Title

Modifying quinolone antibiotics yields new anxiolytics

Document Type

Article

Publication Title

Nature Medicine

ISSN

1078-8956

Volume

10

Issue

1

DOI

10.1038/nm967

First Page

31

Last Page

32

Publication Date

1-1-2004

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 GABA receptor complex (GRC). Modification of norfloxacin yields molecules such as compound 4 that potentiate GABA action with α 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. A 2

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