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https://www.readbyqxmd.com/read/28927604/preparation-of-a-novel-chitosan-based-biosorbent-cross-linked-with-phenethylamine-for-adsorption-of-aromatic-amino-acids
#1
Wen Jiang, Yang Yang, Renyou Tao, Xiaoqin Jiang, Xiaohua Zhou, Zhiming Zhou
Rice protein was successively hydrolyzed by rice protein hydrolysis special enzyme, chymotrypsin and carboxypeptidases A. Then a novel chitosan-based biosorbent cross-linked with phenethylamine (PMCCR) was synthesized and firstly used for adsorption of aromatic amino acids (AAA) from rice protein enzymatic hydrolysates (RPEH). The characterizations of PMCCR indicated that phenethylamine was successfully cross-linked with chitosan, and the particle size of PMCCR was 500-1000μm with pore diameter of 50-100μm...
November 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28917801/development-of-a-quantitative-approach-in-blood-plasma-for-low-dosed-hallucinogens-and-opioids-using-lc-high-resolution-mass-spectrometry
#2
Achim T Caspar, Andreas B Kollas, Hans H Maurer, Markus R Meyer
The WHO annually reports an increasing abuse of new psychoactive substances (NPS), which are a heterogeneous group of synthetic drugs and are consumed as substitute for controlled drugs of abuse. In this work, we focused on highly potent derivatives such those of phenethylamine (2C), N-2-methoxybenzyl phenethylamine (NBOMes), lysergic acid diethylamide (LSD), and fentanyl. Severe to fatal intoxications were described due to their high potency. Therefore, they have to be taken at very low doses resulting in low blood concentration in the low ng/mL range, which is a challenge for reliable analytical detection and quantification...
January 1, 2018: Talanta
https://www.readbyqxmd.com/read/28890736/the-psychoactive-drug-25b-nbome-recapitulates-rhabdomyolysis-in-zebrafish-larvae
#3
Genri Kawahara, Hideyuki Maeda, Ruri Kikura-Hanajiri, Ken-Ichi Yoshida, Yukiko K Hayashi
N-Benzyl-substituted 2C class phenethylamines (NBOMes) are psychoactive designer drugs, with strong hallucinogenic and stimulant effects, even at low doses. The designer drug, 2-(4-bromo-2, 5-dimethoxyphenyl)-N-(2-methoxybenzyl) ethanamine (25B-NBOMe) is considered to be one of the most potent agonists of the serotonin-2A (5-HT2A) receptor. Recently, we reported the first lethal case of 25B-NBOMe intoxication with severe rhabdomyolysis, concluded by clinical, pathological and toxicological analyses. There are currently no good animal models that closely recapitulate serotonin receptor-dependent rhabdomyolysis...
2017: Forensic Toxicology
https://www.readbyqxmd.com/read/28885973/hemorrhagic-stroke-in-a-young-healthy-male-following-use-of-pre-workout-supplement-animal-rage-xl
#4
Brandon F Harris, Coty Winn, Thomas B Ableman
So-called "pre-workout" supplements are substances marketed as natural dietary supplements with claims of helping athletes achieve more focused and intense workouts. The use of such products remains popular among American youth as a whole, but is especially high among active duty service members. Supplements are minimally regulated by the Food and Drug Administration (FDA), and unlike pharmaceuticals, supplements are often brought to market without any testing to show neither efficacy nor safety. Several case reports have documented serious adverse events and raise the question of whether supplement use was a causative factor...
September 2017: Military Medicine
https://www.readbyqxmd.com/read/28877397/meta-selective-c-h-borylation-of-benzylamine-phenethylamine-and-phenylpropylamine-derived-amides-enabled-by-a-single-anionic-ligand
#5
Holly J Davis, Georgi R Genov, Robert Phipps
Selective functionalization at the meta position of arenes remains a significant challenge. In this work, we demonstrate that an anionic bipyridine ligand bearing a remote sulfonate group enables selective iridium-catalyzed borylation of a range of common amine-containing aromatic molecules at the arene meta position. We propose that this selectivity is the result of a key hydrogen bonding interaction between the substrate and catalyst. The scope of this meta-selective borylation is demonstrated on amides derived from benzylamines, phenethylamines and phenylpropylamines; amine-containing building blocks of great utility in many applications...
September 6, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28842491/conformational-state-interactions-provide-clues-to-the-pharmacochaperone-potential-of-serotonin-transporter-partial-substrates
#6
Shreyas Bhat, Peter S Hasenhuetl, Ameya Kasture, Ali El-Kasaby, Michael H Baumann, Bruce E Blough, Sonja Sucic, Walter Sandtner, Michael Freissmuth
Point mutations in SLC6 transporters cause misfolding, which can be remedied by pharmacochaperones. The serotonin transporter (SERT/SLC6A4) has a rich pharmacology including inhibitors, releasers (amphetamines, which promote the exchange mode) and more recently discovered partial substrates. We hypothesized that partial substrates trapped the transporter in one or several states of the transport cycle. This conformational trapping may also be conducive to folding. We selected napthylpropane-2-amines of the phenethylamine library (PAL) including the partial substrate PAL1045 and its congeners PAL287 and PAL1046...
August 23, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28830123/application-of-a-urine-and-hair-validated-lc-ms-ms-method-to-determine-the-effect-of-hair-color-on-the-incorporation-of-25b-nbome-25c-nbome-and-25i-nbome-into-hair-in-the-rat
#7
Lorna A Nisbet, Rafael Venson, Fiona M Wylie, Karen S Scott
NBOMes are a group of new psychoactive substances derived from phenethylamines. Recreational abuse is thought to have begun in 2010 and they are commonly associated with the "club drug" scene. They are administered in liquid form or as blotters due to their high potency. An LC-MS-MS method was validated using Scientific Working Group for Forensic Toxicology parameters for the detection of 25B-, 25C- and 4-iodo-2,5-dimethoxy-N-[(2-methoxyphenyl)methyl]-benzeneethanamine (25I-NBOMe) using 4-bromo-2,5-dimethoxy-N-[(2-methoxyphenyl)methyl]-benzeneethanamine (25B-NBOMe)-D3 as internal standard for urine and hair...
July 1, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28813419/vaccine-driven-pharmacodynamic-dissection-and-mitigation-of-fenethylline-psychoactivity
#8
Cody J Wenthur, Bin Zhou, Kim D Janda
Fenethylline, also known by the trade name Captagon, is a synthetic psychoactive stimulant that has recently been linked to a substance-use disorder and 'pharmacoterrorism' in the Middle East. Although fenethylline shares a common phenethylamine core with other amphetamine-type stimulants, it also incorporates a covalently linked xanthine moiety into its parent structure. These independently active pharmacophores are liberated during metabolism, resulting in the release of a structurally diverse chemical mixture into the central nervous system...
August 24, 2017: Nature
https://www.readbyqxmd.com/read/28766952/inhibition-of-the-%C3%AE-carbonic-anhydrase-from-the-dandruff-producing-fungus-malassezia-globosa-with-monothiocarbamates
#9
Alessio Nocentini, Daniela Vullo, Sonia Del Prete, Sameh M Osman, Fatmah A S Alasmary, Zeid AlOthman, Clemente Capasso, Fabrizio Carta, Paola Gratteri, Claudiu T Supuran
A series of monothiocarbamates (MTCs) was investigated for the inhibition of the β-class carbonic anhydrase (CAs, EC 4.2.1.1) from the fungal parasite Malassezia globosa, MgCA. These MTCs incorporate various scaffolds, among which aliphatic amine with 1-4 carbons atom in their molecule, morpholine, piperazine, as well as phenethylamine and benzylamine derivatives. All the reported MTCs displayed a better efficacy in inhibiting MgCA compared to the clinically used sulphonamide drug acetazolamide (KI of 74 μM), with KIs spanning between 1...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28762065/lc-high-resolution-ms-ms-for-identification-of-69-metabolites-of-the-new-psychoactive-substance-1-4-ethylphenyl-n-2-methoxyphenyl-methyl-propane-2-amine-4-ea-nbome-in-rat-urine-and-human-liver-s9-incubates-and-comparison-of-its-screening-power-with-further
#10
Achim T Caspar, Folker Westphal, Markus R Meyer, Hans H Maurer
4-EA-NBOMe (N-(2-methoxybenzyl)-4-ethylamphetamine, 1-(4-ethylphenyl-)-N-[(2-methoxyphenyl)methyl]propane-2-amine) is an amphetamine-derived new psychoactive substance (NPS) of the N-methoxybenzyl (NBOMe) group first seized by German custom authorities. In contrast to the phenethylamine NBOMes, studies on the pharmacological, toxicological, or metabolic properties are not yet published. The aims of the presented work were the use of LC-HR-MS/MS for identification of the phase I and II metabolites of 4-EA-NBOMe in rat urine and pooled human S9 fraction (pS9) incubations, to compare metabolite formation in both models, to identify involved monooxygenases, and to elucidate its detectability in standard urine screening approaches (SUSAs) using GC-MS, LC-MS(n), and LC-HR-MS/MS...
July 31, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28747562/isothiocyanates-suppress-the-invasion-and-metastasis-of-tumors-by-targeting-fak-mmp-9-activity
#11
Yun-Jeong Jeong, Hyun-Ji Cho, Fung-Lung Chung, Xiantao Wang, Hyang-Sook Hoe, Kwan-Kyu Park, Cheorl-Ho Kim, Hyeun-Wook Chang, Sang-Rae Lee, Young-Chae Chang
Isothiocyanates, which are present as glucosinolate precursors in cruciferous vegetables, have strong activity against various cancers. Here, we compared the anti-metastatic effects of isothiocyanates (benzyl isothiocyanate (BITC), phenethyl isothiocyanate (PEITC), and sulforaphane (SFN)) by examining how they regulate MMP-9 expression. Isothiocyanates, particularly PEITC, suppressed 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced MMP-9 activity and invasion in various cancer cell lines. By contrast, N-methyl phenethylamine, a PEITC analog without an isothiocyanate functional group, had no effect...
July 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/28720478/monoamine-receptor-interaction-profiles-of-4-thio-substituted-phenethylamines-2c-t-drugs
#12
Dino Luethi, Daniel Trachsel, Marius C Hoener, Matthias E Liechti
BACKGROUND: 4-Thio-substituted phenethylamines (2C-T drugs) are potent psychedelics with poorly defined pharmacological properties. Because of their psychedelic effects, 2C-T drugs are sometimes sold as new psychoactive substances (NPSs). The aim of the present study was to characterize the monoamine receptor and transporter interaction profiles of a series of 2C-T drugs. METHODS: We determined the binding affinities of 2C-T drugs at monoamine receptors and transporters in human cells that were transfected with the respective receptors or transporters...
July 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28714411/pharmacology-and-literature-review-based-on-related-death-and-non-fatal-case-reports-of-the-benzofurans-and-benzodifurans-designer-drugs
#13
Bernardino Barceló Martín, Isabel Gomila
BACKGROUND: Benzofurans and benzodifurans are two groups of psychoactive substances that had originally been synthesized for research purpose. Benzofurans' structure is quite similar to the known recreational drug 3,4-methylenedioxymethamphetamine together with its active metabolite 3,4-methylenedioxyamphetamine. Benzodifurans are closely related to phenethylamines, but have more hallucinogens effects and much longer duration of action. This study aims to review the accessible evidence-based literature on benzofurans and benzodifurans pharmacology and toxicology...
July 14, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28696353/array-of-chemosensitive-resistors-with-composites-of-gas-chromatography-gc-materials-and-carbon-black-for-detection-and-recognition-of-vocs-a-basic-study
#14
Bartosz Wyszynski, Rui Yatabe, Atsuo Nakao, Masaya Nakatani, Akio Oki, Hiroaki Oka, Kiyoshi Toko
Mimicking the biological olfaction, large odor-sensor arrays can be used to acquire a broad range of chemical information, with a potentially high degree of redundancy, to allow for enhanced control over the sensitivity and selectivity of artificial olfaction systems. The arrays should consist of the largest possible number of individual sensing elements while being miniaturized. Chemosensitive resistors are one of the sensing platforms that have a potential to satisfy these two conditions. In this work we test viability of fabricating a 16-element chemosensitive resistor array for detection and recognition of volatile organic compounds (VOCs)...
July 11, 2017: Sensors
https://www.readbyqxmd.com/read/28696072/comparison-of-three-s-%C3%AE-cds-with-different-degrees-of-substitution-for-the-chiral-separation-of-12-drugs-in-capillary-electrophoresis
#15
Zhaokun Wang, Qiongwen Zhang, Linda Luo, Tiemin Sun, Xingjie Guo
Three kinds of sulfated β-cyclodextrin (S-β-CD), including a single isomer, heptakis-6-sulfato-β-cyclodextrin (HS-β-CD), degree of substitution (DS) of 7, which was synthesized in our laboratory and another two commercialized randomly substituted mixtures, a sulfated β-cyclodextrin with DS of 7 to 11, as well as a highly sulfated-β-cyclodextrin with DS of 12 to 15, were used for the enantioresolution of 12 drugs (the β-blockers, phenethylamines, and anticholinergic agents) in capillary electrophoresis...
September 2017: Chirality
https://www.readbyqxmd.com/read/28689465/design-synthesis-and-taste-evaluation-of-a-high-intensity-umami-imparting-oxazole-based-compound
#16
Yusuke Amino, Yu-Ki Tahara, Kei Yamada, Masakazu Nakazawa, Uno Tagami, Takaho Tajima, Motonaka Kuroda
Umami taste is imparted predominantly by monosodium glutamate (MSG) and 5'-ribonucleotides. Recently, several different classes of hydrophobic umami-imparting compounds, the structures of which are quite different from MSG, have been reported. To obtain a novel umami-imparting compound, N-cinnamoyl phenethylamine was chosen as the lead compound, and a rational structure-optimization study was conducted on the basis of the pharmacophore model of previously reported compounds. The extremely potent umami-imparting compound 2-[[[2-[(1E)-2-(1,3-benzodioxol-5-yl)ethenyl]-4-oxazolyle]methoxy]methyl]pyridine, which exhibits 27,000 times the umami taste of MSG, was found...
September 2017: Bioscience, Biotechnology, and Biochemistry
https://www.readbyqxmd.com/read/28672699/qualitative-screening-for-new-psychoactive-substances-in-wastewater-collected-during-a-city-festival-using-liquid-chromatography-coupled-to-high-resolution-mass-spectrometry
#17
Ana Causanilles, Juliet Kinyua, Christoph Ruttkies, Alexander L N van Nuijs, Erik Emke, Adrian Covaci, Pim de Voogt
The inclusion of new psychoactive substances (NPS) in the wastewater-based epidemiology approach presents challenges, such as the reduced number of users that translates into low concentrations of residues and the limited pharmacokinetics information available, which renders the choice of target biomarker difficult. The sampling during special social settings, the analysis with improved analytical techniques, and data processing with specific workflow to narrow the search, are required approaches for a successful monitoring...
October 2017: Chemosphere
https://www.readbyqxmd.com/read/28670781/structural-characterization-and-pharmacological-evaluation-of-the-new-synthetic-cannabinoid-cumyl-pegaclone
#18
Verena Angerer, Lukas Mogler, Jan-Patrick Steitz, Philippe Bisel, Cornelius Hess, Clara T Schoeder, Christa E Müller, Laura M Huppertz, Folker Westphal, Jan Schäper, Volker Auwärter
The number of new psychoactive substances (NPS) that have emerged on the European market has been rapidly growing in the last years, with a particularly high number of new compounds from the group of synthetic cannabinoid receptor agonists. There have been various political efforts to control the trade and the use of NPS worldwide. In Germany, the 'Act to control the distribution of new psychoactive substances' (NpSG) came into force in November 2016. In this new Act two groups of substances were defined, the group 'cannabimimetics/synthetic cannabinoids' covering indole, indazole and benzimidazole core structures, and a second group named 'compounds derived from 2-phenethylamine'...
July 3, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28659208/-intoxication-with-new-psychoactive-substances-drug-unknown-but-complications-are-still-treatable
#19
M N Boersma, J J Nugteren-van Lonkhuyzen, E M van Maarseveen, H A H Kaasjager, A J H P van Riel, D Dekker
Abuse of new psychoactive substances (NPS) and the number of patients presenting to the ER with intoxication are increasing. Treatment may at first sight seem complicated because of limited knowledge of the substance involved, but should be based on a general supportive approach recognising the relatively predictable spectrum of symptoms caused by adrenergic, serotonergic and dopaminergic stimulation. In this article, we discuss the vital elements of this approach and possible complications of NPS intoxication...
2017: Nederlands Tijdschrift Voor Geneeskunde
https://www.readbyqxmd.com/read/28643397/experimental-study-on-the-postmortem-redistribution-of-the-substituted-phenethylamine-25b-nbome
#20
Kaori Shintani-Ishida, Kanju Saka, Mami Nakamura, Ken-Ichi Yoshida, Hiroshi Ikegaya
2-(4-Bromo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine (25B-NBOMe) is a substituted phenethylamine, which has become highly prevalent worldwide since 2014. Recently, in an autopsy case involving fatal 25B-NBOMe intoxication, we found the postmortem increase of 25B-NBOMe concentration in the cardiac blood approximately 2 days after death. The aim of this study was to investigate the distribution of 25B-NBOMe and reproduce the postmortem redistribution using a rat model. Sprague-Dawley rats were killed 30 min after intraperitoneal injection of 25B-NBOMe (0...
June 23, 2017: Journal of Forensic Sciences
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