α-Amino acid phenolic ester derivatives: novel water-soluble general anesthetic agents which allosterically modulate GABAA receptors

…, FH Sansbury, D Stevenson, H Sundaram

文献索引：Anderson; Belelli; Bennett; Buchanan; Casula; Cooke; Feilden; Gemmell; Hamilton; Hutchinson; Lambert; Maidment; McGuire; McPhail; Miller; Muntoni; Peters; Sansbury; Stevenson; Sundaramt Journal of Medicinal Chemistry, 2001 , vol. 44, # 22 p. 3582 - 3591

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被引用次数: 20

摘要

In the search for a novel water-soluble general anesthetic agent the activity of an α-amino acid phenolic ester lead, identified from patent literature, was markedly improved. In addition to improving in vivo activity in mice, good in vitro activity at GABAA receptors was also conferred. Within the series of compounds good enantioselectivity for both in vitro and in vivo activity was found, supporting a protein-mediated mechanism of action for anesthesia ...