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https://www.readbyqxmd.com/read/28229437/pharmacokinetic-modeling-of-11-c-flumazenil-kinetics-in-the-rat-brain
#1
Isadora Lopes Alves, David Vállez García, Andrea Parente, Janine Doorduin, Rudi Dierckx, Ana Maria Marques da Silva, Michel Koole, Antoon Willemsen, Ronald Boellaard
BACKGROUND: Preferred models for the pharmacokinetic analysis of [(11)C]flumazenil human studies have been previously established. However, direct translation of these models and settings to animal studies might be sub-optimal. Therefore, this study evaluates pharmacokinetic models for the quantification of [(11)C]flumazenil binding in the rat brain. Dynamic (60 min) [(11)C]flumazenil brain PET scans were performed in two groups of male Wistar rats (tracer dose (TD), n = 10 and pre-saturated (PS), n = 2)...
December 2017: EJNMMI Research
https://www.readbyqxmd.com/read/28215510/short-term-treatment-with-flumazenil-restores-long-term-object-memory-in-a-mouse-model-of-down-syndrome
#2
Damien Colas, Bayarsaikhan Chuluun, Craig C Garner, H Craig Heller
Down syndrome (DS) is a common genetic cause of intellectual disability yet no pro-cognitive drug therapies are approved for human use. Mechanistic studies in a mouse model of DS (Ts65Dn mice) demonstrate that impaired cognitive function is due to excessive neuronal inhibitory tone. These deficits are normalized by chronic, short-term low doses of GABAA receptor (GABAAR) antagonists in adult animals, but none of the compounds investigated are approved for human use. We explored the therapeutic potential of flumazenil (FLUM), a GABAAR antagonist working at the benzodiazepine binding site that has FDA approval...
February 12, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28192273/gabaa-receptor-subtypes-in-the-mouse-brain-regional-mapping-and-diazepam-receptor-occupancy-by-in-vivo-18-f-flumazenil-pet
#3
Adrienne Müller Herde, Dietmar Benke, William T Ralvenius, Linjing Mu, Roger Schibli, Hanns Ulrich Zeilhofer, Stefanie D Krämer
Classical benzodiazepines, which are widely used as sedatives, anxiolytics and anticonvulsants, exert their therapeutic effects through interactions with heteropentameric GABAA receptors composed of two α, two β and one γ2 subunit. Their high affinity binding site is located at the interface between the γ2 and the adjacent α subunit. The α-subunit gene family consists of six members and receptors can be homomeric or mixed with respect to the α-subunits. Previous work has suggested that benzodiazepine binding site ligands with selectivity for individual GABAA receptor subtypes, as defined by the benzodiazepine-binding α subunit, may have fewer side effects and may even be effective in diseases, such as schizophrenia, autism or chronic pain, that do not respond well to classical benzodiazepines...
February 10, 2017: NeuroImage
https://www.readbyqxmd.com/read/28160425/anxiolytic-like-effect-of-2-4-1-phenyl-1h-pyrazol-4-yl-methyl-piperazin-1-yl-ethan-1-ol-is-mediated-through-the-benzodiazepine-and-nicotinic-pathways
#4
Adriane F Brito, James O Fajemiroye, Hiasmin F S Neri, Dayane M Silva, Daiany P B Silva, Germán Sanz, Boniek G Vaz, Flávio S de Carvalho, Paulo C Ghedini, Luciano M Lião, Ricardo Menegatti, Elson A Costa
In this study we proposed the design, synthesis of a new compound 2-(4-((1-phenyl-1H-pyrazol-4-yl)methyl)piperazin-1-yl)ethan-1-ol (LQFM032), and pharmacological evaluation of its anxiolytic-like effect. This new compound was subjected to pharmacological screening refered to as Irwin test, prior to sodium pentobarbital-induced sleep, open field and wire tests. The anxiolytic-like effect of this compound was evaluated using elevated plus maze and light-dark box tests. In addition, the mnemonic activity was evaluated through step-down test...
February 3, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28150939/antinociceptive-effects-of-a-novel-%C3%AE-2-%C3%AE-3-subtype-selective-gabaa-receptor-positive-allosteric-modulator
#5
Lakeisha A Lewter, Janet L Fisher, Justin N Siemian, Kashi Reddy Methuku, Michael M Poe, James M Cook, Jun-Xu Li
Pain remains a challenging clinical condition and spinal GABAA receptors are crucial modulators of pain processing. α2/α3-subtype GABAA receptors mediate the analgesic actions of benzodiazepines. Positive allosteric modulators (PAMs) at α2/α3-subtype GABAA receptors may have analgesic potential. Here we report a new selective α2/α3-subtype GABAA receptor PAM in in vitro and in vivo pain assays. KRM-II-81 demonstrated similar efficacy at α1/α2/α3 GABAA receptors and negligible efficacy at α4/α5/α6 GABAA receptors, with α2 and α3-subtypes being 17- and 28-fold more potent than α1 subtypes in HEK-293T cells expressing GABAA receptors with different α subunits...
February 2, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28145981/the-anxiolytic-like-effect-of-rutin-in-rats-involves-gabaa-receptors-in-the-basolateral-amygdala
#6
Alberto Hernandez-Leon, María E González-Trujano, Alonso Fernández-Guasti
Rutin is a bioflavonoid found in medicinal plants used to reduce anxiety. Evidence is lacking of rutin's anxiolytic-like activity, putative mechanism(s) of action, and neural sites of effects. The basolateral amygdala (BLA) is the main brain region that regulates anxiety, through GABAA/benzodiazepine (BDZ) receptors, which are modulated by flavonoids. Therefore, the main aim of this study was to investigate whether the anxiolytic-like effect of rutin involves GABAA/BDZ receptors in the BLA. Rutin was administered systemically (30-1000 mg/kg, intraperitoneal) or microinjected into the BLA (16 nmol/4 µl, intracerebral), and its effects were assessed in the elevated plus-maze and open-field tests...
January 31, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28120243/flow-metabolism-uncoupling-in-the-cervical-spinal-cord-of-als-patients
#7
Toru Yamashita, Tetsuhiro Hatakeyama, Kota Sato, Yusuke Fukui, Nozomi Hishikawa, Yasuyuki Ohta, Yoshihiro Nishiyama, Nobuyuki Kawai, Takashi Tamiya, Koji Abe
Amyotrophic lateral sclerosis (ALS) is a fatal motor neuron disease. In ALS, both glucose consumption and neuronal intensity reportedly decrease in the cerebral motor cortex when measured by positron emission tomography (PET). In this study, we evaluated cervical spinal glucose metabolism, blood flow, and neuronal intensity of 10 ALS patients with upper extremity (U/E) atrophy both with (18)F-2-fluoro-2-deoxy-D-glucose ((18)F-FDG) PET and (11)C-flumazenil ((11)C-FMZ) PET. On the ipsilateral side of C5 and T1 levels, (18)F-FDG uptake increased significantly (*p < 0...
January 24, 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28111292/disruption-of-brain-mek-erk-sequential-phosphorylation-and-activation-during-midazolam-induced-hypnosis-in-mice-roles-of-gabaa-receptor-mek1-inactivation-and-phosphatase-mkp-3
#8
María Álvaro-Bartolomé, Glòria Salort, Jesús A García-Sevilla
Midazolam is a positive allosteric modulator at GABAA receptor that induces a short hypnosis and neuroplasticity, in which the sequential phosphorylation of MEK1/2 and ERK1/2 was shown to play a role. This study investigated the parallel activation of p-MEK and p-ERK and regulatory mechanisms induced by midazolam through the stimulation of GABAA receptors in the mouse brain. During the time course of midazolam (60mg/kg)-induced sleep in mice (lasting for about 2h) p-Ser217/221 MEK1/2 was increased (+146% to +258%) whereas, unexpectedly, p-Tyr204/Thr202 ERK1/2 was found decreased (-16% to -38%), revealing uncoupling of MEK to ERK signals in various brain regions...
January 19, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28098615/a-rising-tide-lifts-all-boats-increased-ventilation-may-be-involved-in-accelerated-recovery-from-isoflurane-anesthesia-after-flumazenil-administration
#9
Andrey B Petrenko, Hiroshi Baba
No abstract text is available yet for this article.
February 2017: Anesthesiology
https://www.readbyqxmd.com/read/28098614/flumazenil-modulation-of-the-%C3%AE-aminobutyric-acid-type-a-receptor-competitive-versus-noncompetitive-antagonism-at-the-agonist-binding-site
#10
Douglas E Raines
No abstract text is available yet for this article.
February 2017: Anesthesiology
https://www.readbyqxmd.com/read/28066107/anxiolytic-activity-of-aqueous-extract-of-camellia-sinensis-in-rats
#11
Rajeshwari Shastry, Sheetal Dinkar Ullal, Shreyas Karkala, Seema Rai, Akash Gadgade
OBJECTIVES: The present study was undertaken to evaluate anxiolytic effect of Camellia sinensis (CS) and possible mechanism on acute and chronic administration in rats. MATERIALS AND METHODS: Eight groups of rats with six in each group were used. Group I served as control. Group II received diazepam (1 mg/kg). Groups III, IV, and V received CS in doses of 3.3, 16.5, and 33 mg/kg, respectively. Three pharmacologically validated experimental models - elevated plus maze (EPM), light and dark box (LDB), and open field tests (OFT) - were employed...
November 2016: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28038309/diazepam-inhibits-electrically-evoked-and-tonic-dopamine-release-in-the-nucleus-accumbens-and-reverses-the-effect-of-amphetamine
#12
Alexander Gomez-A, Amanda M Fiorenza, Suelen L Boschen, Adam H Sugi, Danielle Beckman, Sergio T Ferreira, Kendall Lee, Charles D Blaha, Claudio Da Cunha
Diazepam is a benzodiazepine receptor agonist with anxiolytic and addictive properties. Although most drugs of abuse increase the level of release of dopamine in the nucleus accumbens, here we show that diazepam not only causes the opposite effect but also prevents amphetamine from enhancing dopamine release. We used 20 min sampling in vivo microdialysis and subsecond fast-scan cyclic voltammetry recordings at carbon-fiber microelectrodes to show that diazepam caused a dose-dependent decrease in the level of tonic and electrically evoked dopamine release in the nucleus accumbens of urethane-anesthetized adult male Swiss mice...
February 15, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28013354/gabaa-receptor-occupancy-by-subtype-selective-gabaa%C3%AE-2-3-modulators-pet-studies-in-humans
#13
Aurelija Jucaite, Zsolt Cselényi, Jaakko Lappalainen, Dennis J McCarthy, Chi-Ming Lee, Svante Nyberg, Katarina Varnäs, Per Stenkrona, Christer Halldin, Alan Cross, Lars Farde
RATIONALE: Sedation, dependence, and abuse liability limit the use of non-selective γ-aminobutyric acid (GABAA) receptor positive modulators for the treatment of anxiety. AZD7325 and AZD6280 are novel, subtype-selective GABAAα2,3 receptor positive modulators with limited sedative effects. OBJECTIVES: The current study aimed to confirm target engagement at GABAA receptors by AZD7325 and AZD6280 in humans and to determine the relationship between exposure, GABAA receptor occupancy, and tolerability...
February 2017: Psychopharmacology
https://www.readbyqxmd.com/read/27986927/histological-underpinnings-of-grey-matter-changes-in-fibromyalgia-investigated-using-multimodal-brain-imaging
#14
F B Pomares, T Funck, N A Feier, S Roy, A Daigle-Martel, M Ceko, S Narayanan, D Araujo, A Thiel, N Stikov, M A Fitzcharles, P Schweinhardt
: Chronic pain patients present with cortical grey matter alterations, observed with anatomical magnetic resonance (MR) imaging. Reduced regional grey matter volumes are often interpreted to reflect neurodegeneration but studies investigating the cellular origin of grey matter changes are lacking. We used multi-modal imaging to compare 26 post-menopausal women with 25 healthy controls (age range: 50-75 years) to test whether regional grey matter volume decreases in chronic pain are associated with compromised neuronal integrity...
December 16, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27932682/preliminary-assessment-of-midazolam-fentanyl-and-fluanisone-combination-for-the-sedation-of-rhesus-macaques-macaca-mulatta
#15
Henri G M J Bertrand, Charlotte F Sandersen, Paul A Flecknell
This study was undertaken to assess the suitability of fentanyl/fluanisone ('Hypnorm', VetaPharma; 0.315 mg/mL of fentanyl citrate and 10 mg/mL of fluanisone) alone or combined with midazolam in rhesus macaques. Fifteen rhesus macaques requiring sedation for veterinary procedures received an intramuscular (IM) dose range of Hypnorm from 0.01 mL/kg to 0.3 mL/kg either alone or combined with 0.5 mg/kg of midazolam. To reverse the sedation, flumazenil in combination with either naloxone, buprenorphine or butorphanol was administered intravenously (IV) or IM...
December 8, 2016: Laboratory Animals
https://www.readbyqxmd.com/read/27924205/risperidone-in-a-child-with-untractable-emergency-delirium-a-case-report
#16
Young Hee Shin, Seung Hyeon Lee, Dae Yoon Kim
A 6-year-old boy was scheduled for thoracic magnetic resonance imaging under deep sedation with midazolam 1.8 mg and propofol 100 µg/kg/min via intravenous injection. He showed emergence delirium in the post-anesthesia care unit. The staff attempted to calm him by administering flumazenil as an antidote for midazolam, propofol for further sedation, and meperidine. However, this was not successful. A psychiatrist recommended the use of antipsychotics. Administration of risperidone led to immediate resolution of the boy's symptoms and relaxed him...
December 2016: Korean Journal of Anesthesiology
https://www.readbyqxmd.com/read/27920113/flumazenil-in-benzodiazepine-overdose
#17
Howard An, Jesse Godwin
No abstract text is available yet for this article.
December 6, 2016: CMAJ: Canadian Medical Association Journal, Journal de L'Association Medicale Canadienne
https://www.readbyqxmd.com/read/27898636/flumazenil-use-for-isolated-ataxia-in-a-child
#18
Angela Regina, David Lee, Payal Sud, Diana Crevi
No abstract text is available yet for this article.
December 2016: Pediatric Emergency Care
https://www.readbyqxmd.com/read/27886620/pet-measurement-of-gaba-shift-in-the-rat-brain-a-preclinical-application-of-bolus-plus-constant-infusion-paradigm-of-18-f-flumazenil
#19
Wook Kim, Hyun Soo Park, Byung Seok Moon, Byung Chul Lee, Sang Eun Kim
INTRODUCTION: We measured the tiagabine-induced enhancement of the GABAA receptor's affinity for benzodiazepine ligands ("GABA shift") using [(18)F]flumazenil (FMZ) PET with preclinical application of bolus plus constant infusion (B/I). Differences in quantified results of [(18)F]FMZ binding were compared to that of [(18)F]FMZ PET with single bolus injection (SB). MATERIALS AND METHODS: Sprague-Dawley rats underwent [(18)F]FMZ PET scans with B/I, which consisted of baseline and "GABA shift" sessions in a scan, or scans with SB one week apart...
February 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27875053/pharmacological-reversal-agents-in-dental-practice-keys-to-patient-safety
#20
Mark Donaldson, Jason H Goodchild
Though uncommon, medical emergencies in the dental office are harrowing occurrences that can be the result of adverse drug reactions. Pharmacological antagonists have been developed for administration as reversal agents in emergency situations in which patients may have an untoward effect, typically caused by too much medication. Dental practitioners should be familiar with these agents to keep patients safe and help mitigate drug-induced medical emergencies. This article reviews the pharmacokinetic and pharmacodynamic principles of pharmacological antagonists; it emphasizes six specific reversal agents as they relate to the clinical practice of dentistry: naloxone, flumazenil, epinephrine, diphenhydramine, phentolamine, and atropine...
November 2016: Compendium of Continuing Education in Dentistry
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