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https://www.readbyqxmd.com/read/28079248/inhibition-of-matrix-metalloproteinase-9-by-a-barbiturate-nitrate-hybrid-ameliorates-dextran-sulphate-sodium-induced-colitis-effect-on-inflammation-related-genes
#1
Shane O'Sullivan, Jun Wang, Maria T Pigott, Neil Docherty, Noreen Boyle, Samuel Kana Lis, John F Gilmer, Carlos Medina
BACKGROUND AND PURPOSE: Matrix metalloproteinase-9 is upregulated in Ulcerative Colitis and implicated in the pathology of the disease. In this study, we have examined the effects of a barbiturate-based MMP inhibitor incorporating a nitric oxide donor/mimetic group (dinitrate-barbiturate) in the intestinal injury induced by dextran sulphate sodium (DSS). EXPERIMENTAL APPROACH: In-vivo experiments were carried out using male Wistar rats given DSS 5% ad libitum in drinking water...
January 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28029372/cajal-s-unbearable-cephalalgias-the-consequences-of-a-misdiagnosis
#2
REVIEW
S Giménez-Roldán
Around the age of 66 Cajal consulted neurologist Nicolas Achúcarro complaining of "unbearable cephalalgias". He had not ever suffered from headaches. The diagnosis of early arteriosclerosis that was considered at the time a physiological, irreversible ailment of ageing had a strong emotional impact on Cajal. Comorbid depression, insomnia and self-treatment with escalating doses of Veronal(®) (barbital), a short-acting barbiturate, presumably aggravated the situation. Exposure to warm environments and being involved in tense discussions were identified as triggering factors of the headaches...
October 28, 2016: Revue Neurologique
https://www.readbyqxmd.com/read/28007369/pentobarbital-in-the-context-of-possible-suicides-analysis-of-a-case
#3
Paula Melo, Pedro Costa, Maria José Quintas, André Castro, Sónia Tarelho, João Miguel Franco, Helena M Teixeira
Pentobarbital is a barbiturate, acting as a central nervous system depressant (CNS), being used for its anticonvulsant, sedative, hypnotic and anaesthetic properties. Barbiturates were replaced by benzodiazepines, leading to a decrease in poisoning cases with these compounds. However, pentobarbital is still used in many countries as an anaesthetic in veterinary medicine. Due to its properties, this compound is sought after by people who wish to commit suicide, acquiring it on the black market. The authors present an unusual fatal pentobarbital intoxication case, in a 37 years-old male salesperson, with no known connection with the veterinary field, being more difficult to obtain this compound...
December 8, 2016: Forensic Science International
https://www.readbyqxmd.com/read/27995785/dearomatizing-radical-cyclizations-and-cyclization-cascades-triggered-by-electron-transfer-reduction-of-amide-type-carbonyls
#4
Huan-Ming Huang, David J Procter
Highly selective dearomatizing radical cyclizations and cyclization cascades, triggered by single electron-transfer to amide-type carbonyls by SmI2-H2O-LiBr provide efficient access to unprecedented spirocyclic scaffolds containing five stereocenters with high diastereocontrol. The first dearomatizing radical cyclizations involving radicals derived from the amide carbonyls by single electron-transfer take place under mild conditions and engage a range of aromatic and heteroaromatic systems present in the barbiturate substrates...
December 20, 2016: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/27992389/contrasting-effects-of-the-%C3%AE-aminobutyric-acid-type-a-receptor-%C3%AE-3-subunit-n265m-mutation-on-loss-of-righting-reflexes-induced-by-etomidate-and-the-novel-anesthetic-barbiturate-r-mtfd-mpab-erratum
#5
https://www.readbyqxmd.com/read/27986812/barbiturates-bind-in-the-glic-ion-channel-pore-and-cause-inhibition-by-stabilizing-a-closed-state
#6
Zaineb Fourati, Reinis Reinholds Ruza, Duncan Laverty, Emmanuelle Drège, Sandrine Delarue-Cochin, Delphine Joseph, Patrice Koehl, Trevor Smart, Marc Delarue
Barbiturates induce anesthesia by modulating the activity of anionic and cationic pentameric ligand-gated ion channels (pLGICs). Despite more than a century of use in clinical practice, the prototypic binding site for this class of drugs within pLGICs is yet to be described. In this study, we present the first X-ray structures of barbiturates bound to GLIC, a cationic prokaryotic pLGIC with excellent structural homology to other relevant channels sensitive to general anesthetics and, as shown here, to barbiturates, at clinically-relevant concentrations...
December 16, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27979642/severe-carisoprodol-withdrawal-after-a-14-year-addiction-and-acute-overdose
#7
Kathy T Vo, Howard Horng, Craig G Smollin, Neal L Benowitz
BACKGROUND: Carisoprodol, a centrally acting muscle relaxant with a high abuse potential, has barbiturate-like properties at the GABA-A receptor, leading to central nervous system depression and desired effects. Its tolerance and dependence has been previously demonstrated in an animal model, and withdrawal has been described in several recent case reports. Many cases can be effectively managed with a short course of benzodiazepines or antipsychotic agents. However, abrupt cessation in a patient with a history of long-term and high-dose carisoprodol abuse may result in symptoms that are more difficult for providers to treat...
December 12, 2016: Journal of Emergency Medicine
https://www.readbyqxmd.com/read/27974971/the-psychological-wellbeing-of-iranian-journalists-a-descriptive-study
#8
Anthony Feinstein, Saul Feinstein, Maziar Behari, Bennis Pavisian
OBJECTIVE: Iran ranks 173 out of 180 countries on an index of press freedom. The purpose of the study was to assess the psychological wellbeing of Iranian journalists and document the stressors encountered in their work. DESIGN: A secure website was established and participants were given their unique identifying number and password to access the site. SETTING: Newsrooms in Iran and the diaspora. PARTICIPANTS: Responses were received from 114 journalists (76%) of whom 65...
December 2016: JRSM Open
https://www.readbyqxmd.com/read/27935723/remote-photoregulated-ring-gliding-in-a-2-rotaxane-via-a-molecular-effector
#9
Arnaud Tron, Isabelle Pianet, Alberto Martinez-Cuezva, James H R Tucker, Luca Pisciottani, Mateo Alajarin, Jose Berna, Nathan D McClenaghan
A molecular barbiturate messenger, which is reversibly released/captured by a photoswitchable artificial molecular receptor, is shown to act as an effector to control ring gliding on a distant hydrogen-bonding [2]rotaxane. Thus, light-driven chemical communication governing the operation of a remote molecular machine is demonstrated using an information-rich neutral molecule.
December 9, 2016: Organic Letters
https://www.readbyqxmd.com/read/27922194/pharmacodynamic-response-profiles-of-anxiolytic-and-sedative-drugs
#10
Xia Chen, Freerk Broeyer, Marieke de Kam, Joke Baas, Adam Cohen, Joop van Gerven
INTRODUCTION: Centrally-acting acutely anxiolytic drugs, like benzodiazepines, barbiturates and gabapentinoids, affect various central nervous system (CNS) functions, which reflect not only their anxiolytic effects but also neuropsychological side-effects. To validate the pharmacodynamic biomarkers for GABA-ergic anxiolytics, this study determined the pharmacodynamics of two anxiolytics and a non-anxiolytic control and linked them to their anxiolytic and sedative effects, during an anxiety-challenge study day...
December 6, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27866392/drug-caused-deaths-in-australian-medical-practitioners-and-health-care-professionals
#11
Jennifer L Pilgrim, Rhyse Dorward, Olaf H Drummer
BACKGROUND AND AIMS: There are numerous factors putting health-care professionals (HCP) at a higher risk of substance abuse and premature death, including high-stress jobs, access to controlled substances, long hours of practice and constant contact with the critically ill. This study aimed to examine fatal drug toxicity in this high-risk cohort, in order to: (1) estimate the rate of drug-caused deaths of Australian HCPs; (2) describe the key characteristics of the cohort; and (3) examine the relationship between HCP occupation and drug type, or intent...
November 20, 2016: Addiction
https://www.readbyqxmd.com/read/27861834/an-algorithm-for-opioid-and-barbiturate-reduction-in-the-acute-management-of-headache-in-the-emergency-department
#12
Zubair A Ahmed, Dimitrios A Nacopoulos, Seby John, Nancy Papesh, David Levine, Cynthia C Bamford
OBJECTIVE: To develop and implement an algorithm for the management of headaches presenting to the emergency department (ED) in order to decrease the frequency of opioid and barbiturate treatment both acutely as well as on discharge. BACKGROUND: Headache is the fifth leading cause of ED visits in the United States. In the case of primary headache, particularly migraine, treatment in the ED can be highly variable. Patients with migraine continue to be treated with opioids more commonly than nonopioid, migraine specific medications...
January 2017: Headache
https://www.readbyqxmd.com/read/27857927/a-fatal-adverse-effect-of-barbiturate-coma-therapy-dyskalemia
#13
Hyun Mook Kwon, Jin Wook Baek, Sang Pyung Lee, Jae Ik Cho
The management guideline for traumatic brain injury (TBI) recommends high-dose barbiturate therapy to control increased intracranial pressure refractory to other therapeutic options. High-dose barbiturate therapy, however, may cause many severe side effects; the commonly recognized ones include hypotension, immunosuppression, hepatic dysfunction, renal dysfunction, and prolonged decrease of cortical activity. Meanwhile, dyskalemia remains relatively uncommon. In this study, we report the case of a hypokalemic patient with severe rebound hyperkalemia, which occurred as a result of barbiturate coma therapy administered for TBI treatment...
October 2016: Korean Journal of Neurotrauma
https://www.readbyqxmd.com/read/27853314/imprinting-of-cerebral-cytochrome-p450s-in-offsprings-prenatally-exposed-to-cypermethrin-augments-toxicity-on-rechallenge
#14
Anshuman Singh, Anita Agrahari, RadhaDutt Singh, Sanjay Yadav, Vikas Srivastava, Devendra Parmar
Epigenetic studies were carried in the rat offsprings, born to dams treated with cypermethrin (orally; 5.0 mg/kg) from gestation day (GD) 5 to 21 and rechallenged with cypermethrin (orally; 10 mg/kg for 6 days), at adulthood (12 weeks) to understand the mechanism underlying the overexpression of cerebral cytochrome P450s (CYPs) in exposed offsprings. The data revealed alterations in histone H3 acetylation and DNA methylation in promoter regions of CYP1A- and 2B- isoenzymes in the brain isolated from rechallenged animals...
November 17, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27853105/clinical-characteristics-of-patients-who-overdose-on-multiple-psychotropic-drugs-in-tokyo
#15
Satoshi Hori, Kosaku Kinoshita
OBJECTIVE: The purpose of this study was to identify the clinical aspects leading to overdose of multiple psychotropic drugs, in order to determine areas which need attention in the proper treatment of overdose patients. METHODS: Patients who were treated for overdose of psychotropic drugs at our emergency and critical center over two years were targeted. The clinical data was gathered from the medical records and database of all patients, including age, gender, vital signs, and laboratory data, drugs, and medical complications during hospital stay...
2016: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/27848906/-attempted-suicide-with-barbiturates-purchased-online
#16
S F Chavoushi, L Mesman, P G Noordzij, M A Sikma, E M van Maarseveen
BACKGROUND: Barbiturate intoxication is potentially lethal. With the availability of the newer anticonvulsants the use of barbiturates in treating epilepsy has decreased significantly, with a concurrent decrease in the incidence of overdose with these medications. There have, however, been recent alarm signals from governmental sources concerning the increase in the Internet purchase of illegal medications, including barbiturates, for use in attempted suicide. CASE DESCRIPTION: Here we describe two patient cases involving barbiturate intoxication with amobarbital and thiopental, respectively...
2016: Nederlands Tijdschrift Voor Geneeskunde
https://www.readbyqxmd.com/read/27834137/in-vivo-piroxicam-metabolites-possible-source-for-synthesis-of-central-nervous-system-cns-acting-depressants
#17
Saganuwan Alhaji Saganuwan
Piroxicam has been reported to be convertible to central nervous system (CNS) acting agents. It has serious depressant effects at high doses. In view of this structures of piroxicam metabolites were assessed for possible conversion to CNS depressants. Structural barbituric compounds, carboxamide, cyclohydrated, benzothiazone and carboxybenzothiazone metabolites which may act via dopamine and adrenergic receptors causing depression of CNS activities.
November 10, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27821594/general-anesthetic-binding-sites-in-human-%C3%AE-4%C3%AE-3%C3%AE-%C3%AE-aminobutyric-acid-type-a-receptors-gabaars
#18
David C Chiara, Youssef Jounaidi, Xiaojuan Zhou, Pavel Y Savechenkov, Karol S Bruzik, Keith W Miller, Jonathan B Cohen
Extrasynaptic γ-aminobutyric acid type A receptors (GABAARs),which contribute generalized inhibitory tone to the mammalian brain, are major targets for general anesthetics. To identify anesthetic binding sites in an extrasynaptic GABAAR, we photolabeled human α4β3δ GABAARs purified in detergent with [(3)H]azietomidate and a barbiturate, [(3)H]R-mTFD-MPAB, photoreactive anesthetics that bind with high selectivity to distinct but homologous intersubunit binding sites in the transmembrane domain of synaptic α1β3γ2 GABAARs...
December 16, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27805767/synthesis-and-antiangiogenic-properties-of-tetrafluorophthalimido-and-tetrafluorobenzamido-barbituric-acids
#19
Agnieszka Ambrożak, Christian Steinebach, Erin R Gardner, Shaunna L Beedie, Gregor Schnakenburg, William D Figg, Michael Gütschow
The development of novel thalidomide derivatives as immunomodulatory and anti-angiogenic agents has revived over the last two decades. Herein we report the design and synthesis of three chemotypes of barbituric acids derived from the thalidomide structure: phthalimido-, tetrafluorophthalimido-, and tetrafluorobenzamidobarbituric acids. The latter were obtained by a new tandem reaction, including a ring opening and a decarboxylation of the fluorine-activated phthalamic acid intermediates. Thirty compounds of the three chemotypes were evaluated for their anti-angiogenic properties in an ex vivo assay by measuring the decrease in microvessel outgrowth in rat aortic ring explants...
December 6, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27796461/the-use-of-a-temperature-responsive-column-for-the-direct-analysis-of-drugs-in-serum-by-two-dimensional-heart-cutting-liquid-chromatography
#20
Toshiyasu Mikuma, Ryo Uchida, Mizuki Kajiya, Yuki Hiruta, Hideko Kanazawa
A novel pretreatment method, which was performed using a two-dimensional high-performance liquid chromatography (2D-HPLC) system, was proposed for the direct analysis of drugs in human serum. A temperature-responsive column was used as a pretreatment column. The stationary phase of the temperature-responsive column exhibits temperature-regulated hydrophilic/hydrophobic characteristics. Controlling the ionic strength of the eluent enables human serum albumin (HSA) to pass through the column without retention...
October 29, 2016: Analytical and Bioanalytical Chemistry
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