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Neuropharmacology

Antibiotic yields anxiolytic

Nature Reviews Drug Discovery volume 3, page 14 (2004)Cite this article

The search strategy devised by Gee et al. was based on the hypothesis that mitigation of side effects might be achieved by targeting non-benzodiazepine-binding sites of the GRC. Compounds related to the fluoroquinolone antibiotic norfloxacin were chosen as screening candidates for two reasons: first, a small proportion of patients taking this antibiotic experience anxiety as a side effect; second, norfloxacin is known to antagonize GABAA receptors at an undefined site. So, chemical modification of norfloxacin could generate compounds with the opposite, GABA-enhancing anxiolytic effect.

In a standard assay for GABA modulation, several norfloxacin-related chemotypes inhibited the binding of the convulsant TBPS to the GRC. Analysis of the most active product — dubbed compound 4 — showed that this compound does not act directly on the GRC-binding sites for TBPS, norfloxacin, GABA or benzodiazepines.

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References

ORIGINAL RESEARCH PAPER

  1. Johnstone, T. B. C. et al. Modifying quinolone antibiotics yields new anxiolytics. Nature Med. 30 Nov 2003 (doi: 10.1038/nm967)

FURTHER READING

  1. Christopoulos, A. Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nature Rev. Drug Discov. 1, 198–210 (2002)

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Authors
  1. Suzanne Farley
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Farley, S. Antibiotic yields anxiolytic. Nat Rev Drug Discov 3, 14 (2004). https://doi.org/10.1038/nrd1293

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