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June 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Yao Li, Cyndi Qixin He, Fei-Xiang Gao, Zhen Li, Xiao-Song Xue, Xin Li, K N Houk, Jin-Pei Cheng
A new chiral HBD system, N-tert-butyl sulfinyl squaramide, was designed and synthesized. The core N-tert-butyl sulfinyl squaramide with an 1-aminoindan-2-ol skeleton was found to be an efficient catalyst in the enantioselective Friedel-Crafts alkylation of indoles and acyl phosphonates.
April 7, 2017: Organic Letters
Amira Guirguis, Sarah Girotto, Benedetta Berti, Jacqueline L Stair
The chemical identification of new psychoactive substances (NPS) in the field is challenging due not only to the plethora of substances available, but also as a result of the chemical complexity of products and the chemical similarity of NPS analogues. In this study, handheld Raman spectroscopy and the use of two excitation wavelengths, 785 and 1064nm, were evaluated for the identification of 60 NPS products. The products contained a range of NPS from classes including the aminoindanes, arylalkylamines, benzodiazepines, and piperidines & pyrrolidines...
February 4, 2017: Forensic Science International
Linda Vårdal, Hilde-Merete Askildsen, Astrid Gjelstad, Elisabeth Leere Øiestad, Hilde Marie Erøy Edvardsen, Stig Pedersen-Bjergaard
Parallel artificial liquid membrane extraction (PALME) was combined with ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS) and the potential for screening of new psychoactive substances (NPS) was investigated for the first time. PALME was performed in 96-well format comprising a donor plate, a supported liquid membrane (SLM), and an acceptor plate. Uncharged NPS were extracted from plasma or whole blood, across an organic SLM, and into an aqueous acceptor solution, facilitated by a pH gradient...
March 24, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Jerzy Zoń, Piotr Miziak
Five new geminal aminocycloalkanephosphonic acids (4-8) containing both an aromatic ring and a cycloalkane ring were synthesized and evaluated as potential inhibitors of buckwheat phenylalanine ammonia-lyase (PAL). Within the set of compounds which are related to 2-aminoindane-2-phosphonic acid (AIP, 3), a known powerful inhibitor of PAL, racemic 1-aminobenzocyclobutene-1-phosphonic acid (4), was six times weaker than AIP as an in vitro inhibitor of buckwheat PAL, but six times stronger than AIP as an in vivo inhibitor of phenylalanine-derived anthocyanin synthesis in buckwheat...
February 7, 2017: Chemistry & Biodiversity
Jakob A Shimshoni, Ilan Winkler, Nir Edery, Ezekiel Golan, René van Wettum, David Nutt
5-Methoxy-2-aminoindane (MEAI) is a psychoactive compound of the aminoindane class, which in recent years has been recreationally used by many people, who reported of a mild euphoric, alcohol-like tipsy experience and reduced desire to consume alcoholic beverages. In the light of these observations it was decided to progress MEAI through a preliminary drug development route and evaluate the acute and subacute toxicity of MEAI administrated orally to Sprague Dawley rats, as well as to determine potential in-vitro cytotoxic and mutagenic effects using state-of-the-art protocols...
February 4, 2017: Toxicology and Applied Pharmacology
Hayriye Genç, Ramazan Kalin, Zeynep Köksal, Nastaran Sadeghian, Umit M Kocyigit, Mustafa Zengin, İlhami Gülçin, Hasan Özdemir
β-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. β-Lactams were synthesized from benzylidene-inden derivatives and acetoxyacetyl chloride. The inhibitory effect of these compounds was examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The results reveal that β-lactams are inhibitors of hCA I, II and AChE. The Ki values of β-lactams (2a-k) were 0.44-6.29 nM against hCA I, 0.93-8.34 nM against hCA II, and 0...
October 20, 2016: International Journal of Molecular Sciences
Joe Kakish, Kevin J H Allen, Troy A Harkness, Ed S Krol, Jeremy S Lee
The misfolding of α-synuclein is a critical event in the death of dopaminergic neurons and the progression of Parkinson's disease. Previously, it was suggested that drugs, which bind to α-synuclein and form a loop structure between the N- and C-termini, tend to be neuroprotective, whereas others, which cause a more compact structure, tend to be neurotoxic. To improve the binding to α-synuclein, eight novel compounds were synthesized from a caffeine scaffold attached to (R,S)-1-aminoindan, (R,S)-nicotine, and metformin, and their binding to α-synuclein determined through nanopore analysis and isothermal titration calorimetry...
December 21, 2016: ACS Chemical Neuroscience
Nils Rackelmann, Hans Matter, Heinrich Englert, Markus Follmann, Thomas Maier, John Weston, Petra Arndt, Winfried Heyse, Katharina Mertsch, Klaus Wirth, Laurent Bialy
The design, synthesis, and structure-activity relationship of 1-phenoxy-2-aminoindanes as inhibitors of the Na(+)/H(+) exchanger type 3 (NHE3) are described based on a hit from high-throughput screening (HTS). The chemical optimization resulted in the discovery of potent, selective, and orally bioavailable NHE3 inhibitors with 13d as best compound, showing high in vitro permeability and lacking CYP2D6 inhibition as main optimization parameters. Aligning 1-phenoxy-2-aminoindanes onto the X-ray structure of 13d then provided 3D-QSAR models for NHE3 inhibition capturing guidelines for optimization...
October 13, 2016: Journal of Medicinal Chemistry
Monika Židková, Igor Linhart, Marie Balíková, Michal Himl, Lubomír Váňa, Michal Vetýška, Tomáš Páleníček, Eva Lhotková, Martin Dušek
1. 5,6-Methylenedioxy-2-aminoindane (MDAI) is a member of aminoindane drug family with serotoninergic effect, which appeared on illicit drug market as a substitute for banned stimulating and entactogenic drugs. 2. Metabolism of MDAI, which has been hitherto unexplored, was studied in rats dosed with a subcutaneous dose of 20 mg MDAI.HCl/kg body weight. The urine of rats was collected within 24 h after dosing for analyses by HPLC-ESI-HRMS and GC/MS. 3. The main metabolic pathways proceeding in parallel were found to be oxidative demethylenation followed by O-methylation and N-acetylation...
June 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Christopher Murgatroyd, Lisa Pirrie, Fanny Tran, Terry K Smith, Nicholas J Westwood, Catherine S Adamson
UNLABELLED: HIV-1 maturation inhibitors are a novel class of antiretroviral compounds that consist of two structurally distinct chemical classes: betulinic acid derivatives and the pyridone-based compound PF-46396. It is currently believed that both classes act by similar modes of action to generate aberrant noninfectious particles via inhibition of CA-SP1 cleavage during Gag proteolytic processing. In this study, we utilized a series of novel analogues with decreasing similarity to PF-46396 to determine the chemical groups within PF-46396 that contribute to antiviral activity, Gag binding, and the relationship between these essential properties...
September 15, 2016: Journal of Virology
Tomáš Páleníček, Eva Lhotková, Monika Žídková, Marie Balíková, Martin Kuchař, Michal Himl, Petra Mikšátková, Martin Čegan, Karel Valeš, Filip Tylš, Rachel R Horsley
MDAI (5,6-Methylenedioxy-2-aminoindane) has a reputation as a non-neurotoxic ecstasy replacement amongst recreational users, however the drug has been implicated in some severe and lethal intoxications. Due to this, and the fact that the drug is almost unexplored scientifically we investigated a broad range of effects of acute MDAI administration: pharmacokinetics (in sera, brain, liver and lung); behaviour (open field; prepulse inhibition, PPI); acute effects on thermoregulation (in group-/individually-housed rats); and systemic toxicity (median lethal dose, LD50) in Wistar rats...
August 1, 2016: Progress in Neuro-psychopharmacology & Biological Psychiatry
Ansoo Lee, Hyunwoo Kim
A complementary solution for Rh-catalyzed enantioselective 1,2- and 1,4-arylation with two structurally related chiral ligands is reported. A chiral bicyclic bridgehead phosphoramidite (briphos) ligand derived from 1-aminoindane was efficient for the 1,2-arylation of N-sulfonyl imines, while that derived from 1,2,3,4-tetrahydro-1-naphthylamine was efficient for 1,4-arylation of α,β-unsaturated cyclic ketones. For α,β-unsaturated N-tosyl ketimines, the briphos derived from 1-aminoindane was found to selectively provide γ,γ-diaryl N-tosyl enamines with high yields and stereoselectivities...
May 6, 2016: Journal of Organic Chemistry
Ting Wang, Leting Yang, Jing Hua, Huiru Xie, Xuehua Jiang, Ling Wang
Rasagiline is a selective, irreversible inhibitor of monoamine oxidase type-B (MAO-B) and has been used both as a monotherapy and in addition to levodopa in the treatment of Parkinson's disease (PD). Rasagiline is metabolized by the cytochrome P450 (CYP) system, and the following three major metabolites with potential neuroprotective activity have been identified: 1-aminoindan (AI), 3-hydroxy-N-propargyl-1-aminoindan (3-OH-PAI) and 3-hydroxy-1-aminoindan (3-OH-AI). In this study, a novel liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous determination of rasagiline and its major metabolites in human plasma...
June 5, 2016: Journal of Pharmaceutical and Biomedical Analysis
Michael B Gatch, Sean B Dolan, Michael J Forster
5,6-Methylenedioxy-2-aminoindane (MDAI) has become a common substitute for (±)-3,4-methylenedioxymethamphetamine (MDMA) in Ecstasy. MDAI is known to produce MDMA-like discriminative stimulus effects, but it is not known whether MDAI has psychostimulant or hallucinogen-like effects. MDAI was tested for locomotor stimulant effects in mice and subsequently for discriminative stimulus effects in rats trained to discriminate cocaine (10 mg/kg, intraperitoneally), methamphetamine (1 mg/kg, intraperitoneally), ±MDMA (1...
September 2016: Behavioural Pharmacology
Xia Chen, Qian Zhao, Ji Jiang, Jian Liu, Pei Hu
BACKGROUND AND OBJECTIVE: Although there is evidence indicating cytochome P450 (CYP) 1A2 is responsible for the metabolism of rasagiline, the role of other CYP isoforms is unclear. This study investigated the pharmacokinetics of rasagiline in adult Chinese healthy volunteers with various CYP genotypes. METHODS: This single-center, open-label study was conducted in 12 subjects. Fasted subjects received rasagiline 1 mg daily for 7 days. Blood samples were taken to determine plasma concentrations of rasagiline, its major metabolite R-1-aminoindan (AI), and the genotyping of CYP2D6 and CYP2C19...
May 2016: Clinical Drug Investigation
Sara Odoardi, Francesco Saverio Romolo, Sabina Strano-Rossi
The diffusion of New Psychoactive Substances (NPS) in the illicit drug market is a worldwide problem. The aim of the study is to describe the qualitative distribution of drugs of abuse in seized materials confiscated in the Italian territory over the last two years. Between 2013 and 2015 162 seizures of substances purchased through the Internet and confiscated by police authorities were analyzed: 35 seizures (22%) were crystals of 3-methylmethcathinone (3-MMC). Although 3-MMC is subject to the relevant legislation in Italy, it is not controlled in other countries such as the Netherlands, from which the shipments originated...
August 2016: Forensic Science International
Linda D Simmler, Danièle Buchy, Sylvie Chaboz, Marius C Hoener, Matthias E Liechti
Trace amine-associated receptor 1 (TAAR1) has been implicated in the behavioral effects of amphetamine-type stimulant drugs in rodents. TAAR1 has also been suggested as a target for novel medications to treat psychostimulant addiction. We previously reported that binding affinities at TAAR1 can differ between structural analogs of psychostimulants, and species differences have been observed. In this study, we complement our previous findings with additional substances and the determination of functional activation potencies...
April 2016: Journal of Pharmacology and Experimental Therapeutics
S Pal Choudhuri, R J Delay, E R Delay
G-protein-coupled receptors are thought to be involved in the detection of umami and L-amino acid taste. These include the heterodimer taste receptor type 1 member 1 (T1r1)+taste receptor type 1 member 3 (T1r3), taste and brain variants of mGluR4 and mGluR1, and calcium sensors. While several studies suggest T1r1+T1r3 is a broadly tuned lLamino acid receptor, little is known about the function of metabotropic glutamate receptors (mGluRs) in L-amino acid taste transduction. Calcium imaging of isolated taste sensory cells (TSCs) of T1r3-GFP and T1r3 knock-out (T1r3 KO) mice was performed using the ratiometric dye Fura 2 AM to investigate the role of different mGluRs in detecting various L-amino acids and inosine 5' monophosphate (IMP)...
March 1, 2016: Neuroscience
Aurélie Ledreux, Heather A Boger, Vanessa K Hinson, Kelsey Cantwell, Ann-Charlotte Granholm
The anti-Parkinsonian drug rasagiline is a selective, irreversible inhibitor of monoamine oxidase and is used in the treatment of Parkinson׳s disease (PD). Its postulated neuroprotective effects may be attributed to MAO inhibition, or to its propargylamine moiety. The major metabolite of rasagiline, aminoindan, has shown promising neuroprotective properties in vitro but there is a paucity of studies investigating in vivo effects of this compound. Therefore, we examined neuroprotective effects of rasagiline and its metabolite aminoindan in a double lesion model of PD...
January 15, 2016: Brain Research
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