scholarly journals Erratum to: Toxicological profiles of selected synthetic cannabinoids showing high binding affinities to the cannabinoid receptor subtype CB1

2013 ◽  
Vol 87 (7) ◽  
pp. 1299-1299
Author(s):  
Verena J. Koller ◽  
Gerhard J. Zlabinger ◽  
Volker Auwärter ◽  
Sabine Fuchs ◽  
Siegfried Knasmueller
Keyword(s):  
Cannabinoid Receptor ◽  
Synthetic Cannabinoids ◽  
Receptor Subtype ◽  
Binding Affinities ◽  
High Binding

Toxicological profiles of selected synthetic cannabinoids showing high binding affinities to the cannabinoid receptor subtype CB1

2013 ◽  
Vol 87 (7) ◽  
pp. 1287-1297 ◽  
Author(s):  
Verena J. Koller ◽  
Gerhard J. Zlabinger ◽  
Volker Auwärter ◽  
Sabine Fuchs ◽  
Siegfried Knasmueller
Keyword(s):  
Cannabinoid Receptor ◽  
Synthetic Cannabinoids ◽  
Receptor Subtype ◽  
Binding Affinities ◽  
High Binding

scholarly journals Identification and Analytical Characterization of a Novel Synthetic Cannabinoid-Type Substance in Herbal Material in Europe

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 793
Author(s):  
Emmanouil D. Tsochatzis ◽  
Joao Alberto Lopes ◽  
Margaret V. Holland ◽  
Fabiano Reniero ◽  
Giovanni Palmieri ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Cannabinoid Receptor ◽  
Analytical Data ◽  
Synthetic Cannabinoids ◽  
Synthetic Cannabinoid ◽  
Gas Chromatography Mass Spectrometry ◽  
New Psychoactive Substances ◽  
Synthetic Cannabinoid Receptor Agonists ◽  
Analytical Laboratories

The rapid diffusion of new psychoactive substances (NPS) presents unprecedented challenges to both customs authorities and analytical laboratories involved in their detection and characterization. In this study an analytical approach to the identification and structural elucidation of a novel synthetic cannabimimetic, quinolin-8-yl-3-[(4,4-difluoropiperidin-1-yl) sulfonyl]-4-methylbenzoate (2F-QMPSB), detected in seized herbal material, is detailed. An acid precursor 4-methyl-3-(4,4-difluoro-1-piperidinylsulfonyl) benzoic acid (2F-MPSBA), has also been identified in the same seized material. After extraction from the herbal material the synthetic cannabimimetic, also referred to as synthetic cannabinoid receptor agonists or “synthetic cannabinoids”, was characterized using gas chromatography-mass spectrometry (GC-MS), 1H, 13C, 19F and 15N nuclear magnetic resonance (NMR) and high-resolution tandem mass spectrometry (HR-MS/MS) combined with chromatographic separation. A cheminformatics platform was used to manage and interpret the analytical data from these techniques.

Rotenoids and Other Specialized Metabolites from the Roots of Mirabilis multiflora: Opioid and Cannabinoid Receptor Radioligand Binding Affinities

2021 ◽  
Vol 84 (4) ◽  
pp. 1392-1396
Author(s):  
Vimal K. Sharma ◽  
Radhakrishnan Srivedavyasasri ◽  
Zulfiqar Ali ◽  
Jordan K. Zjawiony ◽  
Samir A. Ross ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Radioligand Binding ◽  
Binding Affinities ◽  
Specialized Metabolites

A Reference Scale of Cucurbit[7]uril Binding Affinities

2021 ◽  
Author(s):  
Mohammad A. Alnajjar ◽  
Werner M Nau ◽  
Andreas Hennig
Keyword(s):  
Accurate Determination ◽  
Binding Affinities ◽  
High Binding ◽  
Reference Scale ◽  
Direct Binding ◽  
Guest Chemistry

The accurate determination of ultra-high binding affinities in supramolecular host-guest chemistry is a challenging endeavour because direct binding titrations are generally limited to affinities <106 M-1 due to sensitivity constraints...

scholarly journals Can Physical Activity Support the Endocannabinoid System in the Preventive and Therapeutic Approach to Neurological Disorders?

2020 ◽  
Vol 21 (12) ◽  
pp. 4221
Author(s):  
Tomasz Charytoniuk ◽  
Hubert Zywno ◽  
Karolina Konstantynowicz-Nowicka ◽  
Klaudia Berk ◽  
Wiktor Bzdega ◽  
...  
Keyword(s):  
Physical Activity ◽  
Neurodegenerative Disorders ◽  
Therapeutic Approach ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoids ◽  
Endocannabinoid System ◽  
Antidepressant Effect ◽  
Brain Physiology ◽  
Current State ◽  
Neurological Effects

The worldwide prevalence of neurological and neurodegenerative disorders, such as depression or Alzheimer’s disease, has spread extensively throughout the last decades, becoming an enormous health issue. Numerous data indicate a distinct correlation between the altered endocannabinoid signaling and different aspects of brain physiology, such as memory or neurogenesis. Moreover, the endocannabinoid system is widely regarded as a crucial factor in the development of neuropathologies. Thus, targeting those disorders via synthetic cannabinoids, as well as phytocannabinoids, becomes a widespread research issue. Over the last decade, the endocannabinoid system has been extensively studied for its correlation with physical activity. Recent data showed that physical activity correlates with elevated endocannabinoid serum concentrations and increased cannabinoid receptor type 1 (CB1R) expression in the brain, which results in positive neurological effects including antidepressant effect, ameliorated memory, neuroplasticity development, and reduced neuroinflammation. However, none of the prior reviews presented a comprehensive correlation between physical activity, the endocannabinoid system, and neuropathologies. Thus, our review provides a current state of knowledge of the endocannabinoid system, its action in physical activity, as well as neuropathologies and a possible correlation between all those fields. We believe that this might contribute to finding a new preventive and therapeutic approach to both neurological and neurodegenerative disorders.

scholarly journals Human Hepatocyte Metabolism of Novel Synthetic Cannabinoids MN-18 and Its 5-Fluoro Analog 5F-MN-18

2017 ◽  
Vol 63 (11) ◽  
pp. 1753-1763 ◽  
Author(s):  
Xingxing Diao ◽  
Jeremy Carlier ◽  
Mingshe Zhu ◽  
Marilyn A Huestis
Keyword(s):  
Carboxylic Acid ◽  
High Resolution ◽  
High Resolution Mass Spectrometry ◽  
Synthetic Cannabinoids ◽  
Human Hepatocytes ◽  
Binding Affinities ◽  
High Resolution Mass ◽  
Full Scan ◽  
Resolution Mass

Abstract BACKGROUND In 2014, 2 novel synthetic cannabinoids, MN-18 and its 5-fluoro analog, 5F-MN-18, were first identified in an ongoing survey of novel psychoactive substances in Japan. In vitro pharmacological assays revealed that MN-18 and 5F-MN-18 displayed high binding affinities to human CB1 and CB2 receptors, with Ki being 1.65–3.86 nmol/L. MN-18 and 5F-MN-18 were scheduled in Japan and some other countries in 2014. Despite increasing prevalence, no human metabolism data are currently available, making it challenging for forensic laboratories to confirm intake of MN-18 or 5F-MN-18. METHODS We incubated 10 μmol/L of MN-18 and 5F-MN-18 in human hepatocytes for 3 h and analyzed the samples on a TripleTOF 5600+ high-resolution mass spectrometer to identify appropriate marker metabolites. Data were acquired via full scan and information-dependent acquisition-triggered product ion scans with mass defect filter. RESULTS In total, 13 MN-18 metabolites were detected, with the top 3 abundant metabolites being 1-pentyl-1H-indazole-3-carboxylic acid, pentyl-carbonylated MN-18, and naphthalene-hydroxylated MN-18. For 5F-MN-18, 20 metabolites were observed, with the top 3 abundant metabolites being 5′-OH-MN-18, MN-18 pentanoic acid, and 1-(5-fluoropentyl)-1H-indazole-3-carboxylic acid. CONCLUSIONS We have characterized MN-18 and 5F-MN-18 metabolism with human hepatocytes and high-resolution mass spectrometry, and we recommend characteristic major metabolites for clinical and forensic laboratories to identify MN-18 and 5F-MN-18 intake and link observed adverse events to these novel synthetic cannabinoids.

scholarly journals Activity-Based Detection of Cannabinoids in Serum and Plasma Samples

2018 ◽  
Vol 64 (6) ◽  
pp. 918-926 ◽  
Author(s):  
Annelies Cannaert ◽  
Jolien Storme ◽  
Cornelius Hess ◽  
Volker Auwärter ◽  
Sarah M R Wille ◽  
...  
Keyword(s):  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoids ◽  
Receptor Activation ◽  
Synthetic Cannabinoid ◽  
New Psychoactive Substances ◽  
Simple Liquid ◽  
Analytical Sensitivity ◽  
Monitoring Centre ◽  
Screening Strategies

Abstract BACKGROUND Synthetic cannabinoids are the largest group of new psychoactive substances monitored by the European Monitoring Centre of Drugs and Drug Addiction. The rapid proliferation of novel analogs makes the detection of these new derivatives challenging and has initiated considerable interest in the development of so-called “untargeted” screening strategies to detect these compounds. METHODS We developed new, stable bioassays in which cannabinoid receptor activation by cannabinoids led to recruitment of truncated β-arrestin 2 (βarr2) to the cannabinoid receptors, resulting in functional complementation of a split luciferase, allowing readout via bioluminescence. Aliquots (500 μL) of authentic serum (n = 45) and plasma (n = 73) samples were used for simple liquid–liquid extraction with hexane:ethyl acetate (99:1 v/v). Following evaporation and reconstitution in 100 μL of Opti-MEM® I/methanol (50/50 v/v), 10 μL of these extracts was analyzed in the bioassays. RESULTS Truncation of βarr2 significantly (for both cannabinoid receptors; P = 0.0034 and 0.0427) improved the analytical sensitivity over the previously published bioassays applied on urine samples. The new bioassays detected cannabinoid receptor activation by authentic serum or plasma extracts, in which synthetic cannabinoids were present at low- or sub-nanogram per milliliter concentration or in which Δ9-tetrahydrocannabinol was present at concentrations &gt;12 ng/mL. For synthetic cannabinoid detection, analytical sensitivity was 82%, with an analytical specificity of 100%. CONCLUSIONS The bioassays have the potential to serve as a first-line screening tool for (synthetic) cannabinoid activity in serum or plasma and may complement conventional analytical assays and/or precede analytical (mass spectrometry based) confirmation.

scholarly journals Library of Sequence-specific Radioimmunoassays for Human Chromogranin A

1999 ◽  
Vol 45 (4) ◽  
pp. 549-560 ◽  
Author(s):  
Tine Børglum Jensen ◽  
Linda Hilsted ◽  
Jens F Rehfeld
Keyword(s):  
Carcinoid Tumor ◽  
Neuroendocrine Tumors ◽  
Chromogranin A ◽  
Acidic Protein ◽  
Binding Affinities ◽  
Cleavage Sites ◽  
Tumor Patients ◽  
High Binding ◽  
Low Concentrations ◽  
Different Tissues

Abstract Background: Human chromogranin A (CgA) is an acidic protein widely expressed in neuroendocrine tissue and tumors. The extensive tissue- and tumor-specific cleavages of CgA at basic cleavage sites produce multiple peptides. Methods: We have developed a library of RIAs specific for different epitopes, including the NH2 and COOH termini and three sequences adjacent to dibasic sites in the remaining part of CgA. Results: The antisera raised against CgA(210–222) and CgA(340–348) required a free NH2 terminus for binding. All antisera displayed high titers, high indexes of heterogeneity (∼1.0), and high binding affinities (Keff0 ∼ 0.1 × 1012 to 1.0 × 1012 L/mol), implying that the RIAs were monospecific and sensitive. The concentration of CgA in different tissues varied with the assay used. Hence, in a carcinoid tumor the concentration varied from 0.5 to 34.0 nmol/g tissue depending on the specificity of the CgA assay. The lowest concentration in all tumors was measured with the assay specific for the NH2 terminus of CgA. This is consistent with the relatively low concentrations measured in plasma from carcinoid tumor patients by the N-terminal assay, whereas the assays using antisera raised against CgA(210–222) and CgA(340–348) measured increased concentrations. Conclusion: Only some CgA assays appear useful for diagnosis of neuroendocrine tumors, but the entire library is valuable for studies of the expression and processing of human CgA.

scholarly journals Difference and Influence of Inactive and Active States of Cannabinoid Receptor Subtype CB2: From Conformation to Drug Discovery

2016 ◽  
Vol 56 (6) ◽  
pp. 1152-1163 ◽  
Author(s):  
Jianping Hu ◽  
Zhiwei Feng ◽  
Shifan Ma ◽  
Yu Zhang ◽  
Qin Tong ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Cannabinoid Receptor ◽  
Receptor Subtype
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