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https://www.readbyqxmd.com/read/28097528/pharmacology-and-toxicology-of-n-benzylphenethylamine-nbome-hallucinogens
#1
Adam L Halberstadt
Serotonergic hallucinogens induce profound changes in perception and cognition. The characteristic effects of hallucinogens are mediated by 5-HT2A receptor activation. One class of hallucinogens are 2,5-dimethoxy-substituted phenethylamines, such as the so-called 2C-X compounds 2,5-dimethoxy-4-bromophenethylamine (2C-B) and 2,5-dimethoxy-4-iodophenethylamine (2C-I). Addition of an N-benzyl group to phenethylamine hallucinogens produces a marked increase in 5-HT2A-binding affinity and hallucinogenic potency...
January 18, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28088737/the-hemostatic-effect-study-of-cirsium-setosum-on-regulating-%C3%AE-1-ars-via-mediating-norepinephrine-synthesis-by-enzyme-catalysis
#2
Nianwei Chang, Yanmei Li, Mengge Zhou, Jie Gao, Yuanyuan Hou, Min Jiang, Gang Bai
BACKGROUND: Cirsium setosum (CS) is the aboveground part of Cephalanoplos segetum Kitam. Although it has been used as a hemostatic treatment for thousands of years and is still in use today, the mechanism of CS on regulating ARs is still not clear. PURPOSE: In this study, we aimed to clarify the mechanism of CS on regulating ARs. METHODS: We developed a simple method based on UPLC/Q-TOF MS combined adrenergic receptor dual-luciferase reporter assay systems for the rapid determination of active constituents in CS...
January 12, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28088088/prevalence-of-new-psychoactive-substances-in-northeast-asia-from-2007-to-2015
#3
Junhui Lee, Songhee Yang, Yujin Kang, Eunyoung Han, Ling-Yi Feng, Jih-Heng Li, Heesun Chung
The proliferation of new psychoactive substances (NPS) has been a global trend in drug abuse and its regulation has been a worldwide concern. There is no doubt that it is necessary to share information related to these emerging substances between countries and continents for the effective regulation of NPS. With efforts for the efficient regulation of NPS, many studies and information have been published for the prevalence of NPS in the United States and other countries in Europe and Oceania. However, there is lack of information available for the prevalence of NPS in Asian and African countries...
October 20, 2016: Forensic Science International
https://www.readbyqxmd.com/read/28059498/rapid-screening-method-for-new-psychoactive-substances-of-forensic-interest-electrochemistry-and-analytical-determination-of-phenethylamines-derivatives-nbome-via-cyclic-and-differential-pulse-voltammetry
#4
Ana Flávia B Andrade, Samuel Kasahun Mamo, Jose Gonzalez-Rodriguez
The NBOMe derivatives are phenethylamines derived from the 2C class of hallucinogens. Only a few human pharmacologic studies have been conducted on these drugs, and several cases of intoxication and deaths have been reported. Presently, NBOMe are not a part of the routine drugs-of-abuse screening procedure for many police forces, and there are no rapid immunoassay screening tests that can detect the presence of those compounds. In this Article, the voltammetric behavior of 25B NBOMe and 25I NBOMe were investigated and their electroanalytical characteristics determined for the first time...
January 6, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28057408/dithiocarbamates-effectively-inhibit-the-%C3%AE-carbonic-anhydrase-from-the-dandruff-producing-fungus-malassezia-globosa
#5
Daniela Vullo, Sonia Del Prete, Alessio Nocentini, Sameh M Osman, Zeid AlOthman, Clemente Capasso, Murat Bozdag, Fabrizio Carta, Paola Gratteri, Claudiu T Supuran
A series of dithiocarbamates (DTCs) was investigated for the inhibition of the β-class carbonic anhydrase (CAs, EC 4.2.1.1) from the fungal parasite Malassezia globosa, MgCA, a validated anti-dandruff drug target. These DTCs incorporate various scaffold, among which those of N,N-dimethylaminoethylenediamine, the aminoalcohols with 3-5 carbon atoms in their molecule, 3-amino-quinuclidine, piperidine, morpholine and piperazine derivatives, as well as phenethylamine and its 4-sulfamoylated derivative. Several DTCs resulted more effective in inhibiting MgCA compared to the standard sulfonamide drug acetazolamide (KI of 74μM), with KIs ranging between 383 and 6235nM...
December 27, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28000107/analytical-validation-of-a-portable-mass-spectrometer-featuring-interchangeable-ambient-ionization-sources-for-high-throughput-forensic-evidence-screening
#6
Zachary E Lawton, Angelica Traub, William L Fatigante, Jose Mancias, Adam E O'Leary, Seth E Hall, Jamie R Wieland, Herbert Oberacher, Michael C Gizzi, Christopher C Mulligan
Forensic evidentiary backlogs are indicative of the growing need for cost-effective, high-throughput instrumental methods. One such emerging technology that shows high promise in meeting this demand while also allowing on-site forensic investigation is portable mass spectrometric (MS) instrumentation, particularly that which enables the coupling to ambient ionization techniques. While the benefits of rapid, on-site screening of contraband can be anticipated, the inherent legal implications of field-collected data necessitates that the analytical performance of technology employed be commensurate with accepted techniques...
December 20, 2016: Journal of the American Society for Mass Spectrometry
https://www.readbyqxmd.com/read/27993913/direct-stamp-of-technology-or-origin-on-the-genotypic-and-phenotypic-variation-of-indigenous-saccharomyces-cerevisiae-population-in-a-natural-model-of-boiled-grape-juice-fermentation-into-traditional-msalais-wine-in-china
#7
Li-Xia Zhu, Guan-Qiong Wang, Ju-Lan Xue, Dong-Qi Gou, Chang-Qing Duan
Saccharomyces cerevisiae strains worldwide show genetic and phenotypic diversity and their population substructures are greatly affected by their technological application or geographical origins. Msalais is a traditional wine obtained via a unique method of spontaneous fermentation of local boiled grape juice in Southern Xinjiang. We analyzed 436 indigenous S. cerevisiae strains associated with Msalais fermentation. These strains were highly diverse with respect to the inter-delta region and 24 phenotypic traits, with apparent differentiation according to strain origins and technologies used to produce Msalais...
December 18, 2016: FEMS Yeast Research
https://www.readbyqxmd.com/read/27951637/ligand-enabled-meta-selective-c-h-arylation-of-nosyl-protected-phenethylamines-benzylamines-and-2-aryl-anilines
#8
Qiuping Ding, Shengqing Ye, Guolin Cheng, Peng Wang, Marcus E Farmer, Jin-Quan Yu
A Pd-catalyzed, meta-selective C-H arylation of nosyl-protected phenethylamines and benzylamines is disclosed using a combination of norbornene and pyridine-based ligands. Subjecting nosyl protected 2-aryl anilines to this protocol led to meta-C-H arylation at the remote aryl ring. A diverse range of aryl iodides are tolerated in this reaction, along with select heteroaryl iodides. Select aryl bromides bearing ortho-coordinating groups can also be utilized as effective coupling partners in this reaction. The use of pyridine ligands has allowed the palladium loading to be reduced to 2...
December 23, 2016: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/27939599/i-like-the-old-stuff-better-than-the-new-stuff-subjective-experiences-of-new-psychoactive-substances
#9
Allison Matthews, Rachel Sutherland, Amy Peacock, Joe Van Buskirk, Elizabeth Whittaker, Lucinda Burns, Raimondo Bruno
BACKGROUND: Over the past decade, monitoring systems have identified the rapid emergence of new psychoactive substances (NPS). While the use of many NPS is minimal and transitory, little is known about which products have potential for capturing the attention of significant proportions of the drug consuming market. The aim of this study was to explore self-reported experiences of three commonly used NPS classes within the Australian context (synthetic cathinones, hallucinogenic phenethylamines and hallucinogenic tryptamines) relative to traditional illicit drug counterparts...
December 8, 2016: International Journal on Drug Policy
https://www.readbyqxmd.com/read/27888011/antiproliferative-and-ultrastructural-effects-of-phenethylamine-derivatives-on-promastigotes-and-amastigotes-of-leishmania-leishmania-infantum-chagasi
#10
Paula Ferreira Brasil, Júlia Araújo de Freitas, Anna Léa Silva Barreto, Camila Marques Adade, Leandro Figueira Reis de Sá, Pamella Constantino-Teles, Fabiano Travanca Toledo, Bruno A de Sousa, Augusto Cesar Gonçalves, Maria Teresa Villela Romanos, João V Comasseto, Alcindo A Dos Santos, Ana Claudia Tessis, Thais Souto-Padrón, Rosangela Maria A Soares, Antonio Ferreira-Pereira
Leishmania (Leishmania) infantum chagasi is one of the agents that cause visceral leishmaniasis. This disease occurs more frequently in third world countries, such as Brazil. The treatment is arduous, and is dependent on just a few drugs like the antimonial derivatives and amphotericin B. Moreover, these drugs are not only expensive, but they can also cause severe side effects and require long-term treatment. Therefore, it is very important to find new compounds that are effective against leishmaniasis. In the present work we evaluated a new group of synthetic amides against the promastigote and amastigote forms of L...
November 22, 2016: Parasitology International
https://www.readbyqxmd.com/read/27874182/synthesis-and-analysis-of-glucuronic-acid-conjugated-metabolites-of-4-bromo-2-5-dimethoxyphenethylamine
#11
Tatsuyuki Kanamori, Tadashi Yamamuro, Kenji Kuwayama, Kenji Tsujikawa, Yuko T Iwata, Hiroyuki Inoue
In the study reported here, two glucuronic acid-conjugated metabolites of 4-bromo-2,5-dimethoxyphenethylamine (2C-B)-a ring-substituted psychoactive phenethylamine-were chemically synthesized for the first time and a method for analyzing them in urine was developed. β-D-Glucuronide of 4-bromo-2,5-dimethoxyphenylethylalcohol was successfully synthesized using methyl 2,3,4-tri-Ο-acetyl-1-O-(trichloroacetimidoyl)-α-D-glucuronate as a glucuronyl donor and boron trifluoride diethylether complex as a Lewis acid catalyst...
November 22, 2016: Journal of Forensic Sciences
https://www.readbyqxmd.com/read/27862205/antioxidant-activity-acetylcholinesterase-and-carbonic-anhydrase-inhibitory-properties-of-novel-ureas-derived-from-phenethylamines
#12
Kadir Aksu, Bünyamin Özgeriş, Parham Taslimi, Ali Naderi, İlhami Gülçin, Süleyman Göksu
A series of ureas derived from phenethylamines were synthesized and evaluated for human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activities and antioxidant properties. The ureas were synthesized from the reactions of substituted phenethylamines with N,N-dimethylcarbamoyl chloride; then, the synthesized compounds were converted to their corresponding phenolic derivatives via O-demethylation. hCA I and II were effectively inhibited by the newly synthesized compounds, with Ki values in the range of 0...
December 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27834146/recent-trends-in-analytical-methods-to-determine-new-psychoactive-substances-in-hair
#13
Chrystalla Kyriakou, Manuela Pellegrini, Oscar García-Algar, Enrico Marinelli, Simona Zaami
New Psychoactive Substances (NPS) belong to several chemical classes, including phenethylamines, piperazines, synthetic cathinones and synthetic cannabinoids. Development and validation of analytical methods for the determination of NPS both in traditional and alternative matrices is of crucial importance to study drug metabolism and to associate consumption to clinical outcomes and eventual intoxication symptoms. Among different biological matrices, hair is the one with the widest time window to investigate drug-related history and demonstrate past intake...
November 11, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27814952/liquid-chromatography-tandem-mass-spectrometry-determination-of-synthetic-cathinones-and-phenethylamines-in-influent-wastewater-of-eight-european-cities
#14
Richard Bade, Lubertus Bijlsma, Juan V Sancho, Jose A Baz-Lomba, Sara Castiglioni, Erika Castrignanò, Ana Causanilles, Emma Gracia-Lor, Barbara Kasprzyk-Hordern, Juliet Kinyua, Ann-Kathrin McCall, Alexander L N van Nuijs, Christoph Ort, Benedek G Plósz, Pedram Ramin, Nikolaos I Rousis, Yeonsuk Ryu, Kevin V Thomas, Pim de Voogt, Ettore Zuccato, Félix Hernández
The popularity of new psychoactive substances (NPS) has grown in recent years, with certain NPS commonly and preferentially consumed even following the introduction of preventative legislation. With the objective to improve the knowledge on the use of NPS, a rapid and very sensitive method was developed for the determination of ten priority NPS (N-ethylcathinone, methylenedioxypyrovalerone (MDPV), methylone, butylone, methedrone, mephedrone, naphyrone, 25-C-NBOMe, 25-I-NBOMe and 25-B-NBOMe) in influent wastewater...
February 2017: Chemosphere
https://www.readbyqxmd.com/read/27726316/schedules-of-controlled-substances-placement-of-three-synthetic-phenethylamines-into-schedule-i-final-rule
#15
(no author information available yet)
With the issuance of this final rule, the Administrator of the Drug Enforcement Administration places three synthetic phenethylamines: 2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine (25I-NBOMe; 2C-I-NBOMe; 25I; Cimbi-5), 2-(4-chloro-2,5-dimethoxyphenyl)-N- (2-methoxybenzyl)ethanamine (25C-NBOMe; 2C-C-NBOMe; 25C; Cimbi-82), and 2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine (25B- NBOMe; 2C-B-NBOMe; 25B; Cimbi-36), including their optical, positional, and geometric isomers, salts and salts of isomers, whenever the existence of such salts, isomers, and salts of isomers is possible, into schedule I of the Controlled Substances Act...
September 27, 2016: Federal Register
https://www.readbyqxmd.com/read/27671491/common-substances-that-may-contribute-to-resistant-hypertension-and-recommendations-for-limiting-their-clinical-effects
#16
REVIEW
Samuel J Jurca, William J Elliott
PURPOSE OF REVIEW: The purpose of this review is to highlight common or important substances or habits that elevate blood pressure and offer suggestions, based on recent literature, to limit their use or effects. RECENT FINDINGS: Despite decades of advice to the general populace from public health authorities to avoid or reduce dietary sodium and non-steroidal anti-inflammatory drug (NSAID) use, more evidence has accumulated from nationwide surveys, clinical trials, and pathophysiological or mechanistic studies that show how important these modalities can (and should) be for hypertensive and prehypertensive individuals and the general population...
October 2016: Current Hypertension Reports
https://www.readbyqxmd.com/read/27663984/comparison-of-illegal-drug-use-pattern-in-taiwan-and-korea-from-2006-to-2014
#17
Ling-Yi Feng, Wen-Jing Yu, Wei-Ting Chang, Eunyoung Han, Heesun Chung, Jih-Heng Li
BACKGROUND: Illegal drug use has long been a global concern. Taiwan and Korea are geographically adjacent and both countries have experienced the illegal use problems of methamphetamine, a predominant prototype of New Psychoactive Substances (NPS). NPS, a term coined by the United Nations Office on Drugs and Crime (UNODC) in recent years, have not been scrutinized for their safety and may become a new threat to public health and security worldwide. To conduct evidence-based drug policy, it is imperative to estimate the trend and pattern of illegal drug use...
September 23, 2016: Substance Abuse Treatment, Prevention, and Policy
https://www.readbyqxmd.com/read/27660913/the-presence-of-new-psychoactive-substances-in-a-tor-network-marketplace-environment
#18
Diana S Dolliver, Joseph B Kuhns
Prior research has documented the availability of drugs on many Tor Network websites, with the Internet playing a particularly vital role in the global new psychoactive substances (NPS) market. The primary objective of this research was to document types of NPS for sale on the largest operating Tor site (Agora) over a period of four months. Secondary objectives were to analyze countries and vendors sourcing NPS on Agora. Data from Agora were collected in February and June 2015. The number of total advertisements on Agora increased from 20,742 to 27,431 over the four months, while the number of NPS advertisements increased from 2,205 to 2,271 and the number of vendors increased from 157 to 288...
November 2016: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/27624522/convergent-18-f-labeling-and-evaluation-of-n-benzyl-phenethylamines-as-5-ht2a-receptor-pet-ligands
#19
Ida Nymann Petersen, Jonas Villadsen, Hanne Demant Hansen, Anders A Jensen, Szabolcs Lehel, Nic Gillings, Matthias M Herth, Gitte M Knudsen, Jesper L Kristensen
Positron emission tomography (PET) investigations of the 5-HT2A receptor (5-HT2AR) system can be used as a research tool in diseases such as depression, Alzheimer's disease and schizophrenia. We have previously developed a (11)C-labeled agonist PET ligand ([(11)C]Cimbi-36), and the aim of this study was to identify a (18)F-labeled analogue of this PET-ligand. Thus, we developed a convergent radiochemical approach giving easy access to 5 different (18)F-labeled ligands structurally related to Cimbi-36 from a common (18)F-labeled intermediate...
November 1, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27608273/asymmetric-synthesis-of-an-amino-acid-derivative-from-achiral-aroyl-acrylamide-by-reversible-michael-addition-and-preferential-crystallization
#20
Yuki Kaji, Naohiro Uemura, Yoshio Kasashima, Hiroki Ishikawa, Yasushi Yoshida, Takashi Mino, Masami Sakamoto
Single-handed α-amino acid derivatives were generated from achiral precursors without an external chiral source. Conjugate addition of phenethylamine to an achiral aroyl acrylamide under homogeneous conditions gave the α-amino amides in quantitative yields, which crystallized as a conglomerate of a P21 crystal system. Dynamic preferential crystallization or attrition-enhanced deracemization resulted in the formation of enantiomorphic crystals of 99 % ee.
October 6, 2016: Chemistry: a European Journal
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