1-氨基邻苯二甲酰溴鎓作为GABAA受体配体的合成及构效关系
Synthesis and structure-activity relationships of 1-aminophthalazinium bromides as GABAA receptor ligands.
作者信息
Catarzi D, Cecchi L, Filacchioni G, Bartolini A, Carpenedo R, Galli A, Mori F
机构信息
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
出版信息
Drug Des Discov. 1993;10(1):23-34.
PMID:8399992
Abstract
The synthesis and the GABAA binding activity of a series of 1-amino-2-alkylphthalazinium bromides (series A) and 1-amino-3-alkylphthalazinium bromides (series B) bearing different substituents at position-4 are reported. Some compounds of series A, bearing a lipophilic substituent at position-4, showed a good binding activity as well as in vivo convulsant activity.
摘要
报道了一系列在4位带有不同取代基的1-氨基-2-烷基邻苯二甲酰溴鎓盐（A系列）和1-氨基-3-烷基邻苯二甲酰溴鎓盐（B系列）的合成及其与GABAA的结合活性。A系列中的一些化合物在4位带有亲脂性取代基，表现出良好的结合活性以及体内惊厥活性。
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