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    Fatal intoxications associated with the designer opioid AH-7921

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    AH-7921 (3,4-dichloro-N-[(1-dimethylamino) cyclohexylmethyl] benzamide) is a designer opioid with similar to 80% of morphines m-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 0.03 to 0.99 mu g/g blood. Six of our cases had other drugs of abuse on board and most had other medications such as benzodiazepines, antidepressants and analgesics. However, the other medicinal drugs encountered were present in postmortem therapeutic concentrations and unlikely to have contributed to death. In addition to the parent compound, we identified six possible metabolites where two N-demethylated dominated and four mono-hydroxylated were found in trace amounts in the blood. In conclusion, deaths with AH-7921 seem to occur both at low and high concentrations, probably a result of different tolerance to the drug. Hence, it is reasonable to assume that no sharp dividing line exists between lethal and non-lethal concentrations. Further, poly-drug use did not seem to be a major contributing factor for the fatal outcome.</p

    Göttinger Nobelpreisträger

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    Characterization of AH-7921, a synthetic designer opioid

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    New psychoactive drugs are substances of new synthesis that have been designed to mimicking the psychotropic effect of traditional illicit drugs. The poor knowledge about these emerging drugs represents a serious problem for public health. Here we evaluated the pharmacological profile, the brain penetration and the motivational properties of the synthetic opioid 3,4-dichloro-N-{[1(dimethylamino)cyclohexyl]methyl}benzamide (AH-7921). At this time, no data are available concerning its pharmacokinetic profile and behavioral effects. To reach these goals independent groups of naïve male Wistar rats were used. The doses of AH-7921 to be tested were selected on the basis of the primary observation Irwin test. Pharmacokinetics of AH-7921 was evaluated by HPLC-MS/MS while rewarding properties of the drug were assessed in an unbiased conditioned place preference (CPP) paradigm. Pharmacokinetics studies found that Cmax was reached 30 min after treatment, either in plasma and brain with a brain-to-plasma ratio of ~20. Plasma and brain levels then declined with a similar t1/2 (~3 hours) whereas one of the metabolites (N-didesmethylated) showed a very slow elimination from brain tissue. CPP data demonstrate that like another opioid (morphine 6 mg/kg i.p.), AH-7921 10 mg/kg i.p., but not 1 and 3 mg/kg, induces preference for the drug-paired compartment. Taken together these data demonstrate that AH-7921 is a potent opioid-like drug eliciting positive motivational properties with highly risk of addiction related to the long lasting t1/2 of its metabolites

    EMCDDA–Europol Joint report on a new psychoactive substance: AH-7921. (3,4-dichloro-N-[[1-(dimethylamino)cyclohexyl]methyl]benzamide).

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    The EMCDDA–Europol Joint Report on new psychoactive substance AH-7921 (3,4-dichloro-N-[[1-(dimethylamino)cyclohexyl]methyl]benzamide), submitted in December 2013 to the Council of the EU, the European Commission and the EMA. After assessing the available evidence, the EMCDDA and Europol concluded that sufficient information had been accumulated to merit the production of a Joint Report on AH-7921 as stipulated by Article 5.1 of the Decision. The following street names have been reported: ‘AH-7921’ and ‘doxylan’

    AH-7921: the list of new psychoactive opioids is expanded

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    Abstract 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 l-opioid receptor agonist that has been found to be several times more potent than codeine and at least as potent as morphine. This novel psychoactive sub-stance has already led to eight non-fatal intoxications an

    Going Beyond Counting First Authors in Author Co-citation Analysis

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    The present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
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