Modifying quinolone antibiotics yields new anxiolytics.

Johnstone, Timothy B C; Hogenkamp, Derk J; Coyne, Leanne; Su, Jiping; Halliwell, Robert F; Tran, Minhtam B; Yoshimura, Ryan F; Li, Wen-Yen et al. · Nat Med · 2004

basic_science · Level V

Where this comes from

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