化合物简介
Naluzotan (INN, USAN; PRX-00023) is a serotonergic drug of the phenylpiperazine class that was under investigation by EPIX Pharmaceuticals Inc for the treatment of generalized anxiety disorder and major depressive disorder. It acts as a selective and potent 5-HT1A receptor partial agonist, readily stimulating prolactin responses, though it has also been found to bind to and activate the σ receptor. Naluzotan was well tolerated in clinical trials, with more patients in the control group dropping out due to adverse effects than in the active group in one study. The most frequently reported side effect was headache in 15% of patients (compared to 10% for placebo). In addition, naluzotan demonstrated significant antidepressant and anxiolytic effects as per the HAM-D and MADRS and the HAM-A, respectively, in some trials, but in others it did not. In the end it was not found to be significantly superior enough to placebo and development was stopped.
基本信息
中文名称
N-[3-[4-[4-[(环己基甲基磺酰基)氨基]丁基]哌嗪-1-基]苯基]乙酰胺
英文名称
N-[3-[4-[4-(cyclohexylmethylsulfonylamino)butyl]piperazin-1-yl]phenyl]acetamide
中文别名
英文别名
Naluzotan、UNII-LQ54E5B4EW
CAS号
740873-06-7
分子式
C23H38N4O3S
分子量
450.638
精确质量
450.266
PSA
93.62
LOGP
5.171
编号系统
UNII
LQ54E5B4EW
物化性质
密度
1.169
合成路线
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