کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
6283367 | 1615154 | 2013 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The discovery of 071031B, a novel serotonin and noradrenaline reuptake inhibitor
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کلمات کلیدی
5-HTSerotonin and Norepinephrine Reuptake InhibitorsSNRIsNRIsTCAsSSRIsTSTFSTLD50NETs - NET هاForced swimming test - آزمون اجباری شناTail suspension test - آزمون تعلیق دمR&D - تحقیق و توسعهResearch & development - تحقیق و توسعهANOVA - تحلیل واریانس Analysis of varianceone-way analysis of variance - تحلیل واریانس یک راههNorepinephrine transporters - حمل کننده های نوراپی نفرینSerotonin transporters - حملونقل سروتونینAntidepressants - داروهای ضد افسردگیtricyclic antidepressants - داروهای ضد افسردگی سه حلقه ایCNS - دستگاه عصبی مرکزیSerotonin - سروتونینcentral nervous system - سیستم عصبی مرکزیselective serotonin reuptake inhibitors - مهار کننده های بازجذب سروتونین انتخابیMonoamine oxidase inhibitors - مهار کننده های مونوآمین اکسیدازnorepinephrine reuptake inhibitors - مهارکننده های بازجذب نوراپی نفرینMonoamine transporters - مونوآمین ها
موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب (عمومی)
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
Depression is a severe mood disorder with increasing morbidity and suicidality, while the current therapy is not satisfactory. Serotonin and noradrenaline reuptake inhibitors (SNRIs) have been reported to have higher efficacy and/or faster acting rate than commonly used antidepressants. The present study was designed to screen the potential SNRIs, using in vitro radioligand receptor binding assays and in vivo animal tests, and introduced the discovery of 071031B. In the tail suspension test and forced swimming test in mice, six compounds (071017S, 071026W, 071031A, 071031B, 080307A and 080307B) showed robust antidepressant activity, without stimulant effect on the locomotor activity or other side effects, and the minimal effective dose of 071017S, 071026W, 071031A and 071031B was less than that of duloxetine; in vitro binding tests indicated that 071031B had high affinity to both serotonin transporter and noradrenaline transporter with similar inhibitory rates to duloxetine at 1 and 100Â nM; acute toxicity test indicated that the LD50 value of 071031B was similar to that of duloxetine. These findings demonstrated that this integrated system, combining high throughput screening technology and in vivo animal tests, is effective to screen potential monoamine reuptake inhibitors fast and accurately; 071031B is expected to be a novel serotonin and noradrenaline reuptake inhibitor for its robust antidepressant activity and transporter affinity.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Neuroscience Letters - Volume 544, 7 June 2013, Pages 68-73
Journal: Neuroscience Letters - Volume 544, 7 June 2013, Pages 68-73
نویسندگان
Rui Xue, Yan-Ping Zhang, Zeng-Liang Jin, Li Yuan, Xin-Hua He, Nan Zhao, Hong-Xia Chen, Li-Ming Zhang, Shi-Yong Fan, Bo-Hua Zhong, You-Zhi Zhang, Yun-Feng Li,