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https://www.readbyqxmd.com/read/29778948/bioisosteres-of-ethyl-8-ethynyl-6-pyridin-2-yl-4h-benzo-f-imidazo-1-5-a-1-4-diazepine-3-carboxylate-hz-166-as-novel-alpha-2-3-selective-potentiators-of-gaba-a-receptors-improved-bioavailability-enhances-anticonvulsant-efficacy
#1
J M Witkin, J L Smith, X Ping, S D Gleason, M M Poe, G Li, X Jin, J Hobbs, J M Schkeryantz, J S McDermott, A I Alatorre, J N Siemian, J W Cramer, D C Airey, K R Methuku, V V N P B Tiruveedhula, T M Jones, J Crawford, M J Krambis, J L Fisher, J M Cook, R Cerne
HZ-166 has previously been characterized as an α2,3-selective GABAA receptor modulator with anticonvulsant, anxiolytic, and anti-nociceptive properties but reduced motor effects. We discovered a series of ester bioisosteres with reduced metabolic liabilities, leading to improved efficacy as anxiolytic-like compounds in rats. In the present study, we evaluated the anticonvulsant effects KRM-II-81 across several rodent models. In some models we also evaluated key structural analogs. KRM-II-81 suppressed hyper-excitation in a network of cultured cortical neurons without affecting the basal neuronal activity...
May 3, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29767950/different-benzodiazepines-bind-with-distinct-binding-modes-to-gaba-a-receptors
#2
Alshaimaa A Elgarf, David C B Siebert, Friederike Steudle, Angelika Draxler, Guanguan Li, Shengming Huang, James M Cook, Margot Ernst, Petra Scholze
Benzodiazepines are clinically relevant drugs, which bind to GABAA neurotransmitter receptors at the α+/γ2- interfaces and thereby enhance GABA induced chloride ion flux leading to neuronal hyperpolarization. However, the structural basis of benzodiazepine interactions with their high affinity site at GABAA receptors is controversially debated in the literature and in silico studies led to discrepant binding mode hypotheses. In the current study computational docking of diazepam into α+/γ2- homology models suggested that a chiral methyl group, which is known to promote preferred binding to α5-containing GABAA receptors (position 3 of the 7-membered diazepine ring), could possibly provide experimental evidence in favor of or against the so far proposed binding modes...
May 16, 2018: ACS Chemical Biology
https://www.readbyqxmd.com/read/29766039/beneficial-outcome-of-urethane-treatment-following-status-epilepticus-in-a-rat-organophosphorus-toxicity-model
#3
Asheebo Rojas, Wenyi Wang, Avery Glover, Zahra Manji, Yujiao Fu, Raymond Dingledine
The efficacy of benzodiazepines to terminate electrographic status epilepticus (SE) declines the longer a patient is in SE. Therefore, alternative methods for ensuring complete block of SE and refractory SE are necessary. We compared the ability of diazepam and a subanesthetic dose of urethane to terminate prolonged SE and mitigate subsequent pathologies. Adult Sprague Dawley rats were injected with diisopropylfluorophosphate (DFP) to induce SE. Rats were administered diazepam (10 mg/kg, ip) or urethane (0...
March 2018: ENeuro
https://www.readbyqxmd.com/read/29753067/drug-interaction-study-of-flavonoids-toward-cyp3a4-and-their-quantitative-structure-activity-relationship-qsar-analysis-for-predicting-potential-effects
#4
Yannan Li, Jing Ning, Yan Wang, Chao Wang, Chengpeng Sun, Xiaokui Huo, Zhenlong Yu, Lei Feng, Baojing Zhang, Xiangge Tian, Xiaochi Ma
The high risk of herb-drug interactions (HDIs) mediated by the herbal medicines and dietary supplements which containing abundant flavonoids had become more and more frequent in our daily life. In our study, the inhibition activities of 44 different structures of flavonoids toward human CYPs were systemically evaluated for the first time. According to our results, a remarkable structure-dependent inhibition behavior toward CYP3A4 was observed in vitro. Some flavonoids such as licoflavone (12) and irilone (30) exhibited the selective inhibition toward CYP3 A4 rather than other major human CYPs...
May 9, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29749988/amelioration-of-pentylenetetrazole-induced-seizures-by-modulators-of-sigma-n-methyl-d-aspartate-and-ryanodine-receptors-in-mice
#5
Mojtaba Keshavarz, Behdad Yekzaman
Background: Sigma receptors, N-methyl-D-aspartate (NMDA) antagonist, and modulators of intracellular calcium may be useful for seizure control. Therefore, we aimed to evaluate the antiepileptic effects of opipramol, a sigma receptor agonist, against pentylenetetrazole (PTZ)-induced seizures in mice and assess ketamine and caffeine interaction with the antiepileptic effects of opipramol. Methods: PTZ (100 mg/kg) was used for the induction of seizure in 72 male albino Swiss strain of mice (n=8)...
March 2018: Iranian Journal of Medical Sciences
https://www.readbyqxmd.com/read/29749024/determining-the-effects-of-adulterants-on-drug-detection-via-elisa-and-adulterant-tests-strips
#6
Bianca Olivieri, Mark Marić, Candice Bridge
The use of immunoassays for drug screening has increased due to their sensitivity towards target analytes, specifically the enzyme linked immunosorbent assay (ELISA) technique. Adulterant test strips are commonly used in conjunction with immunoassay tests to ensure that the integrity of the specimen has not been altered prior to drug screening. This research focuses on determining which adulterants can produce a false negative result, not only with one of the screening tests, but throughout the entire screening process...
May 10, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29748917/taurine-protects-from-pentylenetetrazole-induced-behavioral-and-neurochemical-changes-in-zebrafish
#7
Barbara D Fontana, Paola R Ziani, Julia Canzian, Nathana J Mezzomo, Talise E Müller, Matheus M Dos Santos, Vania L Loro, Nilda V Barbosa, Carlos F Mello, Denis B Rosemberg
Epilepsy is a common neurological disorder characterized by recurrent unprovoked seizures, which culminate in various neurobehavioral and neurochemical changes. Taurine (TAU) is an amino sulfonic acid which acts an endogenous inhibitory neuromodulator. Moreover, TAU displays intrinsic antioxidant activity, contributing to its beneficial actions in the CNS. Here, we evaluated whether TAU pretreatment protects from pentylenetetrazole (PTZ)-induced behavioral alterations and oxidative stress-related parameters in zebrafish brain tissue...
May 11, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29747564/reduse-reducing-antipsychotic-and-benzodiazepine-prescribing-in-residential-aged-care-facilities
#8
Juanita L Westbury, Peter Gee, Tristan Ling, Donnamay T Brown, Katherine H Franks, Ivan Bindoff, Aidan Bindoff, Gregory M Peterson
OBJECTIVE: To assess the impact of a multi-strategic, interdisciplinary intervention on antipsychotic and benzodiazepine prescribing in residential aged care facilities (RACFs). Design, setting: Prospective, longitudinal intervention in Australian RACFs, April 2014 - March 2016. PARTICIPANTS: 150 RACFs (with 12 157 residents) comprised the main participant group; two further groups were consultant pharmacists (staff education) and community pharmacies (prescribing data)...
May 14, 2018: Medical Journal of Australia
https://www.readbyqxmd.com/read/29746845/detection-of-stress-and-the-effects-of-central-nervous-system-depressants-by-gastrointestinal-smooth-muscle-electromyography-in-wakeful-rats
#9
K F Szűcs, G Grosz, M Süle, A Sztojkov-Ivanov, E Ducza, A Márki, A Kothencz, L Balogh, R Gáspár
AIMS: The altered gut-brain interaction can be in the background of functional gastrointestinal (GI) disorders. In the GI tract, the slow-wave myoelectric signals can be detected by electromyography (EMG). The aims of our study were to follow up the stress induced alteration in the GI tract by smooth muscle EMG in wakeful rats. MAIN METHODS: The GI tract myoelectric activity of male rats was measured by an electrode pair under the abdominal skin, the responses were detected and analyzed by a software using fast Fourier transformation...
May 7, 2018: Life Sciences
https://www.readbyqxmd.com/read/29744233/development-of-a-flow-injection-system-for-differential-pulse-amperometry-and-its-application-for-diazepam-determination
#10
Vesna Antunović, Slavna Tešanović, Danica Perušković, Nikola Stevanović, Rada Baošić, Snežana Mandić, Aleksandar Lolić
This work presents the development of a flow injection system for differential pulse amperometry (DPA) for diazepam determination in the presence of oxygen. The thin flow cell consisted of the bare glassy carbon electrode, reference silver/silver chloride, and stainless steel as the auxiliary electrode. Electrochemical reduction of diazepam (DZP) was characterised by cyclic voltammetry. Azomethine reduction peak was used for DZP quantification. The detector response was linear in the range 20-250  µ mol/dm3 of diazepam, with a calculated detection limit of 3...
2018: Journal of Analytical Methods in Chemistry
https://www.readbyqxmd.com/read/29743978/clarified-a%C3%A3-a%C3%A3-euterpe-oleracea-juice-as-an-anticonvulsant-agent-in-vitro-mechanistic-study-of-gabaergic-targets
#11
Gabriela P F Arrifano, Mathieu P Lichtenstein, José Rogério Souza-Monteiro, Marcelo Farina, Hervé Rogez, José Carlos Tavares Carvalho, Cristina Suñol, Maria Elena Crespo-López
Seizures affect about 50 million people around the world. Approximately 30% of seizures are refractory to the current pharmacological arsenal, so, the pursuit of new therapeutic alternatives is essential. Clarified Euterpe oleracea (EO) juice showed anticonvulsant properties similar to diazepam in an in vivo model with pentylenetetrazol, a GABAA receptor blocker. This study investigated the effects of EO on the main GABAergic targets for anticonvulsant drugs, analyzing the effect on the GABA receptor's benzodiazepine and picrotoxinin binding sites and the GABA uptake...
2018: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/29743852/n1-benzenesulfonyl-2-pyrazoline-hybrids-in-neurological-disorders-syntheses-biological-screening-and-computational-studies
#12
Avinash C Tripathi, Savita Upadhyay, Sarvesh Paliwal, Shailendra K Saraf
A novel series of 1,3,5-trisubstituted-2-pyrazolines (5a-5t ) was prepared via Claisen Schmidt condensation, followed by heterocyclization with hydrazine hydrate, substitution of N1 hydrogen of 2-pyrazoline nucleus with 4-chlorobenzenesulfonylchloride, applying conventional and green chemistry approaches. Among the two, microwave assisted organic synthesis (MAOS) emerged as a better synthetic tool in terms of faster reaction rate and high yield. Various physicochemical and spectral studies were conducted to characterize the synthesized derivatives including- IR, Mass, 1 H-NMR, 13 C-NMR and elemental analysis...
2018: EXCLI Journal
https://www.readbyqxmd.com/read/29738701/flavones-bound-in-benzodiazepine-site-on-gaba-a-receptor-concomitant-anxiolytic-like-and-cognitive-enhancing-effects-produced-by-isovitexin-and-6-cglycoside-diosmetin
#13
Daniela Rodrigues de Oliveira, Andréia Hatsue Todo, Gizelda Maia Rêgo, Janete Maria Cerutti, Alberto José Cavalheiro, Daniela Gonçales Galasse Rando, Suzete Maria Cerutti
Increasing evidence suggests that flavones can modulate memory and anxiety-like behaviour. However, these therapeutic effects are inconsistent and induce of adverse effects, which have been associated with interactions at the Benzodiazepine (BZ)-binding site. To improve our understanding of flavone effects on memory and anxiety, we employed a plus-maze discriminative avoidance task. Furthermore, we evaluated the potential of the compounds in modulating GABAA receptors via BZ-binding site using molecular modelling studies...
May 5, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29728779/prevalence-of-selected-pharmaceuticals-in-surface-water-receiving-untreated-sewage-in-northwest-pakistan
#14
Aisha Khan, Dilawar Farhan Shams, Waliullah Khan, Aamir Ijaz, Muhammad Qasim, Maryam Saad, Ayesha Hafeez, Shams Ali Baig, Nisar Ahmed
This study investigated the occurrence of four non-steroidal anti-inflammatory drugs (NSAIDs) and four benzodiazepines/anti-depressants (ADs) in municipal wastewater in Mardan city, Pakistan, and in River Kabul and River Indus receiving untreated sewage. Liquid chromatography with a triple quadrupole tandem mass spectrometry (LC-MS/MS) was used for the analysis of paracetamol, diclofenac, ibuprofen, and codeine (NSAIDs) and diazepam, bromazepam, lorazepam, and temazepam (ADs). Except codeine and lorazepam, all the target compounds were observed in sewage and surface water in various concentrations...
May 4, 2018: Environmental Monitoring and Assessment
https://www.readbyqxmd.com/read/29726630/trends-in-the-long-term-use-of-benzodiazepine-anxiolytics-and-hypnotics-a-national-register-study-for-2006-to-2014
#15
Terhi Kurko, Leena K Saastamoinen, Annamari Tuulio-Henriksson, Tero Taiminen, Jari Tiihonen, Marja Airaksinen, Jarmo Hietala
PURPOSE: Long-term benzodiazepine (BZD) treatment continues to be a debated topic. Because individual BZDs have different clinical profiles, we assessed the nationwide trends of long-term BZD use at active substance level during years 2006 to 2014. METHODS: This study covered all reimbursed BZD purchases (n = 408 572-521 823 annually) for adults recorded in the Finnish Prescription Register. We assessed long-term use (annual cumulative purchase of ≥180 defined daily doses) in general, and at active substance level with the most commonly used BZD anxiolytics (oxazepam, diazepam, alprazolam, and clonazepam for nonepilepsy indications) and hypnotics (zopiclone, zolpidem, and temazepam) included...
May 4, 2018: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/29720907/sedation-and-analgesia-using-medications-delivered-via-the-extravascular-route-in-children-undergoing-laceration-repair
#16
REVIEW
Jamie L Miller, Amanda C Capino, Amber Thomas, Kevin Couloures, Peter N Johnson
OBJECTIVES: To describe the method of delivery, dosage regimens, and outcomes of sedatives and analgesics administered via the extravascular route for laceration repair in children. METHODS: Medline, Embase, and International Pharmaceutical Abstracts were searched using the keywords "child," "midazolam," "ketamine," dexmedetomidine," "fentanyl," "nitrous oxide" (N2 O), and "laceration repair." Articles evaluating the use of extravascular sedation in children for laceration repair published in the English language between 1946 and June 2017 were included...
March 2018: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/29720564/evidence-that-sedative-effects-of-benzodiazepines-involve-unexpected-gaba-a-receptor-subtypes-quantitative-observation-studies-in-rhesus-monkeys
#17
Angela N Duke, Zhiqiang Meng, Donna M Platt, John R Atack, Gerard R Dawson, David S Reynolds, V V N Phani Babu Tiruveedhula, Guanguan Li, Michael Rajesh Stephen, Werner Sieghart, James M Cook, James K Rowlett
Using non-human primates, we introduced a new set of behavioral categories for observable sedative effects based on pediatric anesthesiology classifications. We examined the effects of alprazolam and diazepam (non-selective benzodiazepines), zolpidem (preferential binding to α1 subunit-containing GABAA receptors), HZ-166 (8-ethynyl-6-(2'-pyridine)-4H-2,5,10b-triaza-benzo[e]azulene-3-carboxylic acid ethyl ester; functionally selective for α2 and α3 subunit-containing GABAA receptors), MRK-696 (7-cyclobutyl-6-(2-methyl-2H-1,2,4-triazol-2-ylmethoxy)-3-(2-flurophenyl)-1,2,4-triazolo(4,3-b)pyridazine; no selectivity but partial intrinsic activity), and TPA023B (6,2'-difluro-5'-(3-(1-hydroxy-1-methylethyl)imidazo(1,2-b((1,2,4)triazin-7-yl)(1,1'-biphenyl)-2-carbonitrile; selectivity for α2, α3, α5 subunit-containing GABAA receptors) using quantitative behavioral observation techniques in rhesus monkeys...
May 2, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29717425/removal-of-pharmaceutically-active-compounds-from-synthetic-and-real-aqueous-mixtures-and-simultaneous-disinfection-by-supported-tio-2-uv-a-h-2-o-2-uv-a-and-tio-2-h-2-o-2-uv-a-processes
#18
Morgana Bosio, Suéllen Satyro, João Paulo Bassin, Enrico Saggioro, Márcia Dezotti
Pharmaceutically active compounds are carried into aquatic bodies along with domestic sewage, industrial and agricultural wastewater discharges. Psychotropic drugs, which can be toxic to the biota, have been detected in natural waters in different parts of the world. Conventional water treatments, such as activated sludge, do not properly remove these recalcitrant substances, so the development of processes able to eliminate these compounds becomes very important. Advanced oxidation processes are considered clean technologies, capable of achieving high rates of organic compounds degradation, and can be an efficient alternative to conventional treatments...
May 1, 2018: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29715490/an-antidepressant-related-pharmacological-signature-for-positive-allosteric-modulators-of-%C3%AE-2-3-containing-gaba-a-receptors
#19
K R Methuku, X Li, R Cerne, S D Gleason, J M Schkeryantz, V V N P B Tiruveedhula, L K Golani, G Li, M M Poe, Md T Rahman, J M Cook, J L Fisher, J M Witkin
Data from transgenic animals and novel pharmacological agents has realigned scientific scrutiny on the therapeutic potential of positive allosteric modulators (PAMs) of α2/3-containing GABAA receptors. Evidence for analgesic, anticonvulsant, and anxiolytic activity of α2/3-selective PAMs has been presented along with the clinical potential for a milder motor-impacting profile compared to non-selective GABAA receptor PAMs. A new series of α2/3-selective PAMs was recently introduced which has anxiolytic and anticonvulsant activity in rodent models...
April 28, 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29714490/efficacy-of-ketamine-in-pediatric-sedation-dentistry-a-systematic-review
#20
Samuel Oh, Karl Kingsley
BACKGROUND: Ketamine has been used as a safe and effective sedative to treat adults and children exhibiting high levels of anxiety or fear during dental treatment. Pediatric dentistry often involves patients with high levels of anxiety and fear and possibly few positive dental experiences. Patient management can involve behavioral approaches, as well as the use of sedation or general anesthesia with a variety of agents, including midazolam, diazepam, hydroxyzine, meperidine, and ketamine...
May 2018: Compendium of Continuing Education in Dentistry
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