抗雄激素
抗雄激素(anti-androgens),或稱為雄性激素拮抗劑(androgen antagonists)。於1960年代時被發現,藉由阻斷特定的受體而抑制雄性激素的作用。可以競爭細胞表面的接受器或是影響雄性激素的產生。[1]抗雄激素可用來治療一系列的疾病。在男性,抗雄激素經常用來治療前列腺癌。[2]对女性使用通常用來減少體內過多的雄性激素。抗雄激素對環境的影響已經受到高度的關注。許多的工業化學物質、殺蟲劑都有抗雄激素的作用。一些特定的植物也被發現會產生抗雄激素。環境中的抗雄激素對於生殖系統還在發育的小孩會有深遠的影響。
抗雄激素 | |
---|---|
药物种类 | |
Bicalutamide, a nonsteroidal antiandrogen and the most widely used androgen receptor antagonist in the treatment of prostate cancer. | |
用途 | Various |
生物目标 | Androgen receptor |
ATC代码 | L02BB |
外部链接 | |
MeSH | D000726 |
機轉
抗雄激素可按原理分为雄性激素受體阻断剂、雄性激素合成抑制剂,和抗促性腺激素三种。
阻断受体
物质 | RBA (%) |
---|---|
Metribolone | 100 |
双氢睾酮 | 85 |
醋酸环丙孕酮 | 7.8 |
螺内酯 | 2.3 |
比卡鲁胺 | 1.4 |
Nilutamide | 0.9 |
Hydroxyflutamide | 0.57 |
氟他胺 | <0.0057 |
阻断受体的可按结果分为類固醇類和非類固醇類两种。類固醇類抗雄激素与睾酮、孕酮等类固醇类似,由于其类固醇的结构经常会激活其他激素受体,造成偏离目标的活性。[5]因為它有高脂性,所以可以擴散穿過細胞膜的雙磷脂層,阻擋睪酮和双氢睾酮(DHT)鍵結到受體上,進而影響基因表現活性。[6]比卡鲁胺和氟他胺这类非類固醇類抗雄激素则没有这类副作用,因此有时候也叫“纯”抗雄激素。[5]
参见
参考文献
- Mowszowicz I.(1989). "Antiandrogens. Mechanisms and paradoxical effects". Ann Endocrinol (Paris) 50 (3): 50 (3):189–99.,
- Mowszowicz I.(1989). Gillatt D.(2006). "Antiandrogen treatments in locally advanced prostate cancer: are they all the same?". J Cancer Res Clin Oncol. 1: S17-26.
- Ayub M, Levell MJ. . J. Steroid Biochem. August 1989, 33 (2): 251–5. PMID 2788775. doi:10.1016/0022-4731(89)90301-4.
- Yamasaki K, Sawaki M, Noda S, Muroi T, Takakura S, Mitoma H, Sakamoto S, Nakai M, Yakabe Y. . Toxicology. 2004, 195 (2-3): 177–86. PMID 14751673. doi:10.1016/j.tox.2003.09.012.
- Thomas L. Lemke; David A. Williams. . Lippincott Williams & Wilkins. 24 January 2012: 228–231, 1371–1372. ISBN 978-1-60913-345-0.
- "Steroidal Antiandrogens" 的存檔,存档日期2012-04-26.,Health and Prostate. Retrieved 9 December 2011.
- William Figg; Cindy H. Chau; Eric J. Small. . Springer Science & Business Media. 14 September 2010: 71–72,75,91–96. ISBN 978-1-60327-829-4.
- Jerome F. Strauss, III; Robert L. Barbieri. . Elsevier Health Sciences. 13 September 2013: 90–. ISBN 978-1-4557-2758-2.
- Flores E, Bratoeff E, Cabeza M, Ramirez E, Quiroz A, Heuze I. . Mini-Reviews in Medicinal Chemistry. May 2003, 3 (3): 225–37. PMID 12570838. doi:10.2174/1389557033488196.
- Peter B. Farmer; John M. Walker. . Springer Science & Business Media. 6 December 2012: 232–. ISBN 978-1-4684-7313-1.
- Brueggemeier, Robert W. . 2006. doi:10.1002/3527600906.mcb.200500066.
- de Lignières B, Silberstein S. . Cephalalgia : an International Journal of Headache. April 2000, 20 (3): 200–7. PMID 10997774. doi:10.1046/j.1468-2982.2000.00042.x.
- Neumann F. . Postgraduate Medical Journal. 1978,. 54 Suppl 2: 11–24. PMID 368741.
- Jacobi GH, Altwein JE, Kurth KH, Basting R, Hohenfellner R. . Br J Urol. 1980, 52 (3): 208–15. PMID 7000222. doi:10.1111/j.1464-410x.1980.tb02961.x.
- Wein AJ, Kavoussi LR, Novick AC, Partin AW, Peters CA. . Elsevier Health Sciences. 25 August 2011: 2938–. ISBN 978-1-4160-6911-9.
- Kjeld JM, Puah CM, Kaufman B, Loizou S, Vlotides J, Gwee HM, Kahn F, Sood R, Joplin GF. . Clinical Endocrinology. 1979, 11 (5): 497–504. PMID 519881. doi:10.1111/j.1365-2265.1979.tb03102.x.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.