性腺刺激ホルモン放出ホルモンアナログ化合物, GnRHa
WordNet
- of or related to the anus; "anal thermometer"
- a stage in psychosexual development when the childs interest is concentrated on the anal region; fixation at this stage is said to result in orderliness, meanness, stubbornness, compulsiveness, etc. (同)anal retentive
- the secretion of an endocrine gland that is transmitted by the blood to the tissue on which it has a specific effect (同)endocrine, internal_secretion
- hormone secreted by the anterior pituitary gland and placenta; stimulates the gonads and controls reproductive activity (同)gonadotrophin, gonadotropic_hormone, gonadotrophic hormone
PrepTutorEJDIC
- 肛門(こうもん)(anus)の
- ホルモン
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/07/28 15:41:06」(JST)
[Wiki en表示]
A gonadotropin-releasing hormone analogue (GnRH analogue or analog), also known as a luteinizing hormone releasing hormone agonist (LHRH agonist) or LHRH analogue is a synthetic peptide drug modeled after the human hypothalamic gonadotropin-releasing hormone (GnRH). A GnRH analogue is designed to interact with the GnRH receptor and modify the release of pituitary gonadotropins FSH and LH for therapeutic purposes. Shortly after the discovery of GnRH by Nobel laureates Guillemin and Schally researchers tried to modify the GnRH decapeptide with the intent to synthesize stimulating and blocking variants.
Two types of analogues have to be distinguished:
Agonists[edit]
Main article: Gonadotropin-releasing hormone agonist
A gonadotropin-releasing hormone agonist (GnRH agonist) is an analogue that activates the GnRH receptor resulting in increased secretion of FSH and LH. Initially it was thought that agonists could be used as potent and prolonged stimulators of pituitary gonadotropin release, but it was soon recognized that 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.
Antagonists[edit]
Main article: Gonadotropin-releasing hormone antagonist
A gonadotropin-releasing hormone antagonist (GnRH antagonist) is an analogue that blocks the GnRH receptor resulting in an immediate drop in gonadotropin (FSH, LH) secretion. The GnRH antagonist is primarily used in IVF treatments to block natural ovulation.
All GnRH analogues are contraindicated in pregnancy (pregnancy category X).
References[edit]
- Speroff L, Glass RH, Kase NG. Clinical Gynecologic Endocrinology and Infertility. Fifth Edition. Willimas 7 Wilkins, Baltimore. 1994. Pages 160-161.
- History of GnRH agonist and antagonist development
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Gonadotropins and GnRH (G03G)
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Gonadotropin
preparations |
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Agonists
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- Menotropin
- Urofollitropin
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Antigonadotropins
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- Sex steroids (via negative feedback): Androgens (e.g., testosterone, oxandrolone, etc)
- Estrogens (e.g., estradiol, ethinyl estradiol, etc)
- Progestogens (e.g., progesterone, medroxyprogesterone acetate, etc)
- Steroid synthesis inhibitors: Danazol
- Gestrinone
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| GnRH analogues |
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Agonists
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- Avorelin
- Buserelin
- Deslorelin
- Gonadorelin
- Goserelin
- Histrelin
- Leuprorelin
- Lutrelin
- Nafarelin
- Peforelin
- Triptorelin
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Antagonists
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- Abarelix
- Cetrorelix
- Degarelix
- Detirelix
- Ganirelix
- Iturelix
- Ozarelix
- Prazarelix
- Ramorelix
- Teverelix
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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UpToDate Contents
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English Journal
- Membrane progestin receptor alpha mediates progestin-induced sperm hypermotility and increased fertilization success in southern flounder (Paralichthys lethostigma).
- Tan W1, Aizen J1, Thomas P2.
- General and comparative endocrinology.Gen Comp Endocrinol.2014 May 1;200:18-26. doi: 10.1016/j.ygcen.2014.02.003. Epub 2014 Feb 11.
- Progestin hormones stimulate sperm motility in teleosts but their mechanisms of action remain unclear. Preliminary results suggest that progestin upregulation of sperm motility in southern flounder and several other marine species is mediated through a sperm membrane progestin receptor with the char
- PMID 24530629
- Clinical management of youth with gender dysphoria in Vancouver.
- Khatchadourian K1, Amed S2, Metzger DL2.
- The Journal of pediatrics.J Pediatr.2014 Apr;164(4):906-11. doi: 10.1016/j.jpeds.2013.10.068. Epub 2013 Dec 5.
- OBJECTIVE: To describe patient characteristics at presentation, treatment, and response to treatment in youth with gender dysphoria.STUDY DESIGN: A retrospective chart review of 84 youth with a diagnosis of gender dysphoria seen at BC Children's Hospital from 1998-2011.RESULTS: Of the 84 patients, 4
- PMID 24315505
- Arterial hypertension during treatment with triptorelin in a child with Williams-Beuren syndrome.
- Siomou E1, Kosmeri C, Pavlou M, Vlahos AP, Argyropoulou MI, Siamopoulou A.
- Pediatric nephrology (Berlin, Germany).Pediatr Nephrol.2014 Mar 7. [Epub ahead of print]
- BACKGROUND: Arterial hypertension (AHT) is a common finding in children with Williams-Beuren syndrome (WBS). Although cardiovascular and renal abnormalities can explain the AHT in some patients with WBS, its etiology is not fully understood and most cases are considered idiopathic.CASE-DIAGNOSIS/TRE
- PMID 24604705
Japanese Journal
- Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
- Misu Ryosuke,Noguchi Taro,Ohno Hiroaki,Oishi Shinya,Fujii Nobutaka
- Bioorganic & medicinal chemistry 21(8), 2413-2417, 2013-04-15
- … Neurokinin B (NKB) is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R). … The corresponding substitutions to NKB provided an NK3R selective analog. …
- NAID 120005244454
- Differential Effects of Continuous Exposure to the Investigational Metastin/Kisspeptin Analog TAK-683 on Pulsatile and Surge Mode Secretion of Luteinizing Hormone in Ovariectomized Goats
- , , [他], , , , , , ,
- Journal of Reproduction and Development 59(6), 563-568, 2013
- … The aim of the present study was to determine if the estradiol-induced luteinizing hormone (LH) surge is influenced by the constant exposure to TAK-683, an investigational metastin/kisspeptin analog, that had been established to depress the pulsatile gonadotropin-releasing hormone (GnRH) and LH secretion in goats. …
- NAID 130003361063
- Combined Treatment with Gonadotropin-releasing Hormone Analog and Anabolic Steroid Hormone Increased Pubertal Height Gain and Adult Height in Boys with Early Puberty for Height
- TANAKA Toshiaki,NAIKI Yasuhiro,HORIKAWA Reiko
- Clinical pediatric endocrinology 21(2), 35-43, 2012-04-01
- NAID 10031199640
Related Links
- 1. Endocrinology. 2005 Sep;146(9):4105-16. Epub 2005 Jun 2. Gonadotropin-releasing hormone I analog acts as an antiapoptotic factor in mouse blastocysts. Kawamura K, Fukuda J, Kumagai J, Shimizu Y, Kodama H ...
- 性腺刺激ホルモン放出ホルモンアナログ療法とは性腺刺激ホルモン放出ホルモンを化学的に修飾して作成された性腺刺激ホルモン放出ホルモンアナログを使用して実行される治療法の事になります。
★リンクテーブル★
[★]
- 英
- gonadotropin-releasing hormone analog GnRHa
- 同
- GnRHアナログ GnRH analog
- 関
- 性腺刺激ホルモン放出ホルモン誘導体、性腺刺激ホルモン放出ホルモン拮抗物
[★]
性腺刺激ホルモン放出ホルモンアナログ化合物 gonadotropin-releasing hormone analog
[★]
- 関
- analogue、derivate、derivative、relative
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[★]
- 関
- analyse、analyses、analysis、analytical、analyze、ani、anus、assay、dissect
[★]
性腺刺激ホルモン