Butyrfentanyl
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Butyrfentanyl or butyrylfentanyl is a potent short-acting synthetic opioid analgesic drug. It is an analog of fentanyl with around one quarter of its potency. One of the first mentions of this drug can be found in document written by The College on Problem of Drug Dependence, where it is mentioned as N-butyramide fentanyl analog.[1] This document also states that the article describing its clinical effects (analgesic studies, μ-, δ-, κ-opioid receptor binding, and in vitro measures of drug efficacy, antinociceptive, and narcotic properties) was published in 1987. It is an agonist for the μ-opioid receptors.[2]
Butyrfentanyl has no current legitimate clinical applications; however, it is being sold as a designer drug.[3]
Side effects of fentanyl analogs are similar to those of fentanyl itself, which include
Pharmacokinetics
Butyrfentanyl binds to the opioid receptor. During the studies of
The opioid
Studies on urinary excretion revealed that almost all of the injected butyrfentanyl was excreted or metabolized within the first 3 hours after injection, and only very low concentrations were still detectable after 3 hours.
Legal status
There was a proposal being discussed by the UN Commission on Narcotic Drugs (CND) to include butyrfentanyl in Schedule 1 of the 1961 Single Convention on Narcotic Drugs which was passed 16 March 2017.[5]
United Kingdom
Butyrfentanyl is illegal in the United Kingdom as it is a modification of fentanyl "by replacement of the N-propionyl group by another acyl group".
United States
As of May 2016, butyrfentanyl is a Schedule I controlled substance in the United States.[6]
China
As of October 2015, butyrfentanyl is a controlled substance in China.[7]
Switzerland
Butyrfentanyl is illegal in Switzerland as of December 2015.[8]
See also
- 3-Methylbutyrfentanyl
- 4-Fluorobutyrfentanyl
- 4-Fluorofentanyl
- α-Methylfentanyl
- Acetylfentanyl
- Benzylfentanyl
- Furanylfentanyl
- Homofentanyl
- List of fentanyl analogues
References
- ^ "The College on Problem of Drug Dependence" (PDF). Archived from the original (PDF) on 19 December 2013., Foreword to the Drug Evaluation Committee (DEC) Analgesic, Stimulant, and Depressant Drug Indices
- ^ a b c d e Alburges ME (June 1988). Utilization of a radioreceptor assay for the analysis of fentanyl analogs in urine (PDF) (Ph.D. thesis). The University of Utah. Archived from the original (PDF) on 19 December 2013.
- PMID 26683128.
- PMID 25976511.
- ^ "Inclusion of butyrfentanyl in Schedule I of the Single Convention on Narcotic Drugs of 1961 as amended by the 1972 Protocol" (PDF).
- ^ "Schedules of Controlled Substances: Temporary Placement of Butyryl Fentanyl and Beta-Hydroxythiofentanyl into Schedule I" (PDF). Drug Enforcement Administration. 12 May 2016.
- ^ "关于印发《非药用类麻醉药品和精神药品列管办法》的通知" [Notice on Issuing the Measures for the Listing and Control of Non-Medicinal Narcotic Drugs and Psychotropic Substances] (in Chinese). China Food and Drug Administration. 27 September 2015. Archived from the original on 1 October 2015. Retrieved 1 October 2015.
- ^ "Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien" [EDI regulation on the lists of narcotics, psychotropic substances, precursor substances and auxiliary chemicals] (in German). Der Bundesrat.
Further reading
- Higashikawa Y, Suzuki S (June 2008). "Studies on 1-(2-phenethyl)-4-(N-propionylanilino)piperidine (fentanyl) and its related compounds. VI. Structure-analgesic activity relationship for fentanyl, methyl-substituted fentanyls and other analogues". Forensic Toxicology. 26 (1): 1–5. S2CID 22092512.
- Alburges ME, Hanson GR, Gibb JW, Sakashita CO, Rollins DE (1992). "Fentanyl receptor assay. II. Utilization of a radioreceptor assay for the analysis of fentanyl analogs in urine". Journal of Analytical Toxicology. 16 (1): 36–41. PMID 1322477.
- Woods J, Medzihradsky F, Smith C, Winger G, Gmerek D (1988). "Evaluation of new compounds for opioid activity: 1987 annual report". NIDA Research Monograph. 81: 543–590. PMID 3136388.
- Aceto M, Bowman E, Harris L, May E (1988). "Dependence studies of new compounds in the rhesus monkey, rat, and mouse, 1987". NIDA Research Monograph. 81: 485–542. PMID 3136386.
- Brine GA, Boldt KG, Huang PT, Sawyer DK, Carroll FI (2009). "Carbon-13 nuclear magnetic resonance spectra of fentanyl analogs". Journal of Heterocyclic Chemistry. 26 (3): 677–686. .