کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
8529501 1558860 2018 39 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
In vivo and in vitro ADMET profiling and in vivo pharmacodynamic investigations of a selective α7 nicotinic acetylcholine receptor agonist with a spirocyclic Δ2-isoxazoline molecular skeleton
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
In vivo and in vitro ADMET profiling and in vivo pharmacodynamic investigations of a selective α7 nicotinic acetylcholine receptor agonist with a spirocyclic Δ2-isoxazoline molecular skeleton
چکیده انگلیسی
(±)-3-Methoxy-1-oxa-2,7-diaza-7,10-ethanospiro[4.5]dec-2-ene sesquifumarate (±)-1 was previously characterized as the most selective agonist at α7 neuronal nicotinic acetylcholine receptors in a series of spirocyclic quinuclidinyl-Δ2-isoxazoline derivatives. In this study, we performed different in vitro biological assays aimed at characterizing the ADMET properties of (±)-1. Then, we tested the compound in vivo in behavioral studies including classical novel object recognition and inhibitory avoidance tests in the rat, and a spatial memory assay in zebrafish involving a rapid T-maze task. The results indicated an overall favorable profile for (±)-1 in view of potential therapeutic applications targeting the central nervous system.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 820, 5 February 2018, Pages 265-273
نویسندگان
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