Abstract:
Purpose:A detailed review on the chemistry and pharmacology of non-fentanil novel synthetic opioid receptor agonists, particularly N-substituted benzamides and acetamides (known colloquially as U-drugs) and 4-aminocyclohexanols, developed at the Upjohn Company in the 1970s and 1980s is presented. Method:Peer-reviewed literature, patents, professional literature, data from international early warning systems and drug user fora discussion threads have been used to track their emergence as substances of abuse. Results:In terms of impact on drug markets, prevalence and harm, the most significant compound of this class to date has been U-47700 (trans-3,4-dichloro-N-[2-(dimethylamino)cyclohexyl]-N-methylbenzamide), reported by users to give short-lasting euphoric effects and a desire to re-dose. Since U-47700 was internationally controlled in 2017, a range of related compounds with similar chemical structures, adapted from the original patented compounds, have appeared on the illicit drugs market. Interest in a structurally unrelated opioid developed by the Upjohn Company and now known as BDPC/bromadol appears to be increasing and should be closely monitored. Conclusions:International early warning systems are an essential part of tracking emerging psychoactive substances and allow responsive action to be taken to facilitate the gathering of relevant data for detailed risk assessments. Pre-emptive research on the most likely compounds to emerge next, so providing drug metabolism and pharmacokinetic data to ensure that new substances are detected early in toxicological samples is recommended. As these compounds are chiral compounds and stereochemistry has a large effect on their potency, it is recommended that detection methods consider the determination of configuration.
journal_name
Forensic Toxicoljournal_title
Forensic toxicologyauthors
Sharma KK,Hales TG,Rao VJ,NicDaeid N,McKenzie Cdoi
10.1007/s11419-018-0454-5subject
Has Abstractpub_date
2019-01-01 00:00:00pages
1-16issue
1eissn
1860-8965issn
1860-8973pii
454journal_volume
37pub_type
杂志文章,评审abstract::We identified four cannabimimetic indazole and indole derivatives in new illegal psychoactive substances seized from a clandestine laboratory in China. These four derivatives included N-(1-amino-3,3-dimethyl-1-oxobutan-2-yl)-1-benzyl-1H-indazole-3-carboxamide (ADB-BINACA, 1), N-(1-amino-3-methyl-1-oxobutan-2-yl)-1-(4-...
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doi:10.1007/s11419-015-0297-2
更新日期:2016-01-01 00:00:00
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journal_title:Forensic toxicology
pub_type: 杂志文章,评审
doi:10.1007/s11419-017-0379-4
更新日期:2018-01-01 00:00:00
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journal_title:Forensic toxicology
pub_type: 杂志文章
doi:10.1007/s11419-017-0361-1
更新日期:2017-01-01 00:00:00
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journal_title:Forensic toxicology
pub_type: 杂志文章
doi:10.1007/s11419-015-0280-y
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journal_title:Forensic toxicology
pub_type: 杂志文章
doi:10.1007/s11419-018-0449-2
更新日期:2019-01-01 00:00:00
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pub_type: 杂志文章
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更新日期:2018-01-01 00:00:00
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pub_type: 杂志文章
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更新日期:2017-01-01 00:00:00