Modifying quinolone antibiotics yields new anxiolytics.
basic_science · Level V
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- Record sourced from PubMed, PMID 14647497.
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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.
Medical subject headings
- Anti-Anxiety Agents
- Anti-Infective Agents
- Fluoroquinolones