Article(id=1321426291530772765, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1321426285826519296, articleNumber=null, orderNo=null, doi=10.20251/j.cnki.1003-3734.2026.16.007, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1759939200000, acceptedDateStr=2025-10-09, onlineDate=1792982178814, onlineDateStr=2026-10-26, pubDate=1788019200000, pubDateStr=2026-08-30, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1792982178814, onlineIssueDateStr=2026-10-26, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1792982178814, creator=13701087609, updateTime=1792982178814, updator=13701087609, issue=Issue{id=1321426285826519296, tenantId=1146029695717560320, journalId=1235980733773295621, year='2026', volume='35', issue='16', pageStart='1681', pageEnd='1792', issueExtLink='null', onlineDate='null', pubDate='1788019200000', pubDateStr='2026-08-30', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1792982177454, creator='13701087609', updateTime=1792982881356, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1321429238297776921, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1321426285826519296, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1321429238297776922, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1321426285826519296, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=1728, endPage=1735, ext={EN=ArticleExt(id=1321426291778236702, articleId=1321426291530772765, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Advances in κ-opioid receptor selective agonist analgesics, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=

To identify safer and more effective opioid analgesics, κ-opioid receptor (KOR) selective agonists have been widely investigated for their potent analgesic properties and lack of the abuse liability typically associated with μ-opioid receptor activation. The clinical approval of the peptide-based drug difelikefalin (Korsuva) established a pivotal milestone, creating new pathways for the therapeutic application of KOR-selective agonists. Subsequently, diverse compound scaffolds, including small molecules and peptides, along with innovative research approaches, have been systematically explored through experimental studies. This review examines the latest chemical advancements and challenges related to KOR agonists, as well as their clinical and potential applications.

, authors=Ming YUAN1, 2, Qing LI2, Chao WANG2, Wei-guo SHI2, *, Chun HU1, *, authorsList=Ming YUAN, Qing LI, Chao WANG, Wei-guo SHI, Chun HU, authorCompany=null, correspAuthors=Wei-guo SHI, Chun HU, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1321426292138946847, articleId=1321426291530772765, tenantId=1146029695717560320, journalId=1235980733773295621, language=CN, title=κ-阿片受体选择性激动剂类镇痛药物研究进展, columnId=1236330553964810454, journalTitle=中国新药杂志, columnName=综述, runingTitle=null, highlight=null, articleAbstract=

为了开发更安全有效的新型阿片类镇痛药物,κ-阿片受体(κ-opioid receptor, KOR)选择性激动剂因其显著的镇痛效果和避免μ-阿片受体相关的滥用风险而备受瞩目。多肽类药物地非法林(difelikefalin,商品名为Korsuva)的上市为KOR选择性激动剂的临床应用开辟了新的领域,更多的小分子和多肽等新化合物的结构和研究策略逐渐受到重视。本文综述了KOR激动剂的最新化学进展和面临挑战,并探讨其临床应用和潜在的治疗前景,以期为后续的阿片受体新药设计提供新的选择。

, authors=袁明1, 2, 李晴2, 王潮2, 史卫国2, *, 胡春1, *, authorsList=袁明, 李晴, 王潮, 史卫国, 胡春, authorCompany=null, correspAuthors=史卫国, 胡春, authorNote=

袁明,男,硕士研究生,研究方向:多肽药物的药物化学研究。E-mail: 。

, correspAuthorsNote=
* 史卫国,男,研究员,博士生导师,研究方向:新药设计与合成。联系电话:(010)66931639,E-mail: 。
* 胡春,男,教授,博士生导师,研究方向:靶向药物研究。联系电话:(024)23986403,E-mail: 。
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袁明,男,硕士研究生,研究方向:多肽药物的药物化学研究。E-mail: 。

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κ-阿片受体选择性激动剂类镇痛药物研究进展
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袁明 1, 2 , 李晴 2 , 王潮 2 , 史卫国 2, * , 胡春 1, *
中国新药杂志 | 综述 2026,35(16): 1728-1735
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中国新药杂志 |综述 2026 , 35 (16) : 1728 -1735
κ-阿片受体选择性激动剂类镇痛药物研究进展
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袁明1, 2 , 李晴2, 王潮2, 史卫国2, * , 胡春1, *
作者信息
  • 1沈阳药科大学,沈阳 117004
  • 2军事医学研究院,北京 100850
通讯作者:
* 史卫国,男,研究员,博士生导师,研究方向:新药设计与合成。联系电话:(010)66931639,E-mail: 。
* 胡春,男,教授,博士生导师,研究方向:靶向药物研究。联系电话:(024)23986403,E-mail: 。
作者简介:

袁明,男,硕士研究生,研究方向:多肽药物的药物化学研究。E-mail: 。

Advances in κ-opioid receptor selective agonist analgesics
Ming YUAN1, 2 , Qing LI2, Chao WANG2, Wei-guo SHI2, * , Chun HU1, *
Affiliations
  • 1Shenyang Pharmaceutical University, Shenyang 117004, China
  • 2Academy of Military Medical Sciences, Beijing 100850, China
出版时间: 2026-08-30 doi: 10.20251/j.cnki.1003-3734.2026.16.007
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为了开发更安全有效的新型阿片类镇痛药物,κ-阿片受体(κ-opioid receptor, KOR)选择性激动剂因其显著的镇痛效果和避免μ-阿片受体相关的滥用风险而备受瞩目。多肽类药物地非法林(difelikefalin,商品名为Korsuva)的上市为KOR选择性激动剂的临床应用开辟了新的领域,更多的小分子和多肽等新化合物的结构和研究策略逐渐受到重视。本文综述了KOR激动剂的最新化学进展和面临挑战,并探讨其临床应用和潜在的治疗前景,以期为后续的阿片受体新药设计提供新的选择。

阿片类药物  /  疼痛  /  κ-阿片受体  /  选择性激动剂  /  外周作用激动剂  /  镇痛作用

To identify safer and more effective opioid analgesics, κ-opioid receptor (KOR) selective agonists have been widely investigated for their potent analgesic properties and lack of the abuse liability typically associated with μ-opioid receptor activation. The clinical approval of the peptide-based drug difelikefalin (Korsuva) established a pivotal milestone, creating new pathways for the therapeutic application of KOR-selective agonists. Subsequently, diverse compound scaffolds, including small molecules and peptides, along with innovative research approaches, have been systematically explored through experimental studies. This review examines the latest chemical advancements and challenges related to KOR agonists, as well as their clinical and potential applications.

opioid drugs  /  pain  /  κ-opioid receptor  /  selective agonist  /  peripheral agonist  /  analgesic effect
袁明, 李晴, 王潮, 史卫国, 胡春. κ-阿片受体选择性激动剂类镇痛药物研究进展. 中国新药杂志, 2026 , 35 (16) : 1728 -1735 . DOI: 10.20251/j.cnki.1003-3734.2026.16.007
Ming YUAN, Qing LI, Chao WANG, Wei-guo SHI, Chun HU. Advances in κ-opioid receptor selective agonist analgesics[J]. Chinese Journal of New Drugs, 2026 , 35 (16) : 1728 -1735 . DOI: 10.20251/j.cnki.1003-3734.2026.16.007

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doi: 10.20251/j.cnki.1003-3734.2026.16.007
  • 首发时间:2026-10-26
  • 出版时间:2026-08-30
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  • 录用日期:2025-10-09
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作者信息
    1沈阳药科大学,沈阳 117004
    2军事医学研究院,北京 100850

通讯作者:

* 史卫国,男,研究员,博士生导师,研究方向:新药设计与合成。联系电话:(010)66931639,E-mail: 。
* 胡春,男,教授,博士生导师,研究方向:靶向药物研究。联系电话:(024)23986403,E-mail: 。
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2种不同金属材料的力学参数
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genus
种数
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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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