文章摘要
沈 坤,陈 云,匡雨琼,李 飞.nNOS-PSD-95解耦联剂和加巴喷丁、普瑞巴林孪药的设计合成[J].南京医科大学学报,2014,(10):1441~1445
nNOS-PSD-95解耦联剂和加巴喷丁、普瑞巴林孪药的设计合成
Design and synthesis of twin drug with nNOS-PSD-95 interrupts and gabapentin,pregebalin
投稿时间:2014-05-29  
DOI:10.7655/NYDXBNS20141039
中文关键词: nNOS-PSD-95解耦联剂  加巴喷丁  普瑞巴林  孪药  神经病理性疼痛
英文关键词: nNOS-PSD-95 interrupts  gabapentin  pregebalin  twin drug  neuropathic pain
基金项目:国家自然科学基金(21172108);江苏省自然科学基金(BK2011772)
作者单位
沈 坤 南京医科大学药学院,江苏 南京 211166 
陈 云 南京医科大学药学院,江苏 南京 211167 
匡雨琼 南京医科大学药学院,江苏 南京 211168 
李 飞 南京医科大学药学院,江苏 南京 211169 
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中文摘要:
      目的:设计合成nNOS-PSD-95解耦联剂和加巴喷丁?普瑞巴林的孪药,获得新型神经病理性疼痛治疗药物?方法:将 nNOS-PSD-95解耦联剂及其类似物与加巴喷丁?普瑞巴林以酰胺连接,用神经病理性疼痛模型评价目标化合物的镇痛作用?结果:所有目标化合物具有程度不同的神经病理性疼痛的镇痛作用,nNOS-PSD-95解耦联剂和加巴喷丁?普瑞巴林的孪药对神经病理性疼痛的镇痛作用强于单靶点药物?结论:nNOS-PSD-95解耦联剂和加巴喷丁?普瑞巴林的孪药比单靶点药物对神经病理性疼痛具有更好的镇痛作用?
英文摘要:
      Objective:To design and compound of twin drug with nNOS-PSD-95 interrupts and gabapentin,pregebalin,and to find new drugs for the treatment of neuropathic pain. Methods:The nNOS-PSD-95 interrupts and gabapentin,pregebalin were connected to form amide. The analgesic effects of target compounds were evaluated by neuropathic pain model. Results:All target compounds showed different degree analgesic effects in neuropathic pain, the analgesic effect of twin drug of nNOS-PSD-95 interrupts and gabapentin,pregabalin twin drug in neuropathic pain was stronger than that of single target drugs. Conclusion:Twin drug with nNOS-PSD-95 interrupts and gabapentin,pregebalin may get a better analgesic effect than that of single target drugs in neuropathic pain.
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