Abstract
Bromo-Dragonfly (BDF) is a designer drug chemically related to LSD and amphetamine. The first registration in Denmark was in October 2007. In the present case an 18-year-old man ingested about 2 ml BDF and developed acute psychosis. At the hospital the patient displayed, hyperpyrexia, tachycardia, t...
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PMID: 20470659
PDF is available here.
Abstract
Thirty-two psychotropic substances were listed as designated substances (Shitei-Yakubutsu, 31 compounds and 1 plant) in Japan by the Pharmaceutical Affairs Law in April 2007 for preventing the abuse of these substances. Subsequently, other psychoactive compounds were also added to this category, 40...
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PMID: 20118651
PDF is available here.
Abstract
We describe a generic protocol for the directed molecular evolution of designer receptors exclusively activated by designer drugs (DREADDs). First, the yeast system is validated with the template receptor. Second, a mutant library is generated by error-prone PCR. Third, the library is screened by dr...
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PMID: 20203671
PDF is available here.
Abstract
Anabolic steroids have been studied for over 50 years and during that time numerous compounds with a variety of functional groups have been produced and many have been published. Of these only a small number have been introduced to the pharmaceutical market. WADA has continued the work begun by the...
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PMID: 20020364
PDF is available here.
Abstract
Fluorophenylpiperazine, methoxyphenylpiperazine, chlorophenylpiperazine, methylbenzylpiperazine and methylenedioxybenzylpiperazine had significant inhibitory effects on CYP2D6, CYP1A2, CYP3A4, CYP2C19 and CYP2C9 isoenzymes but each piperazine had a different inhibitory profile. The metabolic interac...
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PMID: 19589229
PDF is available here.
Abstract
We present crystal structures of the editing domain from two eukaryotic cytosolic LeuRS: human and fungal pathogen Candida albicans. In comparison with previous structures of the editing domain from bacterial and archeal kingdoms, these structures show that the LeuRS editing domain has a conserved s...
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PMID: 19426743
PDF is available here.
Abstract
The increasing problem of antibiotic resistance among pathogenic bacteria requires development of new antimicrobial agents. The pivotal assets of the antimicrobial peptide include potential for rapid bactericidal activity and low propensity for resistance. The four new antimicrobial hybrid peptides...
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PMID: 19148638
PDF is available here.
Abstract
Some smokable herbal mixtures under the brand name Spice drugs have been sold on the Internet and in specialised shops (smart shops) since 2004. The mixtures are advertised as an exotic incense blend which releases a rich aroma and not for human consumption. When smoked, Spice drugs products have be...
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PMID: 19718488
PDF is available here.
Abstract
We have analyzed the yeast androgen receptor (AR) reporter gene system to identify anabolic steroids in human urine samples. Analysis of different anabolic steroids dissolved in buffer demonstrated that the yeast reporter gene system is able to detect a variety of different anabolic steroids and the...
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PMID: 18550137
PDF is available here.
Abstract
We will discuss the recent development and the strategies to optimize the effectiveness of designer therapy for GBM....
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PMID: 18990124
PDF is available here.
Abstract
Expressed sequence tag (EST), proteomic, and antibody capture assays are revealing a level of tear film protein complexity far greater than previously appreciated. A systems biology approach will be needed to fully appreciate function as tear protein doses fluctuate in time through different conditi...
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PMID: 18677231
PDF is available here.
Abstract
We present the scientific rationale and study design, discuss key data from other trials, and summarize our expectations of this study....
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PMID: 18363672
PDF is available here.
Abstract
A newly synthesized designer drug, para-methoxyethylamphetamine (PMEA) was unexpectedly detected in the postmortem specimens of fatality involving drug intoxication in 2005, Japan. For unequivocal identification, the isomeric discrimination of PMEA and its positional-isomers was performed by GC/MS w...
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PMID: 18155375
PDF is available here.
Abstract
Androgens remain the most effective and widely abused ergogenic drugs in sport. Although androgen doping has been prohibited for over 3 decades with a ban enforced by mass spectrometric (MS)-based urine testing for synthetic and exogenous natural androgens, attempts continue to develop increasingly...
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PMID: 18385902
PDF is available here.
Abstract
Studies are described on the metabolism and the toxicological detection of the phencyclidine-derived designer drug N-(1-phenylcyclohexyl)-propanamine (PCPR) in rat urine using gas chromatographic-mass spectrometric techniques. The identified metabolites indicated that PCPR was metabolized by hydroxy...
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PMID: 18035363
PDF is available here.
Abstract
A reliable and accurate GC-MS method was developed that allows both mass spectrometric and chromatographic discrimination of the six aromatic positional isomers of trimethoxyamphetamine (TMA). Regardless of the trifluoroacetyl (TFA) derivatization, chromatographic separation of all the investigated...
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PMID: 18035853
PDF is available here.
Abstract
We have characterized the concentration-dependent alignment and dynamic behavior of MSI-103 in lipid membranes by solid-state 2H and 19F NMR, using orientational constraints from seven Ala-d3-labeled analogues and five 4-CF3-phenylglycine labels. As previously found for PGLa, MSI-103, too, assumes a...
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PMID: 18220419
PDF is available here.
Abstract
Studies are described on the metabolism and the toxicological detection of the phencyclidine-derived designer drugs N-(1-phenylcyclohexyl)-2-ethoxyethanamine (PCEEA) and N-(1-phenylcyclohexyl)-2-methoxyethanamine (PCMEA) in rat urine using gas chromatographic/mass spectrometric (GC/MS) techniques. T...
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PMID: 17968862
PDF is available here.
Abstract
Anticoagulant therapy with heparin has been the cornerstone of treatment and prevention of thrombosis for many decades. The properties and indications of heparin, as well as the development of its derivates, the low-molecular-weight heparins, and ultimately the synthetically designed pentasaccharide...
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PMID: 17996279
PDF is available here.
Abstract
The involvement of human hepatic cytochrome P450 (P450) isoenzymes in the metabolism of the new designer drug 4'-methyl-alpha-pyrrolidinobutyrophenone (MPBP) to 4'-(hydroxymethyl)-alpha-pyrrolidinobutyrophenone (HO-MPBP) was studied using insect cell microsomes with cDNA-expressed human P450s and hu...
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PMID: 17962373
PDF is available here.
Abstract
Releasable PEGylation employs customized linkers that reversibly tether a therapeutic moiety with polyethylene glycol polymers. The choice of releasable PEG linkers may have numerous applications that are insufficiently addressed by stable polymer attachment. Releasable PEGylation provides regenerat...
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PMID: 17884239
PDF is available here.
Abstract
The amphetamine-derived designer drug 4-iodo-2,5-dimethoxy-amphetamine (DOI) is an upcoming substance on the illicit drug market. In the current study, the identification of its metabolites in rat urine and their toxicological detection in the authors' systematic toxicological analysis (STA) procedu...
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PMID: 17632045
PDF is available here.
Abstract
This paper documents the bifurcation of the market for commercial marijuana from the market for designer marijuana in New York City. Commercial marijuana is usually grown outdoors, imported to NYC, and of average quality. By contrast, several varities of designer marijuana are usually grown indoors...
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PMID: 17055670
PDF is available here.
Abstract
In recent years, the frequent appearance of phenethylamine designer drugs on the illicit drug market has been a matter of concern for all authorities involved. New phenethylamine drugs are being introduced because these compounds are not covered by existing legislation. Therefore, the new drugs cann...
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PMID: 17098243
PDF is available here.
Abstract
Drugs of abuse belonging to the amphetamine derivatives, which are often taken by adolescents and young adults, pose a serious risk associated with uncontrolled ingestion that sometimes leads to fatal outcomes. The number of deaths, however, related to Ecstasy is small when compared to the frequency...
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PMID: 17320458
PDF is available here.
Abstract
We examined the effects of a newly popular drug, 5-methoxy-diisopropyltryptamine (5-MEO-DIPT; 'foxy' or 'foxy-methoxy'). Two experiments were performed. In the first, 5-MEO-DIPT (0, 10, or 20 mg/kg) was administered to rats four times on a single day and animals were examined 3 days later. The anima...
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PMID: 17047665
PDF is available here.
Abstract
The aim of this study was to evaluate the Bio-Quant Direct ELISA assays for amphetamine and methamphetamine in the routine presumptive screening of biological fluids. Standard concentration curves of the target analytes were assayed to assess sensitivity, and known concentrations of common amphetami...
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PMID: 17555644
PDF is available here.
Abstract
A new analogue of sildenafil was detected in an herbal dietary supplement, which was sold over the internet and promoted as a product for the enhancement of sexual performance. The structure of the compound was established using LC-MS, UV spectroscopy, MS-MS, and NMR. In addition, the compound was c...
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PMID: 17207601
PDF is available here.
Masanari M Itokawa,
Ken K Iwata,
Misako M Takahashi,
Gen-Ichi G Sugihara,
Takeshi T Sasaki,
Yu-Ichiro Y Abe,
Minari M Uno,
Mizue M Hobo,
Daisuke D Jitoku,
Kikue K Inoue,
Makoto M Arai,
Ichiro I Yasuda and
Masahiro M Shintani
Abstract
A 23-year-old Japanese woman was brought to the emergency department about 6.5 h after taking liquid and later a half tablet purchased on the street. About 4.5 h prior to presentation, she displayed excited and disorganized behavior. On examination, she was not alert or oriented, with a Glasgow Coma...
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PMID: 17362440
PDF is available here.
Abstract
We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive...
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PMID: 17223101
PDF is available here.
Abstract
We evolved muscarinic receptors in yeast to generate a family of G protein-coupled receptors (GPCRs) that are activated solely by a pharmacologically inert drug-like and bioavailable compound (clozapine-N-oxide). Subsequent screening in human cell lines facilitated the creation of a family of muscar...
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PMID: 17360345
PDF is available here.
Abstract
A liquid chromatography/time-of-flight mass spectrometry (LC/TOFMS) method was developed using the latest high-resolution LC column technology, the ultra performance liquid chromatography (UPLC), and electrospray ionization (ESI) in the positive ion mode. Gradient UPLC separation conditions were opt...
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PMID: 17386705
PDF is available here.
Abstract
Cholesterol is a well-known component in fats of animal origin and it also is the precursor of natural hormones. Phytosterols appear in plants and only differ slightly in structure from cholesterol. An important difference however is the low absorption in the gut of phytosterols and their saturated...
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PMID: 17386696
PDF is available here.
Abstract
Emerging research will likely make it possible to tailor pharmacological treatment for individuals with tobacco dependence by genotype. This study explored primary care physicians' attitudes about the strengths of and barriers to using genetic testing to match patients to optimal nic...
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PMID: 17365758
PDF is available here.
Helena Carmo,
Marc Brulport,
Matthias Hermes,
Franz Oesch,
Douwe de Boer,
Fernando Remião,
Félix Carvalho,
Michael R Schön,
Niels Krebsfaenger,
Johannes Doehmer,
Maria de Lourdes Bastos and
Jan G Hengstler
Abstract
We tested whether CYP2D6 or its variant alleles as well as CYP3A4 influence the susceptibility to 4-MTA. For this purpose, we used the colony formation assay with Chinese hamster lung fibroblast V79 cells expressing human wild-type CYP2D6 (CYP2D6*1), the low activity alleles CYP2D6*2, CYP2D6*9, as w...
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PMID: 17156908
PDF is available here.
Abstract
A new combined doping control screening method for the analysis of anabolic steroids in human urine using liquid chromatography/electrospray ionization orthogonal acceleration time-of-flight mass spectrometry (LCoaTOFMS) and gas chromatography/electron ionization orthogonal acceleration time-of-flig...
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PMID: 17610244
PDF is available here.
Abstract
A simple method for the simultaneous identification and quantification of four 2,5-methylenedioxy derivatives of 4-thioamphetamine (ALEPH series) in plasma samples was developed. The method consists of solid-phase extraction (SPE) using a Bond Elut C(18) cartridge and capillary electrophoresis coupl...
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PMID: 17955568
PDF is available here.
Abstract
The GC-MS method after mix-mode solid-phase extraction and derivatization with heptafluorobutyric anhydride is presented for screening followed by identification and quantification of AMP, MAMP, EPH, NOREPH, MDA, MDMA, MDEA, and MBDB. The applicability of the GC-MS method was proven by analyzing aut...
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PMID: 17159795
PDF is available here.
Abstract
The phenethylamine-derived designer drug 2,5-dimethoxy-4-methyl-beta-phenethylamine (2C-D) was found to be metabolized in rats by O-demethylation at position 2 or 5 followed by N-acetylation or by deamination with oxidation to the corresponding acids or reduction to the corresponding alcohol. Furthe...
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PMID: 17103384
PDF is available here.
Abstract
Studies are described on the metabolism and the toxicological detection of the amphetamine-derived designer drug 2,4,5-trimethoxyamphetamine (TMA-2) in rat urine using gas chromatographic/mass spectrometric (GC/MS) techniques. The identified metabolites indicated that TMA-2 was metabolized by oxidat...
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PMID: 16810708
PDF is available here.
Abstract
An herbal dietary supplement, marketed as a natural product for the enhancement of sexual function, was purchased covertly over the internet. The product was analyzed by LC-MS and found to contain a compound related to synthetic phosphodiesterase 5 (PDE-5) inhibitors. Based on LC with photodiode arr...
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PMID: 16750214
PDF is available here.
Abstract
These results demonstrate that the analysis of HMMC will be indispensable for proof of the use of methylone in forensic urinalysis....
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PMID: 16891251
PDF is available here.
Abstract
Studies are described on the metabolism and toxicological detection of the phencyclidine-derived designer drug N-(1-phenylcyclohexyl)-3-ethoxypropanamine (PCEPA) in rat urine using gas chromatographic/mass spectrometric techniques. The identified metabolites indicated that PCEPA was metabolized by N...
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PMID: 16817170
PDF is available here.