Abstract:
:5-(2-Aminopropyl)indole (5-IT) is a psychoactive compound that has recently been associated with several fatal and non-fatal intoxications in a number of European countries. There are indications that acute effects may include symptoms of monoaminergic (e.g. serotonin) toxicity and one mechanism involved in the increase of serotonin levels includes the inhibition of monoamine oxidase. This study investigated the effect of 5-IT on human MAO-A and -B isozymes using kynuramine as the substrate. Substrate conversion to 4-hydroxyquinoline was monitored by high-performance liquid chromatography coupled to diode array detection. This method was employed to determine the extent of MAO inhibition (IC50 and Ki ) and it was found that 5-IT was a selective, competitive and reversible inhibitor of MAO-A. 5-IT revealed a relatively potent ability to inhibit MAO-A (IC50 =1.6 μM and Ki =0.25 μM) while MAO-B inhibition was not observed (0-500 μM 5-IT). Under identical experimental conditions, other established inhibitors of MAO-A and antidepressants provided the following IC50 values: clorgyline 16 nM, harmaline 20 nM, toloxatone 6.7 μM and moclobemide >500 μM. These data indicated that 5-IT was less potent than clorgyline and harmaline but more potent than toloxatone and moclobemide under the in-vitro conditions studied. The inhibition of MAO-A suggests that 5-IT by itself or in combination with other substances may be able to potentiate serotonergic/monoaminergic effects and further studies are needed to clarify its relevance to the adverse effects reported for 5-IT.
journal_name
Drug Test Analjournal_title
Drug testing and analysisauthors
Herraiz T,Brandt SDdoi
10.1002/dta.1530subject
Has Abstractpub_date
2014-07-01 00:00:00pages
607-13issue
7-8eissn
1942-7603issn
1942-7611journal_volume
6pub_type
杂志文章abstract::Current doping trends overshadow the traditional interpretation of using prohibited performance-enhancing drugs to improve training and/or sports results. Its definition has evolved due to several recent cases of unconventional manipulation in sports. In this article, we present a case study of an intentional intoxica...
journal_title:Drug testing and analysis
pub_type: 历史文章,杂志文章
doi:10.1002/dta.2753
更新日期:2020-05-01 00:00:00
abstract::The Ministry of Health in the Netherlands has made illicit drug testing for drug users possible since the 1990s, in order to prevent serious health hazards associated with unexpected dangerous substances. This system of illicit drug testing is called the Drug Information and Monitoring System (DIMS). In nearly two dec...
journal_title:Drug testing and analysis
pub_type: 杂志文章,评审
doi:10.1002/dta.323
更新日期:2011-09-01 00:00:00
abstract::Synthetic cathinones continue to proliferate in clandestine drug markets worldwide. N-ethylnorpentylone (also known as N-ethylpentylone or ephylone) is a popular emergent cathinone, yet little information is available about its toxicology and pharmacology. Here we characterize the analytical quantification, clinical p...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2502
更新日期:2019-03-01 00:00:00
abstract::A novel poly (vinyl chloride) PVC membrane sensor for Fe(2+) ions is described. The sensor is based on the use of newly synthesized chiral 2,6-bis-(carboxamide methyl ester)pyridine derivative as neutral ionophore in plasticized PVC membrane. The sensor display a fast, stable and near-Nernstian response over a relativ...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.231
更新日期:2011-06-01 00:00:00
abstract::The laboratory anti-doping services during XXII Winter Olympic and XI Paralympic games in Sochi in 2014 were provided by a satellite laboratory facility located within the strictly secured Olympic Park. This laboratory, established and operated by the personnel of Antidoping Center, Moscow, has been authorized by the ...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1734
更新日期:2014-11-01 00:00:00
abstract::Clinical and forensic toxicology laboratories are continuously confronted by analytical challenges when dealing with the new psychoactive substances phenomenon. The number of synthetic cannabinoids, the chemical diversity, and the speed of emergence make this group of compounds particularly challenging in terms of det...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2160
更新日期:2017-08-01 00:00:00
abstract::Clostebol is a synthetic anabolic androgenic steroid, with potential use as a performance-enhancing drug if taken for long periods in order to produce the desired effect. Recently, the use of medications containing clostebol acetate has led to the suspension of several athletes in various sports. Previous studies have...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2469
更新日期:2019-01-01 00:00:00
abstract::In Italy, Workplace Drug Testing (WDT) has been compulsory by law for specific categories of workers since 2008, offering the opportunity to compare studies conducted within a single regulatory framework. The aims of this paper are to estimate the overall prevalence of WDT positivity (at screening survey) among Italia...
journal_title:Drug testing and analysis
pub_type: 杂志文章,meta分析,评审
doi:10.1002/dta.2189
更新日期:2017-06-01 00:00:00
abstract::Chemical warfare agents (CWA) are highly toxic compounds which have been produced to kill or hurt people during conflicts or terrorist attacks. Despite the fact that their use is strictly prohibited according to international convention, populations' exposure still recently occurred. Development of markers of exposure...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1659
更新日期:2014-06-01 00:00:00
abstract::Vaping of synthetic cannabinoids via e-cigarettes is growing in popularity. In the present study, we tentatively identified 12 by-products found in a pure sample of the synthetic cannabinoid Cumyl-5F-PINACA (1-(5-fluoropentyl)-N-(2-phenylpropan-2-yl)-1H-indazole-3-carboxamide), a prevalent new psychoactive substance (...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2673
更新日期:2020-01-01 00:00:00
abstract::The determination of protein- or peptide-based performance-enhancing pharmaceuticals has gained increasing attention in sports drug testing in recent decades. Proteases possess a high potential for use in the manipulation of regular urine specimens, interfering with established doping control procedures for proteins o...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.20
更新日期:2009-02-01 00:00:00
abstract::Despite the implementation of a new blanket scheduling system in 2013, new psychoactive substance (NPS) abuse remains a serious social concern in Japan. We present a fatal intoxication case involving 5F-ADB (methyl 2-[1-(5-fluoropentyl)-1H-indazole-3-carboxamido]-3,3-dimethylbutanoate) and diphenidine. Postmortem bloo...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2215
更新日期:2018-02-01 00:00:00
abstract::Musk, the dried secretion of the musk pod (sac) of adult male musk deer, has been used as traditional Chinese Medicine (TCM) in China and south-east Asian countries for thousands of years. Due to the anabolic steroid component in this TCM, musk preparations have been included in the list of medical products containing...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2293
更新日期:2017-11-01 00:00:00
abstract::MicroRNAs (miRNAs) are small, non-protein coding transcripts involved in many cellular and physiological mechanisms. Recently, a new class of miRNA called 'circulating miRNAs' was found in cell-free body fluids such as plasma and urine. Circulating miRNAs have been shown to be very stable, specific, and sensitive biom...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.370
更新日期:2011-11-01 00:00:00
abstract::A sensitive and selective ultra fast liquid chromatography (UFLC) method has been developed and validated for the determination of a potent and novel antitubercular compound S006-830 in Sprague Dawley (SD) rat plasma. Samples were extracted and processed by protein precipitation method using acetonitrile. Chromatograp...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1748
更新日期:2015-08-01 00:00:00
abstract::Flubromazolam is a triazole benzodiazepine with high potency and long-lasting central nervous system depressant effects; however, limited data about its pharmacokinetics are available. Here, we report in vitro studies of the human flubromazolam metabolism analyzed by liquid chromatography high-resolution mass spectrom...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2146
更新日期:2017-08-01 00:00:00
abstract::Standard treatment of poisoning by organophosphorus (OP) nerve agents with atropine and oximes lacks efficacy with some nerve agents. Promising in vitro and in vivo results were obtained with the bispyridinium compound SAD-128 which was partly attributed to its interaction with nicotinic acetylcholine receptors. Previ...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.410
更新日期:2012-03-01 00:00:00
abstract::In this tutorial we describe the construction of chemiluminescence detectors for high performance liquid chromatography (HPLC), comprising the components required to deliver the chemiluminescence reagent, a coiled-tubing flow cell, photomultiplier tube and detector housing, and various options for data acquisition. We...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.132
更新日期:2011-03-01 00:00:00
abstract::Buprenorphine and methadone are commonly used medications for opioid maintenance treatment (OMT), using sublingual and oral administration, respectively. Although beneficial for OMT, these drugs can also be abused by intravenous administration. In intravenous abuse cases, the adjuvants lactose and sucrose are excreted...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2050
更新日期:2017-06-01 00:00:00
abstract::Testosterone and related compounds are the most recurrent doping substances. The steroid profile, consisting of the quantification of testosterone and its metabolites, has been described as the most significant biomarker to detect doping with pseudo-endogenous anabolic steroids. The steroidal module of the Athlete Bio...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1851
更新日期:2016-07-01 00:00:00
abstract::The present study was designed to provide preliminary information on the potential impact of metabolic drug-drug interaction on the effectiveness of doping control strategies currently followed by the anti-doping laboratories to detect the intake of prohibited agents. In vitro assays based on the use of human liver mi...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1608
更新日期:2014-10-01 00:00:00
abstract::Abuse of gamma-hydroxybutyric acid (GHB) has been known since the early 1990's, but is not as widespread as the consumption of other illegal drugs. However, the number of severe intoxications with fatal outcomes is comparatively high; not the least of which is brought about by the consumption of the currently legal pr...
journal_title:Drug testing and analysis
pub_type: 杂志文章,评审
doi:10.1002/dta.254
更新日期:2011-09-01 00:00:00
abstract::Three multivariate calibration methods, including classical least square with nonzero intercept (CLS), principal component regression (PCR) and partial least square (PLS), have been used for the determination of pyritinol dihydrochloride in the presence of its degradation product. The CLS, PCR and PLS techniques are u...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.37
更新日期:2009-05-01 00:00:00
abstract::The impact of altitude training on haematological parameters and the Athlete Biological Passport (ABP) was evaluated in international-level elite athletes. One group of swimmers lived high and trained high (LHTH, n = 10) for three to four weeks at 2130 m or higher whereas a control group (n = 10) completed a three-wee...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1757
更新日期:2015-08-01 00:00:00
abstract::Classic examples of psychoactive arylcycloalkylamines include ketamine and 1-(1-phenylcyclohexyl)piperidine (PCP) and many others serve as important structural templates for neuropharmacological research. The recent emergence of PCP analogues that can be obtained from internet retailers requires the implementation of ...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1468
更新日期:2014-07-01 00:00:00
abstract::Designer drugs belong to a group of legally or illegally produced substances that are structurally and pharmacologically very similar to illicit drugs. In the past, designer drugs were often used during all-night dance parties, but they are now consumed in multiple settings from college bars to parks to private house ...
journal_title:Drug testing and analysis
pub_type: 杂志文章,评审
doi:10.1002/dta.210
更新日期:2011-09-01 00:00:00
abstract::A simple, sensitive, and selective spectrophotometric method has been developed for the determination of gabapentin (GBP) in capsules. The method is based on the reaction of GBP and sodium 1,2-naphthoquinone-4-sulfonate (NQS) in the presence of Clark and Lubs buffer of pH 11 to form an orange-coloured product which wa...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.242
更新日期:2011-10-01 00:00:00
abstract::The widespread use of antibiotics in animals is causing concerns about the growing risk for development and the spread of antibiotic-resistant bacteria. Antibiotic consumption is higher in animals than in humans as reported in a joint publication of EFSA (European Food Safety Agency), ECDC (European Centre for Disease...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2010
更新日期:2016-05-01 00:00:00
abstract::The direct alcohol marker ethyl glucuronide (EtG) is widely used for the assessment of alcohol consumption behavior and abstinence monitoring by hair analysis. We investigated the influence of chlorinated swimming pool water on EtG concentrations in hair in comparison to deionized water (Milli-Q) containing no chlorin...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2295
更新日期:2018-04-01 00:00:00
abstract::Driving under the influence of drugs (DUID) is a worldwide problem. Several countries have adopted DUID legislations which prove their deterrent effect and impact on road safety. However, the use of new psychoactive substances (NPS) and prescription drugs is not known, as the applied roadside screening tests have not ...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2232
更新日期:2018-03-01 00:00:00