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https://www.readbyqxmd.com/read/28720478/monoamine-receptor-interaction-profiles-of-4-thio-substituted-phenethylamines-2c-t-drugs
#1
REVIEW
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
#2
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
#3
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
#4
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...
July 11, 2017: Chirality
https://www.readbyqxmd.com/read/28689465/design-synthesis-and-taste-evaluation-of-a-high-intensity-umami-imparting-oxazole-based-compound
#5
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...
July 10, 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
#6
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...
June 26, 2017: Chemosphere
https://www.readbyqxmd.com/read/28670781/structural-characterization-and-pharmacological-evaluation-of-the-new-synthetic-cannabinoid-cumyl-pegaclone
#7
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
#8
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
#9
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
https://www.readbyqxmd.com/read/28617997/a-market-on-both-sides-of-the-law-the-use-of-the-hidden-web-for-the-sale-of-new-psychoactive-substances
#10
Elle Wadsworth, Colin Drummond, Andreas Kimergård, Paolo Deluca
OBJECTIVE: The hidden Web is used for the anonymous sale of drugs, and with the UK Psychoactive Substances Act, 2016, implemented on May 26th 2016; it could increase as a platform for obtaining new psychoactive substances (NPS). This study aims to describe the NPS market on the visible and hidden Web preban, and assess whether the hidden Web is a likely place for the sale of NPS postban. METHODS: Data collection of 113 online shops took place in October 2015. Data collection of 22 cryptomarkets took place every 2 months from October 2015 to 2016 as part of the CASSANDRA project...
June 15, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28532112/preparations-and-doxorubicin-controlled-release-of-amino-acid-based-redox-ph-dual-responsive-nanomicelles
#11
Yuanyuan Ding, Liping Zhang, Gang Shi, Xinxin Sang, Caihua Ni
Terpolymers of poly (Lysine-co-N, N-Bis (acryloyl) cystamine-co-β-Phenethylamine) (PLBP) were synthesized in one-pot by Michael addition terpolymerization. The terpolymers self-assembled into nano-sized spherical micelles (84-123nm) with narrow distributions. The surface charge of the nanomicelles (NMs) was depended on solution's pH and showed negative values under physiological conditions (pH7.4), which was beneficial for long circulation without non-specific protein adsorption. Doxorubicin (DOX) was effectively loaded into the NMs for controlled release...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28527345/a-literature-review-of-blood-concentrations-of-new-psychoactive-substances-classified-as-phenethylamines-aminoindanes-arylalkylamines-arylcyclohexylamines-and-indolalkylamines
#12
REVIEW
Ritva Karinen, Gudrun Høiseth
Interpretation of blood concentrations of new psychoactive substances (NPS) requires comparison of the results to previously published case reports; as only a few experimental studies for these substances exist. A large number of articles representing single or multiple cases have been published for a great number of substances, making a unified overview difficult. In this review we have collected all published blood concentrations from the NPS groups classified as phenethylamines, aminoindanes, arylalkylamines, arylcyclohexylamines, and indolalkylamines, and also included unpublished results for MPA, MXE, 4-FMA, 4-FA and 4-MA analyzed in our laboratory...
March 21, 2017: Forensic Science International
https://www.readbyqxmd.com/read/28506818/measuring-inhibition-of-monoamine-reuptake-transporters-by-new-psychoactive-substances-nps-in-real-time-using-a-high-throughput-fluorescence-based-assay
#13
Anne Zwartsen, Anouk H A Verboven, Regina G D M van Kleef, Fiona M J Wijnolts, Remco H S Westerink, Laura Hondebrink
The prevalence and use of new psychoactive substances (NPS) is increasing and currently over 600 NPS exist. Many illicit drugs and NPS increase brain monoamine levels by inhibition and/or reversal of monoamine reuptake transporters (DAT, NET and SERT). This is often investigated using labor-intensive, radiometric endpoint measurements. We investigated the applicability of a novel and innovative assay that is based on a fluorescent monoamine mimicking substrate. DAT, NET or SERT-expressing human embryonic kidney (HEK293) cells were exposed to common drugs (cocaine, dl-amphetamine or MDMA), NPS (4-fluoroamphetamine, PMMA, α-PVP, 5-APB, 2C-B, 25B-NBOMe, 25I-NBOMe or methoxetamine) or the antidepressant fluoxetine...
May 12, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28485987/assessing-self-reported-use-of-new-psychoactive-substances-the-impact-of-gate-questions
#14
Joseph J Palamar, Patricia Acosta, Fermín Fernández Calderón, Scott Sherman, Charles M Cleland
BACKGROUND: New psychoactive substances (NPS) continue to emerge; however, few surveys of substance use ask about NPS use. Research is needed to determine how to most effectively query use of NPS and other uncommon drugs. OBJECTIVE: To determine whether prevalence of self-reported lifetime and past-year use differs depending on whether or not queries about NPS use are preceded by "gate questions." Gate questions utilize skip-logic, such that only a "yes" response to the use of specific drug class is followed by more extensive queries of drug use in that drug class...
September 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/28485498/plasmonic-nanoparticles-decorated-diatomite-biosilica-extending-the-horizon-of-on-chip-chromatography-and-label-free-biosensing
#15
Xianming Kong, Erwen Li, Kenny Squire, Ye Liu, Bo Wu, Li-Jing Cheng, Alan X Wang
Diatomite consists of fossilized remains of ancient diatoms and is a type of naturally abundant photonic crystal biosilica with multiple unique physical and chemical functionalities. In this paper, we explored the fluidic properties of diatomite as the matrix for on-chip chromatography and, simultaneously, the photonic crystal effects to enhance the plasmonic resonances of metallic nanoparticles for surface-enhanced Raman scattering (SERS) biosensing. The plasmonic nanoparticle-decorated diatomite biosilica provides a lab-on-a-chip capability to separate and detect small molecules from mixture samples with ultra-high detection sensitivity down to 1 ppm...
May 9, 2017: Journal of Biophotonics
https://www.readbyqxmd.com/read/28481522/rapid-hydrogen-deuterium-exchange-in-liquid-droplets
#16
Erik T Jansson, Yin-Hung Lai, Juan G Santiago, Richard N Zare
The rate of hydrogen-deuterium exchange (HDX) in aqueous droplets of phenethylamine has been determined with submillisecond temporal resolution by mass spectrometry using nanoelectrospray ionization with a theta-capillary. The average speed of the microdroplets is measured using microparticle image velocimetry. The droplet travel time is varied from 20 to 320 μs by changing the distance between the emitter and the heated inlet to the mass spectrometer and the voltage applied to the emitter source. The droplets were found to accelerate by ∼30% during their observable travel time...
May 12, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28472697/occurrence-and-fate-of-illicit-drugs-and-pharmaceuticals-in-wastewater-from-two-wastewater-treatment-plants-in-costa-rica
#17
Ana Causanilles, Clemens Ruepert, María Ibáñez, Erik Emke, Félix Hernández, Pim de Voogt
Chemical analysis of raw wastewater in order to assess the presence of biological markers entering a wastewater treatment plant can provide objective information about the health and lifestyle of the population connected to the sewer system. This work was performed in a tropical country of Central America, Costa Rica, with the aim of extending this knowledge to new world regions. This work is the first to report wastewater-based epidemiological data on the use of illicit drugs in this region of the world. Composite wastewater samples from the influents of two different wastewater treatment facilities and surface water samples from surrounding areas were collected applying the best practice protocol and analysed to investigate the occurrence and fate of selected illicit drugs of abuse and pharmaceuticals...
December 1, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28472358/metabolic-profile-determination-of-nbome-compounds-using-human-liver-microsomes-and-comparison-with-findings-in-authentic-human-blood-and-urine
#18
Keith-Dane H Temporal, Karen S Scott, Amanda L A Mohr, Barry K Logan
The emergence of novel psychoactive substances (NPS) such as hallucinogenic NBOMes (N-methoxybenzyl derivatives of 2C phenethylamines) in the past few years into the recreational drug market has introduced various challenges in forensic analytical toxicology in regard to adequate and timely detection of these compounds. This is especially true in samples from individuals who have experienced severe and fatal intoxications. The aim of this research was to identify the major Phase I metabolites of selected NBOMe compounds to generate a predicted human metabolic pathway of these substances...
May 3, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28444659/new-psychoactive-substances-nps-a-challenge-for-the-addiction-treatment-services
#19
Norbert Scherbaum, F Schifano, Udo Bonnet
Over the last few years, hundreds of new psychoactive substances (NPS) have been identified in Europe. Apart from some herbal compounds, NPS mainly include synthetic cannabinoids and a range of new synthetic stimulants (e. g., cathinones). Synthetic NPS are often developed whilst modifying the basic chemical (e. g., phenethylamine or tryptamine) structure. Although the pharmacology and toxicology of most NPS are hardly known, they are being offered, especially online, as "bath salts," as "incense mixtures," or under other misleading labels...
May 2017: Pharmacopsychiatry
https://www.readbyqxmd.com/read/28404688/brain-disposition-of-cis-para-methyl-4-methylaminorex-cis-4-4-dmar-and-its-potential-metabolites-after-acute-and-chronic-treatment-in-rats-correlation-with-central-behavioral-effects
#20
Jacopo Lucchetti, Claudio M Marzo, Alice Passoni, Angelo Di Clemente, Federico Moro, Renzo Bagnati, Marco Gobbi, Luigi Cervo
para-Methyl-4-methylaminorex (4,4'-DMAR) is a phenethylamine derivative with psychostimulant activity whose abuse has been associated with several deaths and a wide range of adverse effects. We recently validated a high-performance liquid chromatography-tandem mass spectrometry method to measure the compound's concentrations in plasma, and we applied it to describe the pharmacokinetic properties of 4,4'-DMAR after a single dose in rats. In this study, we investigated the brain disposition and metabolism of cis-4,4'-DMAR after intraperitoneal injection as well as its central behavioral effects...
June 2017: Journal of Pharmacology and Experimental Therapeutics
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