Modifying quinolone antibiotics yields new anxiolytics.
Modifying quinolone antibiotics yields new anxiolytics.
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改良喹诺酮类抗生素可产生新的抗焦虑药。
DOI：
10.1038/nm967
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发表时间：
2004
期刊：
影响因子：
--
通讯作者：
Gee,KelvinW
中科院分区：
文献类型：
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作者：
Johnstone,TimothyBC;Hogenkamp,DerkJ;Coyne,Leanne;Su,Jiping;Halliwell,RobertF;Tran,MinhtamB;Yoshimura,RyanF;Li,Wen-Yen;Wang,Jeff;Gee,KelvinW
Patients taking fluoroquinolone antibiotics such as norfloxacin exhibit a low incidence of convulsions and anxiety. These side effects probably result from antagonism of the neurotransmitter γ-aminobutyric acid (GABA) at the brain GABAAreceptor complex (GRC). Modification of norfloxacin yields molecules such as compound 4 that potentiate GABA action with α2subunit selectivity. Compound 4 is anxiolytic but does not cause sedation, and may represent a new class of ligands that have anxiolytic activity without sedative liability.
