کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587168 | 981425 | 2012 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Favourable involvement of α2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement
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کلمات کلیدی
MPEIBSadrenoreceptorm-CPBAm-chloroperbenzoic acid1,4-Dioxane nucleusCho - برایChinese Hamster Ovary - تخمدان هامستر چینیMaximum possible effect - حداکثر اثر ممکنCNS - دستگاه عصبی مرکزیImidazoline binding sites - سایت های مرتبط با ایمیدازولینcentral nervous system - سیستم عصبی مرکزیperipheral nervous system - سیستم عصبی پیرامونیPNS - کارمندان دولت
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Favourable involvement of α2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement Favourable involvement of α2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement](/preview/png/10587168.png)
چکیده انگلیسی
Aim of the present study was to obtain novel α2-adrenoreceptor (α2-AR) antagonists, possibly endowed with subtype-selectivity. Therefore, inspired by the non subtype-selective α2-AR antagonist idazoxan, we designed 1,4-dioxane derivatives bearing an aromatic area in position 5 or 6 and the imidazoline nucleus in position 2. Among the novel molecules 1-6, compound 2, with a trans stereochemical relationship between 5-phenyl and 2-imidazoline groups, was able to antagonize the sole α2A-subtype. Moreover, 2 showed an affinity at I2-imidazoline binding sites (I2-IBS) comparable to that at α2A-AR. In in vivo studies 2 strongly increased morphine analgesia. This interesting behaviour appeared to be induced by the favourable involvement of α2A-AR antagonism in the I2-IBS-mediated morphine analgesia enhancement.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 7, 1 April 2012, Pages 2259-2265
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 7, 1 April 2012, Pages 2259-2265
نویسندگان
Valerio Mammoli, Alessandro Bonifazi, Fabio Del Bello, Eleonora Diamanti, Mario Giannella, Alan L. Hudson, Laura Mattioli, Marina Perfumi, Alessandro Piergentili, Wilma Quaglia, Federica Titomanlio, Maria Pigini,