Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.

Autor:	Hsu FL; United States Army CCDC Chemical Biological Center, Aberdeen Proving Ground, Maryland, United States., Walz AJ; United States Army CCDC Chemical Biological Center, Aberdeen Proving Ground, Maryland, United States., Myslinski JM; United States Army CCDC Chemical Biological Center, Aberdeen Proving Ground, Maryland, United States., Kong L; United States Army CCDC Chemical Biological Center, Aberdeen Proving Ground, Maryland, United States., Feasel MG; United States Army CCDC Chemical Biological Center, Aberdeen Proving Ground, Maryland, United States., Goralski TDP; United States Army CCDC Chemical Biological Center, Aberdeen Proving Ground, Maryland, United States., Rose T; Defence Science and Technology Laboratory (Dstl), Porton Down, Salisbury, Wiltshire, U.K., Cooper NJ; Defence Science and Technology Laboratory (Dstl), Porton Down, Salisbury, Wiltshire, U.K., Roughley N; Defence Science and Technology Laboratory (Dstl), Porton Down, Salisbury, Wiltshire, U.K., Timperley CM; Defence Science and Technology Laboratory (Dstl), Porton Down, Salisbury, Wiltshire, U.K.
Jazyk:	angličtina
Zdroj:	ACS medicinal chemistry letters [ACS Med Chem Lett] 2019 Oct 16; Vol. 10 (11), pp. 1568-1572. Date of Electronic Publication: 2019 Oct 16 (Print Publication: 2019).
DOI:	10.1021/acsmedchemlett.9b00404
Abstrakt:	Carfentanil is a synthetic opioid significantly more potent than clinically prescribed fentanyl. The primary metabolites of carfentanil, generated from human liver microsomes, were structurally confirmed through chemical synthesis. The synthesized compounds were evaluated for μ-opioid receptor (MOR) functional activity. Of the six metabolites assayed, a major metabolite showed comparable activity to the parent opioid. Three other metabolites showed significant MOR functional activity. The availability of the metabolites could aid improvements in the analysis of biomedical samples obtained from suspected human exposures to carfentanil and development of treatment protocols. Competing Interests: The authors declare no competing financial interest. (Copyright © 2019 American Chemical Society.)
Databáze:	MEDLINE
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