کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2487911 | 1114440 | 2006 | 16 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Physicochemical and Biopharmaceutical Characterization of endo-2-(8-Methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1H-benz[e]isoindol-1-one (CR3124) a Novel Potent 5-HT3 Receptor Antagonist
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Physicochemical and Biopharmaceutical Characterization of endo-2-(8-Methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1H-benz[e]isoindol-1-one (CR3124) a Novel Potent 5-HT3 Receptor Antagonist Physicochemical and Biopharmaceutical Characterization of endo-2-(8-Methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1H-benz[e]isoindol-1-one (CR3124) a Novel Potent 5-HT3 Receptor Antagonist](/preview/png/2487911.png)
چکیده انگلیسی
The physicochemical and biopharmaceutical properties, such as pKa, crystal habit, water solubility, logD, molecular structure and dynamics, and membrane permeability of CR3124 (endo-2-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1H-benz[e]isoindol-1-one, a novel potent 5-HT3 receptor antagonist) have been studied in order to obtain preformulation information. The study showed that CR3124 is a very rigid molecule in which conformational freedom due to the presence of a rotatable bond is restricted by the interaction between an activated hydrogen and the amide oxygen and the conformation of the tropane piperidine ring is regulated by the environment in such a manner as to optimize the intermolecular interactions with the solvent. This chameleon behavior appears to be capable of explaining the biopharmaceutical properties showed by CR3124, such as low wettability, relatively good solubility, and very high membrane permeability.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 95, Issue 12, December 2006, Pages 2706-2721
Journal: Journal of Pharmaceutical Sciences - Volume 95, Issue 12, December 2006, Pages 2706-2721
نویسندگان
Andrea Cappelli, Valter Travagli, Iacopo Zanardi, Maurizio Anzini, Gianluca Giorgi, Alessandro Donati, Marianna Aggravi, Mario Casolaro, Massimo Fresta, Eugenio Paccagnini, Francesco Makovec, Salvatore Vomero,