Abstract:
:Higenamine was included in the World Anti-Doping Agency (WADA) Prohibited Substances and Methods List as a β2 -adrenoceptor agonist in 2017, thereby resulting in its prohibition both in and out of competition. The present mini review describes the physiology and pharmacology of adrenoceptors, summarizes the literature addressing the mechanism of action of higenamine and extends these findings with previously unpublished in silico and in vitro work. Studies conducted in isolated in vitro systems, whole-animal preparations and a small number of clinical studies suggest that higenamine acts in part as a β2 -adrenoceptor agonist. In silico predictive tools indicated that higenamine and possibly a metabolite have a high probability of interacting with the β2 -receptor as an agonist. Stable expression of human β2 -receptors in Chinese hamster ovary (CHO) cells to measure agonist activity not only confirmed the activity of higenamine at β2 but also closely agreed with the in silico prediction of potency for this compound. These data confirm and extend literature findings supporting the inclusion of higenamine in the Prohibited List.
journal_name
Drug Test Analjournal_title
Drug testing and analysisauthors
Hudzik TJ,Patel M,Brown Adoi
10.1002/dta.2992subject
Has Abstractpub_date
2020-12-26 00:00:00eissn
1942-7603issn
1942-7611pub_type
杂志文章,评审abstract::Fast and unequivocal drug detection is of considerable importance in numerous fields of analytical chemistry, and today mass spectrometry-based approaches are often the method of choice due to their sensitive and specific nature. Mass spectrometry is in constant flux with innovations and thus supports the development ...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.344
更新日期:2012-03-01 00:00:00
abstract::The absence of reference material is a commonly experienced difficulty among medical and forensic professionals tasked with identifying new psychoactive substances that are encountered for the first time. The identification of newly emerging substances lies at the heart of forensic and clinical analysis, and a proacti...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.398
更新日期:2012-01-01 00:00:00
abstract::The steroid profile (SP) is a powerful tool to detect the misuse of endogenous anabolic androgenic steroids in sports, and it is included in the Athlete Biological Passport (ABP). Glucocorticoids (GCs), which are widely prescribed in sports and only prohibited in competition by systemic routes, inhibit the hypothalami...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2351
更新日期:2018-06-01 00:00:00
abstract::Knowing that polyunsaturated fatty acids can lead to the formation of potentially toxic aldehydes as secondary oxidation products, an analytical method using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) detection was developed to measure the concentration of eight aldehydes in animal feed: malo...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2013
更新日期:2016-05-01 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::A new and sensitive multi-residue method (MRM) with detection by LC-MS/MS was developed and validated for the screening, determination, and confirmation of residues of 7 nitroimidazoles and 3 of their metabolites in turkey muscle tissues at concentrations ≥ 0.05 ng/g. The compounds were extracted into a solvent with a...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1356
更新日期:2012-08-01 00:00:00
abstract::1-Propanoyl-lysergic acid diethylamide (1P-LSD) appeared as a non-controlled alternative to LSD a few years ago. Although evidence is beginning to emerge from in vitro and animal studies that 1P-LSD might serve as a prodrug for LSD, an equivalent evaluation in humans is unavailable. Controlled oral and intravenous sel...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2821
更新日期:2020-08-01 00:00:00
abstract::Synthetic cannabinoids are a group of psychoactive drugs presently widespread among drug users in Europe. Analytical methods to measure these compounds in urine are in demand as urine is a preferred matrix for drug testing. For most synthetic cannabinoids, the parent compounds are rarely detected in urine. Therefore u...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1896
更新日期:2016-09-01 00:00:00
abstract::Since the appearance of recombinant human growth hormone (rhGH) in the 1980s, its expansion and acquisition through the black market has increased, so the detection of its abuse continues to be a challenge. New biomarkers that are more reliable and sensitive, allowing a larger detection window, are still needed. In th...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2108
更新日期:2017-07-01 00:00:00
abstract::We recently published two protocols for the detection of Sotatercept (ACE-011, ACVR2A-Fc) and Luspatercept (ACE-536, ACVR2B-Fc) in human serum. Both methods used covalently immobilized antibodies on agarose beads for immunoprecipitation and SAR-PAGE/Western blotting for detection. Disadvantages were the relatively hig...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2500
更新日期:2018-11-01 00:00:00
abstract::Cobalt is a well-established inducer of hypoxia-like responses, which can cause gene modulation at the hypoxia inducible factor pathway to induce erythropoietin transcription. Cobalt salts are orally active, inexpensive, and easily accessible. It is an attractive blood doping agent for enhancing aerobic performance. I...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1719
更新日期:2015-01-01 00:00:00
abstract::An orthogonal signal correction-partial least squares (OSC-PLS) method was developed for the simultaneous spectrophotometric determination of orotic acid (OA), creatinine (CRE), and uric acid (UA) in spiked real samples. By multivariate calibration methods, such as PLS regression, it is possible to obtain a model adju...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.375
更新日期:2013-05-01 00:00:00
abstract::Iso-α-acids (IAAs) can be used as markers for the consumption of beer. Postmortem specimens from a range of coronial cases were analyzed for IAAs in order to determine the prevalence of beer consumption and any correlation to blood alcohol concentrations (BAC). A total of 130 cases were included in this study includin...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1749
更新日期:2015-01-01 00:00:00
abstract::In Australia, drug monitoring systems have been in place for more than a decade allowing for the measurement of ongoing trends in drug use and the detection of new drugs. The Drug Trends Unit at the National Drug and Alcohol Research Centre monitors drugs through four separate systems. The Illicit Drug Reporting Syste...
journal_title:Drug testing and analysis
pub_type: 杂志文章,评审
doi:10.1002/dta.1613
更新日期:2014-07-01 00:00:00
abstract::Trimethoprim (TMP) is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections. It belongs to the class of chemotherapeutic agents known as dihydrofolate reductase inhibitors. Its use is associated with idiosyncratic reactions, including liver toxicity and agranulocytosis. I...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.161
更新日期:2010-09-01 00:00:00
abstract::The accuracy in predicting different chemometric methods was compared when applied on ordinary UV spectra and first order derivative spectra. Principal component regression (PCR) and partial least squares with one dependent variable (PLS1) and two dependent variables (PLS2) were applied on spectral data of pharmaceuti...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.235
更新日期:2011-05-01 00:00:00
abstract::Evidence of the continuous rise of novel doping agents and novel doping strategies calls for the development of more accurate multi-target screening methods. Direct multi-target screening approaches are restricted to the targeted substances and their turnover. The development of effective "indirect" screening methods ...
journal_title:Drug testing and analysis
pub_type: 杂志文章,评审
doi:10.1002/dta.2788
更新日期:2020-06-01 00:00:00
abstract::This work presents an analytical procedure for the identification and characterization of liposome-entrapped haemoglobins, based on flow cytofluorimetry. Flow cytofluorimetric detection is carried out following labelling by two distinct fluorescent reagents, an anti-haemoglobin antibody, fluorescein isothiocyanate con...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1956
更新日期:2017-02-01 00:00:00
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 increa...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1530
更新日期:2014-07-01 00:00:00
abstract::Anabolic-androgenic steroids are synthetic compounds prohibited due to their performance-enhancing characteristics. The use of these substances is known to cause health-related issues, which highlights the importance of being able to evaluate the scale of consumption by the general population. However, most available ...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2591
更新日期:2019-07-01 00:00:00
abstract::The consumption of drugs is of great concern worldwide. Various drug tests for humans have been developed but there is no compact and easy-to-use test device available yet for direct semi-quantitative drug testing in the field. We suggest using attenuated total reflection (ATR) infrared spectroscopy as a sensing metho...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.346
更新日期:2012-06-01 00:00:00
abstract::The amphetamine molecule contains a chiral center and its enantiomers exhibit differences in pharmacological effects, with the S-enantiomer mediating most of the central nervous system stimulating activity. The majority of prescribed amphetamine consists of the pure S-enantiomer, but therapeutic formulations containin...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2879
更新日期:2020-09-01 00:00:00
abstract::Development of a mass spectrometric method for the unambiguous detection of doping with recombinant human erythropoietins (rhEPO) has been attempted for many years. Unfortunately, progress in this field was hampered by the unavailability of highly purified human endogenous EPOs (urinary[uhEPO], serum/plasma EPO)--a pr...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1563
更新日期:2013-11-01 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::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::Several clinical-grade immunoassays exist for the specific measurement of hGH or its isoforms in blood but there is an urgent need to apply these same reliable assays to the measurement of hGH in urine as a preferred 'non-invasive' biofluid. Unfortunately, conventional hGH immunoassays cannot attain the sensitivity re...
journal_title:Drug testing and analysis
pub_type: 杂志文章,评审
doi:10.1002/dta.96
更新日期:2009-09-01 00:00:00
abstract::In the context of post-marketing surveillance supporting public-health authorities to take evidence-based decisions to fight the spread of poor-quality medicines, the quality of antimalarial artemether-lumefantrine (AL) medicines was assessed in the Democratic Republic of the Congo (DRC). A total of 150 samples of AL-...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2420
更新日期:2018-10-01 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::The purpose of this research is to validate the biomarker-based approach for the detection of doping with recombinant human growth hormone (rhGH) in sport. The GH-2000 project proposed an indirect method for the detection of exogenously administered growth hormone (GH) based on the measurement of the GH-dependent mark...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.1423
更新日期:2012-10-01 00:00:00
abstract::Deschloroketamine (2-(methylamino)-2-phenyl-cyclohexanone) is a ketamine analog belonging to a group of dissociative anesthetics, which have been distributed within the illicit market since 2015. However, it was also being sold as 'ketamine' misleading people to believe that they were getting genuine ketamine. Dissoci...
journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.2726
更新日期:2020-03-01 00:00:00