Author: ["Timothy B C Johnstone","Derk J Hogenkamp","Leanne Coyne","Jiping Su","Robert F Halliwell","Minhtam B Tran","Ryan F Yoshimura","Wen-Yen Li","Jeff Wang","Kelvin W Gee"]
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Abstract
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 activity without sedative liability.Cite this article
Johnstone, T., Hogenkamp, D., Coyne, L. et al. Modifying quinolone antibiotics yields new anxiolytics. Nat Med 10, 31–32 (2004). https://doi.org/10.1038/nm967 