中国新药杂志

μ/δ阿片受体双重激动剂研究进展

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李京 ¹^,² , 任凤霞 ¹^,² , 史卫国 ¹^,²

中国新药杂志 | 重大新药创制专项巡礼 2021,30(23): 2166-2172

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中国新药杂志 |重大新药创制专项巡礼 2021 , 30 (23) : 2166 -2172

μ/δ阿片受体双重激动剂研究进展

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李京¹^,², 任凤霞¹^,², 史卫国¹^,²

作者信息

¹天津大学化工学院，天津　300350

²军事科学院军事医学研究院毒物药物研究所，北京　100850

通讯作者:

史卫国，男，研究员，研究方向：新药设计与合成。联系电话：（010）66931639，E-mail：shiwg1988@126.com。

作者简介:

李京，女，硕士研究生，研究方向：新药设计与合成。E-mail：lijing0950@163.com。

Research progress of dual μ/δ opioid receptor agonists

Jing LI¹^,², Feng-xia REN¹^,², Wei-guo SHI¹^,²

Affiliations

¹School of Chemical Engineering and Technology, Tianjin University, Tianjin 300350, China

²State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology & Toxicology, Beijing 100850, China

出版时间: 2021-12-15

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摘要

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阿片类镇痛药对于中度至重度剧烈疼痛的治疗仍不可替代，但由于其产生的成瘾性等不良反应，使用受到限制，临床急需新一代高效安全的阿片类镇痛药。目前有关μ与δ阿片受体间的相互调节作用的研究被大量报道，μ/δ二聚体的存在也为受体的相互作用提供了分子基础，设计具有μ/δ双重激动效应的分子是新一代具有强镇痛作用同时减少不良反应阿片类药物的发展方向。本文按照μ/δ双重激动分子设计策略分类，综述了近年来μ/δ双重激动剂的研究进展。

关键词

μ-δ相互调节作用 / 多靶点配体 / μ/δ双重激动剂 / 高效安全镇痛药

Abstract

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Opioid analgesics are still irreplaceable for the treatment of moderate to severe pain, but the usage is limited because of their dependence and other adverse reactions. There is an urgent need for a new generation of efficient and safe opioid analgesics. At present, many studies on the interaction between μ and δ opioid receptors have been reported, and the existence of μ/δ dimer also provides a molecular basis for the receptor interaction. The design of molecules with double activation effect on μ and δ types is the new development direction of opioid drugs with strong analgesic effect and little or weak adverse reactions. In this paper, the research progress of μ/δ dual agonists in recent years is reviewed according to the classification of design strategy of μ/δ dual agonist.

Key words

mutual regulation between μ and δ opioid receptors / multi-target ligands / dual μ/δ agonists / potent analgesics with diminished adverse effects

引用本文

李京, 任凤霞, 史卫国. μ/δ阿片受体双重激动剂研究进展. 中国新药杂志, 2021 , 30 (23) : 2166 -2172 .

Jing LI, Feng-xia REN, Wei-guo SHI. Research progress of dual μ/δ opioid receptor agonists[J]. Chinese Journal of New Drugs, 2021 , 30 (23) : 2166 -2172 .

基金

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国家“重大新药创制”科技重大专项资助项目(2012ZX09301003)
北京市科技计划课题(Z131100002713004)

参考文献

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2021年第30卷第23期

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首发时间：2026-10-28
出版时间：2021-12-15

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录用日期：2021-08-09

基金

国家“重大新药创制”科技重大专项资助项目(2012ZX09301003)

北京市科技计划课题(Z131100002713004)

作者信息

¹天津大学化工学院，天津　300350

²军事科学院军事医学研究院毒物药物研究所，北京　100850

通讯作者:

史卫国，男，研究员，研究方向：新药设计与合成。联系电话：（010）66931639，E-mail：shiwg1988@126.com。

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2种不同金属材料的力学参数

科 Family	属数 Number of genus	种数 Number of species	占总种数比例 Percentage of total species (%)	属 Genus	种数 Number of species	占总种数比例 Percentage of total species (%)
鹅膏菌科Amanitaceae	2	11	5.26	鹅膏菌属 Amanita	10	4.78
小菇科 Mycenaceae	2	12	5.74	丝盖伞属 Inocybe	5	2.39
多孔菌科 Polyporaceae	8	14	6.70	蜡蘑属 Laccaria	5	2.39
红菇科 Russulaceae	3	23	11.00	小皮伞属 Marasmius	6	2.87
				小菇属 Mycena	11	5.26
				光柄菇属 Pluteus	5	2.39
				红菇属 Russula	17	8.13
				栓菌属 Trametes	5	2.39

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