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作为一种有效的LHRH激动剂,组氨酸释放肽刺激LH和FSH的释放,并抑制性类固醇对男性和女性生殖道的作用。其在体内和体外的效力类似于含有D-Trp6的类似物。
编号:577745
CAS号:220810-26-4
单字母:Pyr-HWSY-DHis(Bzl)-LRP-NHEt
| 参考文献(References): | K.Sundaram et al., Life Sci., 28, 83 (1981) J.DeFazio et al., Endocr. Res., 10, 163 (1984) M.J.Gibson and D.S.Kohtz, Contraception, 31, 91 (1985) M.J.Karten and J.E.Rivier, Endocr. Rev., 7, 44 (1986) G.C.Doelle et al., Horm. Metab. Res., 18, 201 (1986) J.W.Gunnet et al., J. Endocrinol., 131, 211 (1991) M.Montagner et al., Reprod. Fertil. Dev., 17, 222 (2005) Merck Index, 14th ed., No. 4722, (2006) E.D.Deeks, Drugs, 70, 623 (2010) N.Shore et al., BJU Int., 109, 226 (2012) |
Des-Gly10,D-His(Bzl)6,Pro-NHEt 9)-LHRH醋酸盐Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt醋酸盐是LHRH的长效类似物。它是一种生物相容性聚合物药物,已被证明在治疗各种自身免疫性疾病和感染方面具有长期疗效。该药物的功效可能是由于其能够与参与免疫反应的细胞表面的特定受体结合。DesGly10,D-His(Bzl)6,ProNHEt9)-LHRH醋酸盐Pyr-His-Trp-Ser-Tyr D-His(Bzl)-Leu-Arg-Pro-NHEt醋酸盐是LHRH的类似物,已被证明可有效治疗癌症和过敏症状。
Des-Gly10,D-His(Bzl)6,Pro-NHEt 9)-LHRH acetate salt Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt acetate salt is a long acting analog of LHRH. It is a biocompatible polymeric drug that has been shown to have long term efficacy in treating various autoimmune diseases and infections. The drug's efficacy may be due to its ability to bind to the specific receptors on the surface of cells that are involved in the immune response. DesGly10,D-His(Bzl)6,ProNHEt9)-LHRH acetate salt Pyr His Trp Ser Tyr D His(Bzl)-Leu Arg Pro NHEt acetate salt is an analog of LHRH and has been shown to be effective in treating cancer and allergic symptoms as well.
作为一种有效的LHRH激动剂,组氨酸释放肽刺激LH和FSH的释放,并抑制性类固醇对男性和女性生殖道的作用。其在体内和体外的效力类似于含有D-Trp6的类似物。特别是由于其高水溶性和更大的亲脂性,histrelin似乎具有临床应用前景。含有组氨酸植入物的缓释植入物被批准用于晚期激素依赖性前列腺癌的姑息治疗。
As a potent LHRH agonist, histrelin stimulates LH and FSH release and inhibits the actions of sex steroids on the male and female reproductive tracts. Its potency in vivo and in vitro is similar to that of the D-Trp6-containing analog. Especially because of its high water solubility and greater lipophilic character, histrelin appears promising for clinical application.Slow-release implants containing histreline implants were approved for the palliative treatment of advanced hormone-dependent prostate cancer.





