Pharmacodynamics and pharmacokinetics of the novel synthetic opioid, U-47700, in male rats.

Neuropharmacology
Michael T TruverMichael H Baumann

Abstract

Novel synthetic opioids are appearing in recreational drug markets worldwide as adulterants in heroin or ingredients in counterfeit analgesic medications. Trans-3,4-dichloro-N-[2-(dimethylamino)cyclohexyl]-N-methyl-benzamide (U-47700) is an example of a non-fentanyl synthetic opioid linked to overdose deaths. Here, we examined the pharmacodynamics and pharmacokinetics of U-47700 in rats. Male Sprague-Dawley rats were fitted with intravenous (i.v.) catheters and subcutaneous (s.c.) temperature transponders under ketamine/xylazine anesthesia. One week later, rats received s.c. injections of U-47700 HCl (0.3, 1.0 or 3.0 mg/kg) or saline, and blood samples (0.3 mL) were withdrawn via i.v. catheters at 15, 30, 60, 120, 240, 480 min post-injection. Pharmacodynamic effects were assessed at each blood withdrawal, and plasma was assayed for U-47700 and its metabolites by liquid chromatography tandem mass spectrometry. U-47700 induced dose-related increases in hot plate latency (ED50 = 0.5 mg/kg) and catalepsy (ED50 = 1.7 mg/kg), while the 3.0 mg/kg dose also caused hypothermia. Plasma levels of U-47700 rose linearly as dose increased, with maximal concentration (Cmax) achieved by 15-38 min. Cmax values for N-desmethyl-U-47700 and N,N-di...Continue Reading

References

May 1, 1997·Clinical and Experimental Pharmacology & Physiology·J T van CrugtenG Reynolds
Jul 17, 2009·Pharmacological Reports : PR·Ewa TarachaAdam Płaźnik
Aug 28, 2010·The Journal of Pain : Official Journal of the American Pain Society·Amanda GunnMichael M Morgan
Aug 24, 2016·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Matthew J JonesSamuel J Stellpflug
Oct 14, 2016·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Kathy T VoRaymond Y Ho
Apr 13, 2017·International Journal of Legal Medicine·Marek DziadoszJörg Teske
Jun 8, 2017·Journal of Addiction Medicine·Matthew P PrekupecMichael H Baumann
Oct 7, 2017·Journal of Analytical Toxicology·Kayla N EllefsenBrad J Hall
Oct 19, 2017·Journal of Analytical Toxicology·Timothy P RohrigTyson R Baird
May 11, 2018·Current Pharmaceutical Biotechnology·Susanna VogliardiDonata Favretto
Jun 27, 2018·Journal of Analytical Toxicology·Emma PartridgeChris Kostakis
Jul 26, 2018·Frontiers in Pharmacology·Enrico GeraceMarco Vincenti
Sep 20, 2018·Journal of Forensic Sciences·Monika ŽidkováTomáš Hložek
Sep 30, 2018·The Journal of Pharmacology and Experimental Therapeutics·Jeremy CarlierMichael H Baumann
Nov 18, 2018·International Journal of Legal Medicine·Camille RichevalYvan Gaillard
Nov 21, 2018·Trends in Pharmacological Sciences·Michael H BaumannBertha K Madras
Mar 9, 2019·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Christina R SmithMadeleine J Swortwood
Sep 1, 2017·Academic Forensic Pathology·Donna PapsunBarry K Logan

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