Characterization of the designer benzodiazepine pyrazolam and its detectability in human serum and urine

  title={Characterization of the designer benzodiazepine pyrazolam and its detectability in human serum and urine},
  author={Bjoern Moosmann and Melanie Hutter and Laura M Huppertz and Sascha Ferlaino and Lisa Redlingsh{\"o}fer and Volker Auw{\"a}rter},
  journal={Forensic Toxicology},
In 2012, online shops selling so-called research chemicals started offering pyrazolam, a new benzodiazepine that differs from phenazepam and etizolam, which have also recently appeared on the “gray market”, in that it is not marketed by pharmaceutical companies anywhere in the world. This article describes the characterization of pyrazolam (8-bromo-1-methyl-6-pyridin-2-yl-4H-[1,2,4]triazolo[4,3–a][1, 4]benzodiazepine) using gas chromatography-mass spectrometry, liquid chromatography-tandem mass… 
Detection and identification of the designer benzodiazepine flubromazepam and preliminary data on its metabolism and pharmacokinetics.
Flubromazepam appears to have an extremely long elimination half-life of more than 100 h, which means that it could be misused in drug-withdrawal settings or in other circumstances requiring regular drug testing, and may be used indrug-facilitated crimes without being detected.
Characterization of the designer benzodiazepine diclazepam and preliminary data on its metabolism and pharmacokinetics.
Based on this study, diclazepam has an approximate elimination half-life of 42 h and is metabolized into the pharmacologically active benzodiazepines delorazepAm, lorazEPam, and lormetazep am which can be detected in urine for 6, 19, and 11 days, respectively, when applying the presented LC-MS/MS method.
Human urinary metabolic patterns of the designer benzodiazepines flubromazolam and pyrazolam studied by liquid chromatography-high resolution mass spectrometry.
This study performed to further investigate the human metabolic pattern of the NPS, or designer benzodiazepines flubromazolam and pyrazolam, and to propose analytical targets for urine drug testing of these substances.
Detection of the designer benzodiazepine metizolam in urine and preliminary data on its metabolism.
The most relevant potential CYP- and UGT-dependent metabolites of metizolam were investigated in vitro using human liver microsome incubation and, subsequently, liquid chromatography coupled with quadrupole-time of flight mass spectrometry (UHPLC-Q-TOF-MS) analysis.
Bioanalytical studies of designer benzodiazepines
The fast appearance of benzodiazepine analogues, referred to as new psychoactive substance (NPS) or designer benzodiazepines, requires the continuous update of detection methods in order to keep up
Characterization and in vitro phase I microsomal metabolism of designer benzodiazepines: An update comprising flunitrazolam, norflurazepam, and 4'-chlorodiazepam (Ro5-4864).
Three benzodiazepines offered as 'research chemicals' on the Internet were characterized and their main in vitro phase I metabolites tentatively identified after incubation with pooled human liver microsomes, making a sufficient chromatographic separation inevitable.
Flubromazolam - Basic pharmacokinetic evaluation of a highly potent designer benzodiazepine.
The presented data demonstrate the detectability of a single uptake of 0.5 mg of flubromazolam in hair samples collected two weeks after drug uptake by LC-MS3 (cmax 0.6 pg/mg; LOD 0.01 PG/mg).
Characterization of the four designer benzodiazepines clonazolam, deschloroetizolam, flubromazolam, and meclonazepam, and identification of their in vitro metabolites
The characterization of these four designer benzodiazepines using nuclear magnetic resonance spectroscopy, gas chromatography–electron ionization-mass spectrometry, liquid chromatography-tandem mass spectrometric, liquid Chromatography–quadrupole time-of-flight-massSpectroscopy and infrared spectroscopic is presented.
MALDI-TOF mass spectrometric determination of eight benzodiazepines with two of their metabolites in blood.


Colorimetric detection and chromatographic analyses of designer drugs in biological materials: a comprehensive review
A number of analogues of phenethylamine and tryptamine, which are prepared by modification of the chemical structures, are being developed for circulation on the black market. Often called “designer
In vitro and in vivo glucuronidation of midazolam in humans.
A more complete picture of MDZ metabolism and the enzymes involved has been elucidated, with an increased role for UGT1A4 under CYP3A inhibited conditions.
Recently abused β-keto derivatives of 3,4-methylenedioxyphenylalkylamines: a review of their metabolisms and toxicological analysis
Abstractβ-Keto derivatives of 3,4-methylenedioxyphenylalkylamines (bk-MDPAs), especially 2-methylamino-1-(3,4-methylenedioxyphenyl)propan-1-one (methylone),
Cocktail Approach for In Vivo Phenotyping of 5 Major CYP450 Isoenzymes: Development of an Effective Sampling, Extraction, and Analytical Procedure and Pilot Study With Comparative Genotyping
A phenotyping method for CYP1A2, 2C9,2C19, 2D6, and 3A4 using a cocktail of 100 mg caffeine, 125 mg tolbutamide, 20 mg omeprazole, 30 mg dextromethorphan, and 2 mg midazolam is developed.
Identification of the cannabimimetic AM-1220 and its azepane isomer (N-methylazepan-3-yl)-3-(1-naphthoyl)indole in a research chemical and several herbal mixtures
Recently, a large number of synthetic cannabinoids have been identified in herbal mixtures. Moreover, an even higher number of cannabimimetic compounds are currently distributed as research chemicals
Mass spectral and GC data of drugs, poisons, pesticides, pollutants and their metabolites: Part 3 mass spectra (m/z222 to 777 amu).
Volume 1 (Methods, Tables). Methods. 1 Introduction. 2 Experimental Section. 2.1 Origin and choice of samples. 2.2 Sample preparation. 2.2.1 Standard extraction procedures. Standard
Identification of a cannabinoid analog as a new type of designer drug in a herbal product.
A new type of designer drug, a cannabinoid analog (1), was found in a herbal product distributed on the illegal drug market in Japan in expectation of its narcotic effect. The structure of 1 was
Mass spectral and GC data of drugs, poisons, pesticides, pollutants and their metabolites (Parts 1, 2, 3)
SummaryThese three volumes of gas chromatography (GC) and mass spectral (MS) data are an essential reference work for any professional working in the fields of clinical & forensic toxicology or
Metabolism of 8-chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo [4,3-alpha] [1,4] benzodiazepine, triazolam, a new central depressant. I. Absorption, distribution and excretion in rats, dogs and monkeys.
Radioactivity levels in tissues after daily dosing of triazolam to male rats for 21 days did not differ appreciably from single administration, and radioactivity in the liver, blood and kidneys was very low, and was undetectable in other tissues and organs.
Identification of two new-type synthetic cannabinoids, N-(1-adamantyl)-1-pentyl-1H-indole-3-carboxamide (APICA) and N-(1-adamantyl)-1-pentyl-1H-indazole-3-carboxamide (APINACA), and detection of five synthetic cannabinoids, AM-1220, AM-2233, AM-1241, CB-13 (CRA-13), and AM-1248, as designer drugs in
Two new-type synthetic cannabinoids, N-(1-adamantyl)-1-pentyl-1H-indole-3-carboxamide (APICA, 1) and N-(1-adamantyl)-1-pentyl-1H-indazole-3-carboxamide (APINACA, 2), have been identified as designer