阿米贝隆

化合物

阿米贝隆(英语:Amibegron;开发代号:SR-58,611A)是赛诺菲-安万特(现为赛诺菲)开发的药物,作为β3肾上腺素受体英语Beta-3 adrenergic receptor的选择性激动剂。它是第一个开发的口服活性β3激动剂,能够进入中枢神经系统并具有抗抑郁抗焦虑作用。[1][2]

阿米贝隆
临床资料
给药途径口服
ATC码
  • 未分配
法律规范状态
法律规范
  • 开发中止
识别信息
  • Ethyl ([(7S)-7-([(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino)-5,6,7,8-tetrahydronaphthalen-2-yl]oxy)acetate
CAS号121524-08-1  checkY
121524-09-2  checkY
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C22H26ClNO4
摩尔质量403.90 g·mol−1
3D模型(JSmol英语JSmol
  • CCOC(=O)COc3ccc1CCC(Cc1c3)NCC(O)c2cc(Cl)ccc2
  • InChI=1S/C22H26ClNO4.ClH/c1-2-27-22(26)14-28-20-9-7-15-6-8-19(11-17(15)12-20)24-13-21(25)16-4-3-5-18(23)10-16;/h3-5,7,9-10,12,19,21,24-25H,2,6,8,11,13-14H2,1H3;1H/t19-,21-;/m0./s1 checkY
  • Key:NQIZCDQCNYCVAS-RQBPZYBGSA-N checkY

2008年7月31日,赛诺菲-安万特宣布决定停止阿米贝隆的开发。[3]

参考资料

  1. ^ Stemmelin J, Cohen C, Terranova JP, Lopez-Grancha M, Pichat P, Bergis O, et al. Stimulation of the beta3-Adrenoceptor as a novel treatment strategy for anxiety and depressive disorders. Neuropsychopharmacology. February 2008, 33 (3): 574–87. PMID 17460614. doi:10.1038/sj.npp.1301424 . 
  2. ^ Overstreet DH, Stemmelin J, Griebel G. Confirmation of antidepressant potential of the selective beta3 adrenoceptor agonist amibegron in an animal model of depression. Pharmacology, Biochemistry, and Behavior. June 2008, 89 (4): 623–6. PMID 18358519. S2CID 35026036. doi:10.1016/j.pbb.2008.02.020. 
  3. ^ Second quarter 2008 results. July 31, 2008, retrieved March 9, 2009.