阿来司酮 |
|
| 商品名 | Alizin |
|---|
| 其他名稱 | 安哥司酮、RU-46534、RU-534 |
|---|
| 藥物類別 | 抗孕激素、抗糖皮质激素 |
|---|
| ATC碼 | |
|---|
|
(8S,11R,13S,14S,17R)-11-[4-(dimethylamino)phenyl]-17-hydroxy-13-methyl-17-[(Z)-prop-1-enyl]-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
|
| CAS号 | 124478-60-0 |
|---|
| PubChem CID | |
|---|
| ChemSpider | |
|---|
| UNII | |
|---|
| KEGG | |
|---|
| ChEMBL | |
|---|
| CompTox Dashboard (EPA) | |
|---|
| ECHA InfoCard | 100.211.372 |
|---|
|
| 化学式 | C29H37NO2 |
|---|
| 摩尔质量 | 431.62 g·mol−1 |
|---|
| 3D模型(JSmol) | |
|---|
C/C=C\[C@@]1(CC[C@@H]2[C@@]1(C[C@@H](C3=C4CCC(=O)C=C4CC[C@@H]23)C5=CC=C(C=C5)N(C)C)C)O
|
InChI=1S/C29H37NO2/c1-5-15-29(32)16-14-26-24-12-8-20-17-22(31)11-13-23(20)27(24)25(18-28(26,29)2)19-6-9-21(10-7-19)30(3)4/h5-7,9-10,15,17,24-26,32H,8,11-14,16,18H2,1-4H3/b15-5-/t24-,25+,26-,28-,29-/m0/s1 Key:RTCKAOKDXNYXEH-FWSJOHTJSA-N
|
阿来司酮(INN:aglepristone;开发代号:RU-46534、RU-534),或译安哥司酮,是一种与米非司酮相关的合成类甾体抗孕激素,由维克在几个欧洲国家销售,用作兽药。[1][2][3]它专门用作妊娠动物的堕胎药。[1][3][4]阿来司酮也具有一些抗糖皮质激素活性。[5][6]
参考资料
- ^ 1.0 1.1 Kaufman LK, Baldwin CJ. Pregancy Loss in the Bitch and Queen. Bonagura JD, Twedt DC (编). Kirk's Current Veterinary Therapy XV. Elsevier Health Sciences. 1 December 2013: 3009–. ISBN 978-0-323-22762-9.
- ^ Squires EJ. Endocrine manipulation of reproduction.. Applied Animal Endocrinology. CABI. 2010: 207–. ISBN 978-1-84593-755-3.
- ^ 3.0 3.1 Papich MC. Aglepristone. Saunders Handbook of Veterinary Drugs: Small and Large Animal. Elsevier Health Sciences. 3 November 2010: 120–. ISBN 978-1-4377-0192-0.
- ^ Fieni F, Martal J, Marnet PG, Siliart B, Bernard F, Riou M, Bruyas JF, Tainturier D. Concannon PW , 编. Hormonal variation in bitches after early or mid-pregnancy termination with aglepristone (RU534). Journal of Reproduction and Fertility. Supplement. Advances in reproduction in dogs, cats and exotic carnivores: proceedings of the fourth International Symposium on Canine and Feline Reproduction, Oslo, Norway, 29 June-1 July 2000. 2001, 57: 243–8. ISBN 978-0-906545-37-9. PMID 11787157.
- ^ Batista M, Reyes R, Santana M, Alamo D, Vilar J, González F, et al. Induction of parturition with aglepristone in the Majorera goat. Reproduction in Domestic Animals = Zuchthygiene. October 2011, 46 (5): 882–888. PMID 21320179. doi:10.1111/j.1439-0531.2011.01759.x.
- ^ Baan M, Taverne MA, de Gier J, Kooistra HS, Kindahl H, Dieleman SJ, Okkens AC. Hormonal changes in spontaneous and aglépristone-induced parturition in dogs. Theriogenology. March 2008, 69 (4): 399–407. PMID 18054071. doi:10.1016/j.theriogenology.2007.10.008.
|
|---|
黃體素 (及黄体制剂) | | 孕酮衍生物 | |
|---|
| 逆孕酮衍生物 | |
|---|
17α-羟孕酮衍生物 (and closely related) |
- Acetomepregenol (mepregenol diacetate)
- Algestone
- Algestone acetophenide
- Anagestone acetate
- Chlormadinone acetate
- 醋酸环丙孕酮
- Delmadinone acetate
- Flugestone acetate (flurogestone acetate)
- Hydroxyprogesterone
- Hydroxyprogesterone acetate
- Hydroxyprogesterone caproate
- Hydroxyprogesterone heptanoate
- Medroxyprogesterone
- Medroxyprogesterone acetate#
- Megestrol acetate
- Melengestrol acetate
- Osaterone acetate
- Pentagestrone acetate
- Other 17α-substitutions: Haloprogesterone
- Medrogestone
- Proligestone
|
|---|
19-去甲孕酮衍生物 (incl. 17α-substituted) |
- Demegestone
- Gestonorone caproate (gestronol hexanoate)
- Nomegestrol acetate
- Norgestomet
- Promegestone
- Segesterone acetate (nestorone)
- Trimegestone
|
|---|
| 17α-乙炔基睾酮衍生物 | |
|---|
| 19-去甲睾酮衍生物 |
- Estranes: Etynodiol diacetate
- 孕三烯酮
- Lynestrenol
- 炔诺酮#
- 醋酸炔诺酮
- 庚酸炔诺酮
- 异炔诺酮
- Norgestrienone
- Quingestanol acetate
- 替勃龙
- 性腺:去氧孕烯
- Dienogest
- Etonogestrel
- Gestodene
- 左炔诺孕酮#
- Norelgestromin
- Norgestimate
- Norgestrel
- 其他:Allylestrenol
- Altrenogest
- Norgesterone
- Normethandrone (methylestrenolone)
- Norvinisterone
- Oxendolone
|
|---|
| 17α-Spirolactosteroid |
- Canrenone
- Drospirenone
- Potassium canrenoate
- 螺内酯
|
|---|
| 其他 | |
|---|
|
|---|
| SPRMs |
- Asoprisnil†
- Telapristone§
- Ulipristal acetate
|
|---|
| Antiprogestogens | |
|---|
參見 雄激素类 • 雌激素类和抗雌激素类 • Glucocorticoids and antiglucocorticoids • Mineralocorticoids and antimineralocorticoids • {{Gonadotropins and GnRH}} |
|
|---|
| 受體 | |
|---|
酶 (抑制劑) | | 20,22-Desmolase |
- 22-ABC
- 3,3′-Dimethoxybenzidine
- 3-Methoxybenzidine
- Aminoglutethimide
- Cyanoketone
- Danazol
- Etomidate
- Mitotane
- Trilostane
|
|---|
17α-Hydroxylase, 17,20-Lyase |
- 22-ABC
- 22-Oxime
- Abiraterone
- Bifonazole
- 克催瑪汝
- Cyanoketone
- Cyproterone
- Danazol
- 益康唑
- Galeterone
- Gestrinone
- Isoconazole
- 酮康唑
- L-39
- Liarozole
- LY-207,320
- MDL-27,302
- 咪康唑
- 美服培酮
- Orteronel
- 吡格列酮
- 罗格列酮
- 螺内酯
- 司坦唑醇
- SU-10,603
- 转化生长因子-β
- Tioconazole
- Troglitazone
- VN/87-1
- YM116
|
|---|
| 3β-HSD |
- 4-MA
- Azastene
- Cyanoketone
- Danazol
- Epostane
- Genistein
- Gestrinone
- Metyrapone
- Norethisterone
- Oxymetholone
- 吡格列酮
- 罗格列酮
- Trilostane
- Troglitazone
|
|---|
| 21-羥化酶 |
- Aminoglutethimide
- Amphenone B
- Bifonazole
- 克催瑪汝
- 地西泮
- 益康唑
- Genistein
- Isoconazole
- 酮康唑
- Metyrapone
- 咪康唑
- 咪達唑侖
- Tioconazole
|
|---|
| 11β-Hydroxylase |
- Aminoglutethimide
- Canrenone
- Etomidate
- Fadrozole
- FETO
- 酮康唑
- Metomidate
- Metyrapone
- Mitotane
- Potassium canrenoate
- 螺内酯
- Trilostane
|
|---|
| 18-Hydroxylase |
- Aminoglutethimide
- Canrenone
- FAD286
- Fadrozole
- 酮康唑
- LCI699
- Metyrapone
- Mespirenone
- Potassium canrenoate
- 螺内酯
|
|---|
|
|---|
| 其它 | | 内源 |
- 前体: 膽固醇
- 22R-Hydroxycholesterol
- 20α,22R-Dihydroxycholesterol
- 孕烯醇酮
- 17-Hydroxypregnenolone
- 17-Hydroxyprogesterone
- 孕酮
- 11-脱氧皮质酮
|
|---|
| 間接 | |
|---|
| 外科手術 |
- Adrenalectomy
- Hypophysectomy
|
|---|
|
|---|
|
|---|
| PR | | 受體致活劑 | |
|---|
| Mixed (SPRMs) |
- Apigenin
- Asoprisnil
- Asoprisnil ecamate
- Guggulsterone
- 山柰酚
- J1042
- LG-120838
- Naringenin
- PRA-910
- 丁香酸
- Telapristone
- 受體拮抗劑: 美服培酮
- Org-31710
- Org-33628
- Ulipristal acetate
- ZK-137316
|
|---|
| Antagonists |
- 3α-Hydroxytibolone
- 3β-Hydroxytibolone
- 阿来司酮
- 利洛司酮
- 洛那立生
- 奥那司酮
- 托立司酮
- 丙戊酸
- 维拉立生
- 扎诺特隆
- ZM-150271
- ZM-172406
|
|---|
|
|---|
mPRs (PAQRs) | | 受體致活劑 |
- 5α-Dihydroprogesterone
- 5β-Dihydroprogesterone
- 11-脱氧皮质酮
- 17α-Hydroxyprogesterone
- 17α,21-Dihydroxyprogesterone
- Allopregnanolone
- 美服培酮
- 孕烯醇酮
- 孕酮
|
|---|
| Antagonists | |
|---|
|
|---|
參見: 雄激素 • 雌激素 • Glucocorticoidics • Mineralocorticoidics |