Ethylatropine Bromide as a Peripherally Restricted Muscarinic Antagonist

التفاصيل البيبلوغرافية
العنوان: Ethylatropine Bromide as a Peripherally Restricted Muscarinic Antagonist
المؤلفون: Asheebo Rojas, Alec Walker, Thota Ganesh, Raymond Dingledine
المصدر: ACS Chemical Neuroscience. 8:712-717
بيانات النشر: American Chemical Society (ACS), 2017.
سنة النشر: 2017
مصطلحات موضوعية: Male, 0301 basic medicine, Patch-Clamp Techniques, Carbachol, Physiology, Cost effectiveness, Cognitive Neuroscience, Muscarinic Antagonists, Muscarinic Agonists, Pharmacology, Biochemistry, Article, Methylatropine, Mice, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Bromide, medicine, Animals, Humans, Atropine Derivatives, Pilocarpine, Muscarinic antagonist, Cell Biology, General Medicine, Mice, Inbred C57BL, Disease Models, Animal, Atropine, 030104 developmental biology, chemistry, 030217 neurology & neurosurgery, Acetylcholine, medicine.drug
الوصف: Quaternary ammonium analogues of atropine that are unable to cross the blood-brain barrier are used to alleviate peripheral muscarinic toxicity in animal models of epilepsy produced by systemic administration of pilocarpine or diisopropylfluorophosphate (DFP). Currently, methylatropine is the most popular and potent of these quaternary derivatives; however, it is expensive and produced in limited quantity. Here, we propose the use of ethylatropine bromide as an alternative to methylatropine. The synthesis of ethylatropine bromide is simple, inexpensive and has low environmental impact. We demonstrate the efficacy of ethylatropine bromide to antagonize the carbachol induced rise in intracellular calcium in a calcium mobilization assay, and its ability to prevent pilocarpine-induced total fluid secretions in mice without blocking pilocarpine-induced seizures. The ease of synthesis, cost effectiveness, and efficacy makes ethylatropine bromide a desirable alternative to methylatropine as a peripherally restricted acetylcholine receptor antagonist.
تدمد: 1948-7193
الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77a4b08c501a8c4cda69e84c81c19d85Test
https://doi.org/10.1021/acschemneuro.6b00334Test
حقوق: OPEN
رقم الانضمام: edsair.doi.dedup.....77a4b08c501a8c4cda69e84c81c19d85
قاعدة البيانات: OpenAIRE