Search results for "pharmacology [Excitatory Amino Acid Antagonists]"
showing 10 items of 421 documents
Predicting the risk of drug–drug interactions in psychiatric hospitals: a retrospective longitudinal pharmacovigilance study
2021
ObjectivesThe aim was to use routine data available at a patient’s admission to the hospital to predict polypharmacy and drug–drug interactions (DDI) and to evaluate the prediction performance with regard to its usefulness to support the efficient management of benefits and risks of drug prescriptions.DesignRetrospective, longitudinal study.SettingWe used data from a large multicentred pharmacovigilance project carried out in eight psychiatric hospitals in Hesse, Germany.ParticipantsInpatient episodes consecutively discharged between 1 October 2017 and 30 September 2018 (year 1) or 1 January 2019 and 31 December 2019 (year 2).Outcome measuresThe proportion of rightly classified hospital epi…
Frontiers of metal-coordinating drug design
2020
INTRODUCTION: The occurrence of metal ions in biomolecules is required to exert vital cellular functions. Metal-containing biomolecules can be modulated by small-molecule inhibitors targeting their metal-moiety. As well, the discovery of cisplatin ushered the rational discovery of metal-containing-drugs. The use of both drug types exploiting metal–ligand interactions is well established to treat distinct pathologies. Therefore, characterizing and leveraging metal-coordinating drugs is a pivotal, yet challenging, part of medicinal chemistry. AREA COVERED: Atomic-level simulations are increasingly employed to overcome the challenges met by traditional drug-discovery approaches and to compleme…
Isolation and characterization of a cDNA encoding rat liver cytosolic epoxide hydrolase and its functional expression in Escherichia coli.
1993
A cDNA of 1992 base pairs encoding the complete rat liver cytosolic epoxide hydrolase has been isolated using a polymerase chain reaction-derived DNA fragment (Arand, M., Knehr, M., Thomas, H., Zeller, H. D., and Oesch, F. (1991) FEBS Lett. 294, 19-22) known to represent the 3'-end of the cytosolic epoxide hydrolase mRNA. Sequence analysis revealed an open reading frame of 1662 nucleotides corresponding to 554 amino acids (M(r) = 62,268). The DNA sequence obtained did not display significant homology to the sequences of microsomal epoxide hydrolase or leukotriene A4 hydrolase or to any other DNA included in the EMBL Data Bank (release 32). On Northern blotting of rat liver RNA, a single mRN…
Xenobiotic metabolizing enzyme activities and viability are well preserved in EDTA-isolated rat liver parenchymal cells after cryopreservation
1995
Rat liver parenchymal cells (PC) were isolated by EDTA perfusion and were purified by a subsequent Percoll centrifugation. The isolated PC had a viability of 95%, as judged by trypan blue exclusion. Freshly isolated PC were cryopreserved with an optimized protocol in a computer-controlled freezer. After thawing, the PC still retained a viability of 89%. The activities of representative xenobiotic metabolizing enzymes were compared between freshly isolated and cryopreserved PC after thawing. The cytochrome P450 content and the cytochrome P450 2C11 isoenzyme activity, determined by hydroxylation of testosterone in intact cells, were not affected by the cryopreservation. The following phase II…
The telltale structures of epoxide hydrolases.
2003
Traditionally, epoxide hydrolases (EH) have been regarded as xenobiotic-metabolizing enzymes implicated in the detoxification of foreign compounds. They are known to play a key role in the control of potentially genotoxic epoxides that arise during metabolism of many lipophilic compounds. Although this is apparently the main function for the mammalian microsomal epoxide hydrolase (mEH), evidence is now accumulating that the mammalian soluble epoxide hydrolase (sEH), despite its proven role in xenobiotic metabolism, also has a central role in the formation and breakdown of physiological signaling molecules. In addition, a certain class of microbial epoxide hydrolases has recently been identi…
Sequestration of biological reactive intermediates by trapping as covalent enzyme-intermediate complex
2001
One important class of biological reactive intermediates arising in the course of human xenobiotic metabolism are arene and alkene oxides. The major safeguard against the potential genotoxic effects of these compounds is the microsomal epoxide hydrolase (mEH). This enzyme has a broad substrate specificity but--on the first sight--seems to be inadequately suited for this protection task due to its low turnover number with most of its substrates. The recent progress in the understanding of the mechanism of enzymatic epoxide hydrolysis has shed new light on this apparent dilemma: Epoxide hydrolases convert their substrates via the intermediate formation of a covalent enzyme-substrate complex, …
Detection of primary DNA damage: applicability to biomonitoring of genotoxic occupational exposure and in clinical therapy
1995
The biological effect of putative genotoxic chemicals in the work place environment was monitored in peripheral mononuclear blood cells of exposed workers. DNA strand breaks, alkali-labile sites of DNA and DNA cross-links were measured using the alkaline filter elution method. A dose dependent increase in DNA damage was found in sterilization workers exposed to ethylene oxide and metal workers with exposure towards N-nitrosodiethanolamine. Two subpopulations with different response to the external exposure were found in nonsmoking sterilization workers. Nurses handling antineo-plastic agents without adequate safety provisions showed a statistically significantly higher rate of DNA strand br…
sj-pdf-1-tab-10.1177_1759720X20975927 – Supplemental material for Glucosamine sulphate: an umbrella review of health outcomes
2020
Supplemental material, sj-pdf-1-tab-10.1177_1759720X20975927 for Glucosamine sulphate: an umbrella review of health outcomes by Nicola Veronese, Jacopo Demurtas, Lee Smith, Jean-Yves Reginster, Olivier Bruyère, Charlotte Beaudart, Germain Honvo and Stefania Maggi in Therapeutic Advances in Musculoskeletal Disease
sj-pdf-1-tab-10.1177_1759720X20975927 – Supplemental material for Glucosamine sulphate: an umbrella review of health outcomes
2020
Supplemental material, sj-pdf-1-tab-10.1177_1759720X20975927 for Glucosamine sulphate: an umbrella review of health outcomes by Nicola Veronese, Jacopo Demurtas, Lee Smith, Jean-Yves Reginster, Olivier Bruyère, Charlotte Beaudart, Germain Honvo and Stefania Maggi in Therapeutic Advances in Musculoskeletal Disease
Opioids_OAC_supplementary_materials_v2 – Supplemental material for Health outcomes and costs in patients with osteoarthritis and chronic pain treated…
2020
Supplemental material, Opioids_OAC_supplementary_materials_v2 for Health outcomes and costs in patients with osteoarthritis and chronic pain treated with opioids in Spain: the OPIOIDS real-world study by Antoni Sicras-Mainar, Carlos Tornero-Tornero, Francisco Vargas-Negrín, Isabel Lizarraga and Javier Rejas-Gutierrez in Therapeutic Advances in Musculoskeletal Disease