Molecular Characterization of Off-Target Activities of Telithromycin: a Potential Role for Nicotinic Acetylcholine Receptors-Reference-Cited by-同舟云学术

Molecular Characterization of Off-Target Activities of Telithromycin: a Potential Role for Nicotinic Acetylcholine Receptors

Published:2010-12 Issue:12 Volume:54 Page:5399-5402
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Bertrand Daniel¹,Bertrand Sonia¹,Neveu Estelle¹,Fernandes Prabhavathi²

Affiliation:

1. HiQScreen Sàrl, 15 rue de l'Athénée, 1206 Geneva, Switzerland

2. Cempra Pharmaceuticals Inc., Chapel Hill, North Carolina 27514

Abstract

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).

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.00840-10

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