39549-22-9Relevant articles and documents
Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents
Chen, Yin,Huang, Ling,Li, Ziying,Qi, Zhaoyang,Zhang, Guisen,Zhang, Xiaohua,Zhu, Mo,Zhuang, Tao
, (2021/12/20)
In this paper, we designed and synthesized a series of novel phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents. The best compound 10 had relatively high affinity for the GABAA receptor and low affinity for thirteen other off-target receptors. In three animal models (mice, rats, and rabbits), compound 10 exerted potent hypnotic effects (HD50 = 5.2 mg/kg in rabbits), comparable duration of the loss of righting reflex (LORR), and significant shorter recovery time (time to walk) than propanidid. Furthermore, compound 10 (TI = 18.1) showed higher safety profile than propanidid (TI = 14.7) in rabbits. Above results suggested that compound 10 may have predictable and rapid recovery profile in anesthesia.
Pharmaceutical compositions of short-acting sedative hypnotic agent
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Page/Page column 5, (2008/06/13)
The invention provides pharmaceutical compositions comprising a phenylacetic acid ester compound useful for inducing or maintaining general anesthesia or sedation in mammals, methods for preparing such compositions, and methods for inducing or maintaining