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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
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
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
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
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...
November 1, 2016: Chemosphere
(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
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
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...
2016: Substance Abuse Treatment, Prevention, and Policy
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
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
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
Mario González-Jiménez, Jorge Arenas-Valgañón, María Del Pilar García-Santos, Emilio Calle, Julio Casado
Tyramine is a biogenic compound derived from the decarboxylation of the amino acid tyrosine, and is therefore present at important concentrations in a broad range of raw and fermented foods. Owing to its chemical properties, tyramine can react with nitrite, a common food additive, in the acidic medium of stomach to form N- and C-nitroso compounds. Since toxicology studies have shown that the product of C-nitrosation of tyramine is mutagenic, in the present article tyramine nitrosation mechanisms have been characterized in order to discern which of them are favoured under conditions similar to those in the human stomach lumen...
February 1, 2017: Food Chemistry
Jong Suk Park, Shaheed Ur Rehman, In Sook Kim, Min Sun Choi, Jae Sin Lee, Sanghwan In, Hye Hyun Yoo
5-(2-Aminopropyl)-2,3-dihydrobenzofuran (5-APDB) is a designer drug of phenethylamine and amphetamine class. In this study, the in vitro metabolism of 5-APDB was investigated in rat and human liver microsomes and human hepatocytes to characterize its metabolites. 5-APDB was incubated with microsomes or hepatocytes, and the reaction mixture was analyzed using liquid chromatography-quadrupole time-of-flight with tandem mass spectrometry (LC-Q/TOF-MS). 5-APDB was metabolized to yield three metabolites (M1, M2 and M3)...
October 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Sabra Botch-Jones, Jamie Foss, David Barajas, Frank Kero, Craig Young, Jason Weisenseel
New psychoactive substances (NPS) have been associated with fatalities and severe injuries in a number of cases in the United States and have led investigators to rethink traditional drug monitoring protocols. Of particular interest are the variable phenethylamine chemical structures known as 'NBOMes', which pose an emerging threat to public health with incidence steadily growing over the past decade. In this study, direct sample analysis (DSA)-time of flight mass spectrometry was employed to leverage rapid and sensitive ambient ionization mass spectrometry without chromatographic separation as verified with an authentic case sample...
October 2016: Forensic Science International
Fabio Vaiano, Francesco P Busardò, Diego Palumbo, Chrystalla Kyriakou, Alessia Fioravanti, Valeria Catalani, Francesco Mari, Elisabetta Bertol
Identification and quantification of new psychoactive substances (NPS), both in biological and non-biological samples, represent a hard challenge for forensic toxicologists. NPS are increasingly emerging on illegal drug market. Many cases of co-consumption of NPS and other substances have also been reported. Hence, the development of analytical methods aiming at the detection of a broad-spectrum of compounds (NPS and "traditional" drugs) could be helpful. In this paper, a fully validated screening method in blood for the simultaneous detection of 69 substances, including 64 NPS (28 synthetic cannabinoids, 19 synthetic cathinones, 5 phenethylamines, 3 indanes, 2 piperazines, 2 tryptamines, 2 phencyclidine, methoxetamine, ketamine and its metabolite) and 5 amphetamines (amphetamine, methamphetamine, MDMA, MDA, 3,4-methylenedioxy-N-ethylamphetamine - MDEA-) by a dynamic multiple reaction monitoring analysis through liquid chromatography - tandem mass spectrometry (LC-MS/MS) is described...
September 10, 2016: Journal of Pharmaceutical and Biomedical Analysis
Dana J Levine, Tomče Runčevski, Matthew T Kapelewski, Benjamin K Keitz, Julia Oktawiec, Douglas A Reed, Jarad A Mason, Henry Z H Jiang, Kristen A Colwell, Christina M Legendre, Stephen A FitzGerald, Jeffrey R Long
The drug olsalazine (H4olz) was employed as a ligand to synthesize a new series of mesoporous metal-organic frameworks that are expanded analogues of the well-known M2(dobdc) materials (dobdc(4-) = 2,5-dioxido-1,4-benzenedicarboxylate; M-MOF-74). The M2(olz) frameworks (M = Mg, Fe, Co, Ni, and Zn) exhibit high surface areas with large hexagonal pore apertures that are approximately 27 Å in diameter. Variable temperature H2 adsorption isotherms revealed strong adsorption at the open metal sites, and in situ infrared spectroscopy experiments on Mg2(olz) and Ni2(olz) were used to determine site-specific H2 binding enthalpies...
August 17, 2016: Journal of the American Chemical Society
Camilla Montesano, Gabriele Vannutelli, Adolfo Gregori, Luigi Ripani, Dario Compagnone, Roberta Curini, Manuel Sergi
Drug abuse is today a growing global problem. Often the consumers are not aware about the type of substances they are using and the correlated risks. In recent years, new psychoactive substances (NPS) appeared in the illicit market. The presence of NPS, such as synthetic cathinones, cannabinoids and phenethylamines, which are known to be pharmacologically and toxicologically hazardous, has been frequently reported. The aim of this study was the development of a liquid chromatography-high-resolution mass spectrometry (LC-HRMS) method for a broad screening of NPS in plasma...
September 2016: Journal of Analytical Toxicology
Sofyane Andjouh, Yves Blache
Rapid and efficient synthesis of 23 analogues inspired by bromotyramine derivatives, marine natural products, by means of CuSO4-catalysed [3+2] alkyne-azide cycloaddition is described. The final target was then assayed for anti-biofilm activity against three Gram-negative marine bacteria, Pseudoalteromonas ulvae (TC14), Pseudoalteromonas lipolytica (TC8) and Paracoccus sp. (4M6). Most of the synthesised bromotyramine/triazole derivatives are more active than the parent natural products Moloka'iamine (A) and 3,5-dibromo-4-methoxy-β-phenethylamine (B) against biofilm formation by the three bacterial strains...
September 2016: Biofouling
Camilla Montesano, Gabriele Vannutelli, Maristella Massa, Maria Chiara Simeoni, Adolfo Gregori, Luigi Ripani, Dario Compagnone, Roberta Curini, Manuel Sergi
In this paper, an analytical method has been developed and validated for the analysis of new psychoactive substances (NPS) and metabolites in hair samples. The method was based on pressurized liquid extraction (PLE) followed by SPE clean-up and HPLC-HRMS analysis. To evaluate extraction efficiency and the applicability of the method, hair samples were fortified by soaking in order to obtain a good surrogate for drug users' hair; the amount of incorporated drugs related to their lipophilicity, similarly to in vivo drug incorporation...
July 23, 2016: Drug Testing and Analysis
Laura Mercolini, Michele Protti
The term "new psychoactive substances" refers to emerging drugs of abuse whose chemical structure and psychoactive effects are similar to other already known compounds, often providing a "legal" alternative to internationally regulated drugs and mostly available via on-line retail sites. There are several categories of new psychoactive substances, such as synthetic cannabinoids, cathinone analogues, phenethylamines, tryptamines, and the need to identify and quantify an unprecedented and growing number of new compounds represents a unique challenge for toxicological and forensic analysis...
June 25, 2016: Journal of Pharmaceutical and Biomedical Analysis
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