کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
7631177 | 1494647 | 2014 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Metabolism studies of ifenprodil, a potent GluN2B receptor antagonist
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کلمات کلیدی
NADPHSAMeXtracted Ion CurrentUDPGAIfenprodilNMDAN-methyl-d-aspartateCOMTTICBSA - BSALC–MS - LC-MSNMDA receptor - NMDA گیرندهPAPs - PAP هاbovine serum albumin - آلبومین سرم گاوtotal ion current - جریان یونی کلCNS - دستگاه عصبی مرکزیcentral nervous system - سیستم عصبی مرکزیEIC - مهندسانnicotinamide adenine dinucleotide phosphate - نیکوتین آمید adenine dinucleotide phosphatecatechol-o-methyl transferase - کاتچول-ات-متیل ترانسفراز
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آنالیزی یا شیمی تجزیه
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چکیده انگلیسی
The NMDA receptor antagonist ifenprodil is an important lead structure for developing new GluN2B selective NMDA receptor antagonists. Ifenprodil itself has a high affinity to the GluN2B subunit but a poor selectivity for the NMDA receptor. This aspect and the fast biotransformation are the major drawbacks of ifenprodil. In order to optimize the development of new and more selective GluN2B (NMDA) receptor antagonists, the identification of the main metabolic pathways of ifenprodil is necessary.Herein the in vitro and in vivo phase I and phase II metabolites of ifenprodil were generated and analyzed via LC-MSn experiments. In vitro experiments were carried out with rat liver microsomes and various co-factors to generate phase I and phase II metabolites. The application of ifenprodil to a rat and the analysis of its urine led to the identification of diverse formed in vivo metabolites. The phenol represents the metabolically most labile structural element since glucuronide 7 and 8 appeared as main metabolites.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 88, 25 January 2014, Pages 96-105
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 88, 25 January 2014, Pages 96-105
نویسندگان
Evamaria Falck, Frank Begrow, Eugen Verspohl, Bernhard Wünsch,