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Natascha Nebel, Brigitte Strauch, Simone Maschauer, Roman Lasch, Hannelore Rampp, Stefanie K Fehler, Leonard R Bock, Harald Hübner, Peter Gmeiner, Markus R Heinrich, Olaf Prante
18 F-Labeled building blocks from the type of [18 F]fluorophenylazocarboxylic- tert -butyl esters offer a rapid, mild, and reliable method for the18 F-fluoroarylation of biomolecules. Two series of azocarboxamides were synthesized as potential radioligands for dopamine D3 and the μ-opioid receptor, revealing compounds 3d and 3e with single-digit and sub-nanomolar affinity for the D3 receptor and compound 4c with only micromolar affinity for the μ-opioid receptor, but enhanced selectivity for the μ-subtype in comparison to the lead compound AH-7921...
December 31, 2017: ACS Omega
Kraig E Strayer, Heather M Antonides, Matthew P Juhascik, Raminta Daniulaityte, Ioana E Sizemore
The United States and numerous other countries worldwide are currently experiencing a public health crisis due to the abuse of illicitly manufactured fentanyl (IMF) and its analogues. This manuscript describes the development of a liquid chromatography-tandem mass spectrometry-based method for the multiplex detection of N = 24 IMF analogues and metabolites in whole blood at concentrations as low as 0.1-0.5 ng mL-1. These available IMFs were fentanyl, norfentanyl, furanyl norfentanyl, remifentanil acid, butyryl norfentanyl, remifentanil, acetyl fentanyl, alfentanil, AH-7921, U-47700, acetyl fentanyl 4-methylphenethyl, acrylfentanyl, para-methoxyfentanyl, despropionyl fentanyl (4-ANPP), furanyl fentanyl, despropionyl para-fluorofentanyl, carfentanil, (±)-cis-3-methyl fentanyl, butyryl fentanyl, isobutyryl fentanyl, sufentanil, valeryl fentanyl, para-fluorobutyryl fentanyl, and para-fluoroisobutyryl fentanyl...
January 31, 2018: ACS Omega
Jacopo Lucchetti, Claudio M Marzo, Alice Passoni, Federico Moro, Angelo di Clemente, Renzo Bagnati, Luigi Cervo, Marco Gobbi
3,4-Dichloro-N-benzamide (AH-7921) is a cyclohexyl-methylbenzamide derivative with analgesic activity, whose abuse was associated with several fatal intoxications, included in Schedule I of UN Single Convention on Narcotic Drugs. We validated an HPLC-MS/MS method to investigate its brain disposition and metabolism after single and repeated injections; in parallel, we evaluated its central behavioral effects. After an intraperitoneal injection of 10 mg/kg, the analgesic effect appeared after 5 min and persisted up to 4 h; brain absorption was rapid (tmax 30 min) and large (brain-to-plasma ratio 16), with active concentration >700 ng/g...
January 20, 2018: Neuropharmacology
Jolanta B Zawilska
The abuse of novel psychoactive substances (NPS) has been increasing dramatically worldwide since late 2000s. By the end of 2015, more than 560 NPS had been reported to the European Monitoring Centre for Drugs and Drug Addiction. Although the most popular compounds are synthetic cannabinoids and psychostimulatory derivatives of cathinone (so-called β-keto-amphetamines), novel synthetic opioids have recently emerged on the recreational drug market. They include fentanyl (a potent narcotic analgesic) and its analogs (e...
2017: Frontiers in Psychiatry
Ludovic Ventura, Félix Carvalho, Ricardo Jorge Dinis-Oliveira
New psychoactive substances (NPS), often referred to as "legal highs" or "designer drugs", are derivatives and analogues of existing psychoactive drugs that are introduced in the recreational market to circumvent existing legislation on drugs of abuse. Due to inefficient monitoring techniques, as well as limited knowledge concerning long-time effects of NPS, further studies regarding such compounds are constantly required. This systematic review aims to gather the state of the art regarding chemical, molecular pharmacology and toxicological information of opioid class of NPS...
July 4, 2017: Current Molecular Pharmacology
Waqas Rafique, Shivashankar Khanapur, Mona M Spilhaug, Patrick J Riss
Imaging of the mu opioid receptor (MOR) availability with positron emission tomography (PET) is a pertinent challenge in Neuroscience. Both, regulation of receptor expression and occupancy by endogeneous opioids play into cognitive and behavioral phenotypes of healthy function and disease. Receptor expression in the active and inactive states can be measured using high affinity radioagonist and radioantagonist PET tracers, respectively. Occupancy assessment requires radioligands showing competitive and reversible binding with moderate affinity to the MOR, which may lead to physical extinction of the receptor specific signal in vivo...
June 27, 2017: ACS Chemical Neuroscience
Helena Fels, Julia Krueger, Hans Sachs, Frank Musshoff, Matthias Graw, Gabriele Roider, Andreas Stoever
In this study, two fatalities associated with the synthetic opioids AH-7921 and MT-45 are reported. Within the last few years, both compounds have emerged on the recreational drug market and are sold as "research chemicals" on the internet. In the first case, a 22-year-old woman was found dead in the bedroom of her apartment by two of her friends. A plastic bag labeled "AH-7921" was found in the apartment and the two friends stated that the deceased had consumed AH-7921 prior to her death. The woman was a known drug addict...
August 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
Steven W Fleming, Justin C Cooley, Leonard Johnson, C Clinton Frazee, Kristina Domanski, Kurt Kleinschmidt, Uttam Garg
The illicit drug market has rapidly evolved from synthetic cannabinoids to cathinone derivatives and now a new emerging threat of synthetic opioids. These compounds were mostly developed by pharmaceutical companies during drug discovery. The new psychoactive substances are not routinely covered in drug screening and may go undetected. Recently fentanyl analogous, AH-7921, MT-45 and now U-47700 have been encountered in clinical and forensic casework. U-47700 is gaining popularity on drug user forms as a legal alternative to heroin...
April 1, 2017: Journal of Analytical Toxicology
A Bernius, V Blaas, D Rentsch, A Büttner, J Thome
We describe the case of a young male patient who had consumed the morphine-like substance AH-7921 which is available via the internet. He was initially admitted to hospital because of obstipation and presented within a day of inpatient treatment for the first time with a generalized tonic-clonic epileptic seizure with subsequent urinary retention. Within a few hours, the patient then also developed bradycardia, while at the same time describing symptoms of physical opioid withdrawal which gradually deteriorated within the following hours...
October 2016: Fortschritte der Neurologie-Psychiatrie
Amanda L A Mohr, Melissa Friscia, Donna Papsun, Sherri L Kacinko, David Buzby, Barry K Logan
Following series of synthetic cannabinoid and synthetic cathinone derivatives, the illicit drug market has begun to see increased incidence of synthetic opioids including fentanyl and its derivatives, and other chemically unrelated opioid agonists including AH-7921 and MT-45. Among the most frequently encountered compounds in postmortem casework have been furanyl fentanyl (N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylfuran-2-carboxamide, Fu-F) and U-47700 (trans-3,4-dichloro-N-(2-(dimethylamino)cyclohexyl)-N-methylbenzamide)...
November 2016: Journal of Analytical Toxicology
Aaron Schneir, Imir G Metushi, Christian Sloane, David J Benaron, Robert L Fitzgerald
BACKGROUND: In the last decade there has been a worldwide surge in the recreational abuse of novel psychoactive substances, particularly amphetamine derivatives and synthetic cannabinoids. Synthetic opioids such as AH-7921, MT-45, and U-47700, with structures distinct from those ever used therapeutically or described recreationally, have also recently emerged. CASE DETAILS: We report a patient who suffered respiratory failure and depressed level of consciousness after recreationally using a novel synthetic opioid labeled U-47700...
January 2017: Clinical Toxicology
(no author information available yet)
With the issuance of this final order, the Administrator of the Drug Enforcement Administration places the substance AH-7921 (Systematic IUPAC Name: 3,4-dichloro-N-[(1dimethylamino)cyclohexylmethyl]benzamide), including its isomers, esters, ethers, salts, and salts of isomers, esters and ethers, into schedule I of the Controlled Substances Act. This scheduling action is pursuant to the Controlled Substances Act and is required in order for the United States to discharge its obligations under the Single Convention on Narcotic Drugs, 1961...
April 14, 2016: Federal Register
Ariane Wohlfarth, Karl B Scheidweiler, Shaokun Pang, Mingshe Zhu, Marisol Castaneto, Robert Kronstrand, Marilyn A Huestis
AH-7921 (3,4-dichloro-N-[(1-dimethylamino)cyclohexylmethyl]benzamide) is a new synthetic opioid and has led to multiple non-fatal and fatal intoxications. To comprehensively study AH-7921 metabolism, we assessed human liver microsome (HLM) metabolic stability, determined AH-7921's metabolic profile after human hepatocytes incubation, confirmed our findings in a urine case specimen, and compared results to in silico predictions. For metabolic stability, 1 µmol/L AH-7921 was incubated with HLM for up to 1 h; for metabolite profiling, 10 µmol/L was incubated with pooled human hepatocytes for up to 3 h...
August 2016: Drug Testing and Analysis
Maria Katselou, Ioannis Papoutsis, Panagiota Nikolaou, Chara Spiliopoulou, Sotiris Athanaselis
AH-7921 is a structurally unique synthetic opioid analgesic that has recently entered the drug arena in Europe, the USA, and Japan. Although it was synthesized and patented in the mid-1970s, it was first identified in a seized sample purchased via the Internet in July 2012 and formally brought to the attention of the European Union early warning system in August 2012 by the United Kingdom. Several in vitro experiments and animal model studies established the morphine-like analgesic action of AH-7921 as a μ-opioid receptor agonist that has been found to be several times more potent than codeine and at least as potent as morphine...
2015: Forensic Toxicology
Anders Ledberg
BACKGROUND: In recent years the recreational use of new psychoactive substances (NPS) has increased. NPS are considered a threat to public health and the main response to this threat is to make the selling and buying of these substances illegal. In Sweden, during the last 5 years, 62 new substances have been classified as narcotics but little is known of the effects of making a particular substance illegal. The aim of this work is to study how legal status influences the interest in NPS in Sweden...
July 1, 2015: Drug and Alcohol Dependence
R Kronstrand, G Thelander, D Lindstedt, M Roman, F C Kugelberg
AH-7921 (3,4-dichloro-N-[(1-dimethylamino)cyclohexylmethyl]benzamide) is a designer opioid with ∼80% of morphine's µ-agonist activity. Over a 6-month period, we encountered nine deaths where AH-7921 was involved and detected in blood from the deceased. Shortly after the last death, on August 1 2013, AH-7921 was scheduled as a narcotic and largely disappeared from the illicit market in Sweden. AH-7921 was measured by a selective liquid chromatography-MS-MS method and the concentrations of AH-7921 ranged from 0...
October 2014: Journal of Analytical Toxicology
Ritva Karinen, Silja Skogstad Tuv, Sidsel Rogde, Mariana Dadalto Peres, Unni Johansen, Joachim Frost, Vigdis Vindenes, Åse Marit Leere Øiestad
AH-7921 is a synthetic μ-opioid agonist, approximately equipotent with morphine. We report the death of two young individuals after ingestion of AH-7921 in combination with other psychoactive drugs. In the first case a young man died shortly after ingesting Internet drugs. Toxicological analysis of post mortem peripheral blood revealed AH-7921 (0.43 mg/L), 2-FMA (0.0069 mg/L) and 3-MMC (0.0021 mg/L) as well as codeine (0.42 mg/L), codeine-6-glucuronide (0.77 mg/L) and acetaminophen (18.7 mg/L). The second case involved a young female found dead at home...
November 2014: Forensic Science International
Ruri Kikura-Hanajiri, Nahoko Uchiyama Maiko Kawamura, Yukihiro Goda
To counter the spread of the many analogues of psychoactive substances, the Pharmaceutical Affairs Law in Japan was amended in 2006 to establish a new category - Designated Substances - in order to more promptly control these drugs. As of March 2013, 106 substances (including one plant, Salvia divinorum) were listed in the category of Designated Substances, and 13 of them had had their category changed from Designated Substances into the much stricter category, Narcotics. However, new analogues of controlled substances, especially synthetic cannabinoids, appeared one-by-one since the new category was introduced...
July 2014: Drug Testing and Analysis
Yan Ni Annie Soh, Simon Elliott
The evolving nature of new psychoactive substances (NPS) - often referred to as 'legal highs', 'designer drugs' or 'bath salts' - presents an evolving challenge for toxicologists. Apart from the detection and identification of these compounds, further analytical challenges may arise from the presence of possible metabolites or degradation products which may have to be considered when devising an analytical strategy. Whilst there has been some stability research for some more established drugs of abuse and medicinal products, data on emerging NPS are less abundant...
July 2014: Drug Testing and Analysis
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