Endocrinologists at Hospital Bicetre in France studied the mechanisms of action of the 2nd generation gonadotropin releasing hormone (GnRH) antagonist Nal-Glu by administering it to castrated rams to those whose testes had not descended and to intact rams. It caused a significant and precipitous ...
Mechanism of Action of GnRH Antagonists Degarelix and abarelix are gonadotropin-releasing hormone antagonists, they stop secretion ofLH and FSHwith a dramatic reduction of thetestosterone concentration. Indications for GnRH antagonists Abarelix and degarelix are used forhormone therapy of advanced or metasta...
Conn, P. M. (1994). The molecular mechanism of gonadotropin-releasing hormone action in the pituitary. In Knobil, E., and Neill, J. D., et al. (eds.),The Physiology of Reproduction, 2nd ed., Raven Press, New York, pp. 1815–1832. Google Scholar Conn, P. M., Huckle, W. R.,...
GnRH类似物分为GnRH激动剂(gonadotropin-releasing hormone agonist,GnRHa)和拮抗剂(gonadotropin-releasing hormone antagonist,GnRH-ant)两类。 GnRHa应用后可通过竞争性结合垂体的GnRH受体,封闭脑垂体GnRH受体,而使LH、FSH的生成和释放呈一过性增强,但这种刺激的持续,会导致受体的吞噬、分解增多,受体数减少,垂体细胞...
Due to their highly specific site of action, GnRH analogues have few unexpected side effects. Depot GnRH antagonist plus testosterone formulations suitable for administration at up to 3-month intervals could be promising as a hormonal male contraceptive regimen. Whether GnRH antagonists are more cost-...
Gonadotropin-releasing hormone (GnRH) stimulates the synthesis and release of gonadotropins, which induce estrogen production and subsequent ovulation. Therefore, long-term GnRH exposure to regulate ovarian hyperstimulation is recognized as the gold stan
GNRH Receptor (gonadotropin-releasing hormone receptor or GNRHR), also known as the luteinizing hormone releasing hormone receptor (LHRHR), is a member of the seven-transmembrane, G-protein coupled receptor (GPCR) family members. It is expressed on the f
Some GNRHR mutations also adversely affect activation of gonadotropin subunit or Gnrhr gene promoters in vitro (89). A number of the mutant GNRHRs can be rescued in vitro from misfolding and degradation within the cell by the addition of GNRHR antagonist IN3 (91). The prevalence of GNRHR...
This mechanism of GnRH action has been shown to exist in representative members of all vertebrate classes. With the recent identification of multiple GnRH receptors in the pituitary and evidence of multiple hypothalamic GnRH isoforms in primates, understanding the integration of this system will be ...
The exact mechanism(s) of action has not been fully elucidated, but continuous therapy with a GnRH agonist apparently produces a decrease in the number of pituitary GnRH and/or testicular LH receptors, resulting in pituitary and/or testicular desensitization, respectively. The drug does not appear...