Molecular characterization of off-target activities of telithromycin: a potential role for nicotinic acetylcholine receptors.
نویسندگان
چکیده
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).
منابع مشابه
Modulation of Basal Glutamatergic Transmission by Nicotinic Acetylcholine Receptors in Rat Hippocampal Slices
Objective(s) Nicotinic acetylcholine receptors (nAChRs) regulate epileptiform activity and produce a sustained pro-epileptogenic action within the hippocampal slices. In the present study, we investigated the effect of nAChRs on evoked glutamatergic synaptic transmission in area CA3 and CA1 of rat hippocampal slices to identify possible excitatory circuits through which activation of nAChRs pr...
متن کاملPaeoniflorin has anti-inflammation and neurogenesis functions through nicotinic acetylcholine receptors in cerebral ischemia-reperfusion injury rats
Objective(s): Paeoniflorin (PF) has anti-oxidation, anti-inflammation, anti-apoptosis, and neuroprotection pharmacological effects against ischemic injury. The aim of the present study was to investigate the neuroprotection mechanisms of PF in cerebral ischemia-reperfusion injury rats.Materials and Methods: We established an animal model of cerebral infarct by occlusion of the middle cerebral a...
متن کاملCharacterization of inhibitory effects of the potential therapeutic inhibitors, benzoic acid and pyridine derivatives, on the monophenolase and diphenolase activities of tyrosinase
Objective(s):Involvement of tyrosinase in the synthesis of melanin and cell signaling pathway has made it an attractive target in the search for therapeutic inhibitors for treatment of different skin hyperpigmentation disorders and melanoma cancers. Materials and Methods: In the present study, we conducted a comprehensive kinetic analysis to understand the mechanisms of inhibition imposed by 2-...
متن کاملRole of the thalamic parafascicular nucleus cholinergic system in the modulation of acute corneal nociception in rats
The present study investigated the effects of microinjections of acetylcholine (a cholinergic agonist), physostigmine (a cholinesterase inhibitor), atropine (an antagonist of muscarinic cholinergic receptors) and hexamethonium (an antagonist of nicotinic cholinergic receptors) into the parafascicular nucleus of thalamus on the acute corneal nociception in rats. Acute corneal nociception was ind...
متن کاملنقش گیرنده‌های نیکوتینی استیل کولین، پروتئین کیناز B و پروتئین کیناز Mζ بر اثر حفاظتی اسید رزمارینیک در مدل بیماری آلزایمر القا شده به وسیله‌ی بتا آمیلوئید (35-25) در موش صحرایی
Background and Objective: Alzheimer’s disease (AD) is one of the most common neurodegenerative diseases and results from the extracellular accumulation of b-amyloid peptides and the resulting neuronal dysfunction. In this study, the role of nicotinic acetylcholine receptors, protein kinase B (PKB) and protein kinase M (PKM) were evaluated in order to examine the mechanism of the protective effe...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Antimicrobial agents and chemotherapy
دوره 54 12 شماره
صفحات -
تاریخ انتشار 2010