• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

盐酸曲马多的手性转换,一种潜在的致幻药物——过去与未来

Chiral Switches of Tramadol Hydrochloride, a Potential Psychedelic Drug-Past and Future.

作者信息

Agranat Israel, D'Acquarica Ilaria

机构信息

Organic Chemistry, Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Jerusalem 9190401, Israel.

Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Rome 00185, Italy.

出版信息

ACS Med Chem Lett. 2024 Aug 7;15(9):1409-1416. doi: 10.1021/acsmedchemlett.4c00322. eCollection 2024 Sep 12.

DOI:10.1021/acsmedchemlett.4c00322
PMID:39291005
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11403737/
Abstract

The chiral opioid analgesic tramadol was patented (1962) as a - and -racemates mixture. A first chiral switch led to the (±)--(1,2) racemate, patented and approved as Tramal (1980), preferred over the (+)--(1,2)-enantiomer. Consecutive chiral switches of (±)--tramadol to (+)--(1,2)-tramadol/salts were patented. This Viewpoint calls for developing (+)--(1,2)-tramadol medicines and recognizing tramadol medicines as potential psychedelics to overcome the spreading tramadol crisis.

摘要

手性阿片类镇痛药曲马多在1962年获得专利,是一种左旋和右旋对映体的混合物。首次手性转换产生了(±)-(1,2)-对映体混合物,获得专利并被批准为曲马朵(1980年),比(+)-(1,2)-对映体更受青睐。(±)-曲马多连续手性转换为(+)-(1,2)-曲马多/盐类也获得了专利。本文观点呼吁开发(+)-(1,2)-曲马多药物,并将曲马多药物视为潜在的致幻剂,以克服日益蔓延的曲马多危机。

相似文献

1
Chiral Switches of Tramadol Hydrochloride, a Potential Psychedelic Drug-Past and Future.盐酸曲马多的手性转换,一种潜在的致幻药物——过去与未来
ACS Med Chem Lett. 2024 Aug 7;15(9):1409-1416. doi: 10.1021/acsmedchemlett.4c00322. eCollection 2024 Sep 12.
2
Prescription of Controlled Substances: Benefits and Risks管制药品的处方:益处与风险
3
Tramadol with or without paracetamol (acetaminophen) for cancer pain.曲马多联合或不联合对乙酰氨基酚用于癌症疼痛治疗
Cochrane Database Syst Rev. 2017 May 16;5(5):CD012508. doi: 10.1002/14651858.CD012508.pub2.
4
Tramadol for neuropathic pain in adults.曲马多用于成人神经性疼痛。
Cochrane Database Syst Rev. 2017 Jun 15;6(6):CD003726. doi: 10.1002/14651858.CD003726.pub4.
5
Psychedelic-assisted therapy for treating anxiety, depression, and existential distress in people with life-threatening diseases.致幻剂辅助治疗对患有危及生命疾病的人群的焦虑、抑郁和存在性困扰的治疗作用。
Cochrane Database Syst Rev. 2024 Sep 12;9(9):CD015383. doi: 10.1002/14651858.CD015383.pub2.
6
Correlation Between Opioid Drug Prescription and Opioid-Related Mortality in Spain as a Surveillance Tool: Ecological Study.西班牙阿片类药物处方与阿片类相关死亡率的相关性作为监测工具:生态学研究。
JMIR Public Health Surveill. 2023 Jun 28;9:e43776. doi: 10.2196/43776.
7
Tramadol for postoperative pain treatment in children.曲马多用于儿童术后疼痛治疗。
Cochrane Database Syst Rev. 2015 Mar 18;2015(3):CD009574. doi: 10.1002/14651858.CD009574.pub2.
8
Thermal antinociceptive effect of transdermal tramadol hydrochloride in avian.盐酸曲马多经皮给药对禽类的热镇痛作用。
J Vet Med Sci. 2025 Aug 1;87(8):947-953. doi: 10.1292/jvms.25-0009. Epub 2025 Jul 1.
9
Psychedelic use in individuals living with eating disorders or disordered eating: findings from the international MED-FED survey.饮食失调或进食紊乱个体使用迷幻剂的情况:国际MED-FED调查结果
J Eat Disord. 2025 Jul 24;13(1):152. doi: 10.1186/s40337-025-01328-5.
10
Tramadol overdose in total knee arthroplasty: A case report.全膝关节置换术中曲马多过量:一例报告。
World J Clin Cases. 2025 Sep 6;13(25):104742. doi: 10.12998/wjcc.v13.i25.104742.

引用本文的文献

1
Biochemical and Histopathological Alterations Induced by Tramadol.曲马多引起的生化和组织病理学改变。
Med J Islam Repub Iran. 2025 Feb 26;39:31. doi: 10.47176/mjiri.39.31. eCollection 2025.
2
A call to develop tramadol enantiomer for overcoming the tramadol crisis by reducing addiction.呼吁开发曲马多对映体以通过减少成瘾来克服曲马多危机。
Future Med Chem. 2025 Mar;17(5):505-507. doi: 10.1080/17568919.2025.2463314. Epub 2025 Feb 11.

本文引用的文献

1
Chirality of New Drug Approvals (2013-2022): Trends and Perspectives.新药批准的手性(2013-2022):趋势与展望。
J Med Chem. 2024 Feb 22;67(4):2305-2320. doi: 10.1021/acs.jmedchem.3c02239. Epub 2024 Feb 12.
2
Anti-infectives Developed as Racemic Drugs in the 21st Century: Norm or Exception?21世纪开发的外消旋体抗感染药物:常态还是例外?
ACS Med Chem Lett. 2023 Jun 12;14(7):875-878. doi: 10.1021/acsmedchemlett.3c00214. eCollection 2023 Jul 13.
3
Pharmacovigilance Signals of the Opioid Epidemic over 10 Years: Data Mining Methods in the Analysis of Pharmacovigilance Datasets Collecting Adverse Drug Reactions (ADRs) Reported to EudraVigilance (EV) and the FDA Adverse Event Reporting System (FAERS).十年阿片类药物流行的药物警戒信号:用于分析向欧洲药品不良反应数据库(EudraVigilance,EV)和美国食品药品监督管理局不良事件报告系统(FAERS)报告的药物不良反应(ADR)的药物警戒数据集的数据挖掘方法
Pharmaceuticals (Basel). 2022 May 27;15(6):675. doi: 10.3390/ph15060675.
4
Tramadol-associated hallucinations: a systematic review and narrative synthesis of their pathophysiology, diagnosis, and treatment.曲马多相关性幻觉:对其病理生理学、诊断和治疗的系统回顾和叙述性综合。
Can J Anaesth. 2020 Mar;67(3):360-368. doi: 10.1007/s12630-019-01548-9. Epub 2019 Dec 16.
5
An overview of tramadol and its usage in pain management and future perspective.曲马多概述及其在疼痛管理中的应用和未来展望。
Biomed Pharmacother. 2019 Mar;111:443-451. doi: 10.1016/j.biopha.2018.12.085. Epub 2018 Dec 27.
6
Psychedelics.迷幻剂
Pharmacol Rev. 2016 Apr;68(2):264-355. doi: 10.1124/pr.115.011478.
7
Schedule of controlled substances: placement of tramadol into schedule IV. Final rule.受管制物质清单:将曲马多列入第四类。最终规则。
Fed Regist. 2014 Jul 2;79(127):37623-30.
8
The predicated demise of racemic new molecular entities is an exaggeration.外消旋新分子实体注定会消亡的说法有些夸张。
Nat Rev Drug Discov. 2012 Dec;11(12):972-3. doi: 10.1038/nrd3657-c1.
9
The strategy of enantiomer patents of drugs.药物对映异构体专利策略。
Drug Discov Today. 2010 Mar;15(5-6):163-70. doi: 10.1016/j.drudis.2010.01.007. Epub 2010 Jan 29.
10
Trends in the development of chiral drugs.手性药物的发展趋势。
Drug Discov Today. 2004 Feb 1;9(3):105-10. doi: 10.1016/s1359-6446(03)02904-0.