Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant …

…, M Franco, C Altomare, E Sanna, M Usala…

文献索引：Trapani, Giuseppe; Latrofa, Andrea; Franco, Massimo; Altomare, Cosimo; Sanna, Enrico; Usala, Marcello; Biggio, Giovanni; Liso, Gaetano Journal of Medicinal Chemistry, 1998 , vol. 41, # 11 p. 1846 - 1854

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被引用次数: 90

摘要

A number of propofol (2, 6-diisopropylphenol) congeners and derivatives were synthesized and their in vitro capability to affect GABAA receptors determined by the inhibition of the specific [35S]-tert-butylbicyclophosphorothionate ([35S] TBPS) binding to rat whole brain membranes. Introduction of halogen (Cl, Br, and I) and benzoyl substituents in the para position of the phenyl group resulted in ligands with higher potency at inhibiting [35S] ...