,311 得票率 61.8% 38.2% 各縣結果保羅：     50–60%     60–70%     70–80%     80–90%布克：     50–60%     60–70% 选前聯邦參議...

 

 

Paola Taverna

Paola TavernaTaverna a un incontro dell'OSCE nel 2019 Vicepresidente del Movimento 5 Stelle[1]In caricaInizio mandato21 ottobre 2021 PresidenteGiuseppe Conte PredecessoreCarica istituita Vicepresidente del Senato della RepubblicaDurata mandato28 marzo 2018 –12 ottobre 2022 PresidenteMaria Elisabetta Alberti Casellati Senatrice della Repubblica ItalianaDurata mandato15 marzo 2013 –12 ottobre 2022 LegislaturaXVII, XVIII GruppoparlamentareMovimento 5 ...