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Antimicrob Agents Chemother. 2010 Dec;54(12):5399-402. doi: 10.1128/AAC.00840-10. Epub 2010 Sep 20.

Molecular characterization of off-target activities of telithromycin: a potential role for nicotinic acetylcholine receptors.

Author information

1
HiQScreen, 15 rue de l'Athénée, 1206 Geneva, Switzerland. daniel.bertrand@hiqscreen.com

Abstract

Adverse effects have limited the clinical use of telithromycin. Preferential inhibition of the nicotinic acetylcholine receptors (nAChR) at the neuromuscular junction (α3β2 and NMJ), the ciliary ganglion of the eye (α3β4 and α7), and the vagus nerve innervating the liver (α7) could account for the exacerbation of myasthenia gravis, the visual disturbance, and the liver failure seen with telithromycin use. The studies presented here enable the prediction of expected side effects of macrolides in development, such as solithromycin (CEM-101).

PMID:
20855733
PMCID:
PMC2981250
DOI:
10.1128/AAC.00840-10
[Indexed for MEDLINE]
Free PMC Article

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