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• W2890761655 abstract "Abstract Synthetic cathinones continue to proliferate in clandestine drug markets worldwide. N ‐ethylnorpentylone (also known as N ‐ethylpentylone or ephylone) is a popular emergent cathinone, yet little information is available about its toxicology and pharmacology. Here we characterize the analytical quantification, clinical presentation, and pharmacological mechanism of action for N ‐ethylnorpentylone. Liquid chromatography coupled to tandem mass spectrometry (LC–MS/MS) was used to quantify N ‐ethylnorpentylone in blood obtained from human cases. Clinical features exhibited by the intoxicated individuals are described. The activity of N ‐ethylnorpentylone at plasma membrane transporters for dopamine (DAT), norepinephrine (NET) and 5‐HT (SERT) was assessed using in vitro assays measuring uptake inhibition and evoked release of [ 3 H] neurotransmitters in rat brain synaptosomes. Our LC–MS/MS method assayed N ‐ethylnorpentylone concentrations with limits of detection and quantification of 1 and 5 ng/mL, respectively. Quantitation was linear from 5 to 500 ng/mL, and the method displayed specificity and reproducibility. Circulating concentrations of N ‐ethylnorpentylone ranged from 7 to 170 ng/mL in clinical cases, and the associated symptoms included palpitations, tachycardia, agitation, hallucinations, coma and death. N‐ Ethylnorpentylone was a potent inhibitor at DAT (IC 50 = 37 nM), NET (IC 50 = 105 nM) and SERT (IC 50 = 383 nM) but displayed no transporter releasing activity. We present a validated method for quantifying N ‐ethylnorpentylone in human case work. The drug is a psychomotor stimulant capable of inducing serious cardiovascular and neurological side‐effects which can be fatal. In vitro findings indicate that N ‐ethylnorpentylone exerts its effects by potent blockade of DAT and NET, thereby elevating extracellular levels of dopamine and norepinephrine in the brain and periphery." @default.
• W2890761655 created "2018-09-27" @default.
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• W2890761655 date "2018-10-21" @default.
• W2890761655 modified "2023-10-05" @default.
• W2890761655 title "Analytical quantification, intoxication case series, and pharmacological mechanism of action for <i>N</i> ‐ethylnorpentylone ( <i>N</i> ‐ethylpentylone or ephylone)" @default.
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• W2890761655 doi "https://doi.org/10.1002/dta.2502" @default.
• W2890761655 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7316160" @default.
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• W2890761655 hasPublicationYear "2018" @default.
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