Modifying quinolone antibiotics yields new anxiolytics |
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| Authors: | Johnstone Timothy B C Hogenkamp Derk J Coyne Leanne Su Jiping Halliwell Robert F Tran Minhtam B Yoshimura Ryan F Li Wen-Yen Wang Jeff Gee Kelvin W |
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| Affiliation: | Department of Pharmacology, College of Medicine, University of California, Irvine, California 92697, USA. |
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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 gamma-aminobutyric acid (GABA) at the brain GABA(A) receptor complex (GRC). Modification of norfloxacin yields molecules such as compound 4 that potentiate GABA action with alpha(2) 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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