科研之友
微信
新浪微博
Facebook
分享链接
摘要
Amitifadine (E8-1010, DOV-21947) is a "triple reuptake inhibitor" that inhibits the reuptake of serotonin, norepinephrine and dopamine with relative in vitro potencies of 1:2:8. In addition to this in vitro receptor profile, in vivo microdialysis studies demonstrated that amitifadine increases extracellular concentrations of the three monoamines and reduces concentrations of monoamine metabolites. Amitifadine has also shown antidepressant potential in animal models, including the forced swim and tail suspension tests. As a result of these preclinical studies, amitifadine is currently in clinical development as an antidepressant and has demonstrated efficacy and tolerability in a randomized, placebo-controlled, proof-of-concept clinical trial in patients with major depressive disorder. The current monograph describes the chemical properties of amitifadine, as well as information gleaned from the preclinical and clinical studies to date. The premise behind the development of triple reuptake inhibitors is discussed.
- 出版日期2012-4
