Modifying quinolone antibiotics yields new anxiolytics
@article{Johnstone2004ModifyingQA, title={Modifying quinolone antibiotics yields new anxiolytics}, author={Timothy B C Johnstone and Derk J. Hogenkamp and Leanne Coyne and Jiping Su and Robert F. Halliwell and Minhtam B. Tran and Ryan F. Yoshimura and Wen-Yen Li and Jeff J.-H. Wang and Kelvin W. Gee}, journal={Nature Medicine}, year={2004}, volume={10}, pages={31-32} }
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 GABAA receptor complex (GRC). Modification of norfloxacin yields molecules such as compound 4 that potentiate GABA action with α2 subunit selectivity. Compound 4 is anxiolytic but does not cause sedation, and may represent a new class of ligands that have anxiolytic…
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