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.
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Acknowledgements
This research was supported by National Institute of Mental Health grant MH60527 (K.W.G.) and the Wellcome Trust (R.F.H.).
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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
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DOI: https://doi.org/10.1038/nm967
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