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- Title
Modifying quinolone antibiotics yields new anxiolytics.
- Authors
Johnstone, Timothy B. C.; Hogenkamp, Derk J.; Coyne, Leanne; Jiping Su, Leanne; Halliwell, Robert F.; Tran, Minhtam B.; Yoshimura, Ryan F.; Wen-Yen Li, Ryan F.; Wang, Jeff; Gee, Kelvin W.
- 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 ?-aminobutyric acid (GABA) at the brain GABAA receptor complex (GRC). Modification of norfloxacin yields molecules such as compound 4 that potentiate GABA action with a2 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.
- Subjects
GABA; QUINOLONE antibacterial agents; ANTI-infective agents; ANTIBIOTICS; ANXIETY; SEIZURES (Medicine)
- Publication
Nature Medicine, 2004, Vol 10, Issue 1, p31
- ISSN
1078-8956
- Publication type
Article
- DOI
10.1038/nm967