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https://www.readbyqxmd.com/read/28337724/i-123-iomazenil-single-photon-emission-computed-tomography-for-detecting-loss-of-neuronal-integrity-in-patients-with-traumatic-brain-injury
#1
Kagari Abiko, Katsunori Ikoma, Tohru Shiga, Chietsugu Katoh, Kenji Hirata, Yuji Kuge, Kentaro Kobayashi, Nagara Tamaki
BACKGROUND: Traumatic brain injury (TBI) causes brain dysfunction in many patients. Using C-11 flumazenil (FMZ) positron emission tomography (PET), we have detected and reported the loss of neuronal integrity, leading to brain dysfunction in TBI patients. Similarly to FMZ PET, I-123 iomazenil (IMZ) single photon emission computed tomography (SPECT) is widely used to determine the distribution of the benzodiazepine receptor (BZR) in the brain cortex. The purpose of this study is to examine whether IMZ SPECT is as useful as FMZ PET for evaluating the loss of neuronal integrity in TBI patients...
December 2017: EJNMMI Research
https://www.readbyqxmd.com/read/28328950/repeated-anaesthesia-with-isoflurane-and-medetomidine-midazolam-fentanyl-in-guinea-pigs-and-its-influence-on-physiological-parameters
#2
Sabrina Schmitz, Sabine Tacke, Brian Guth, Julia Henke
Repeated anaesthesia may be required in experimental protocols and in daily veterinary practice, but anaesthesia is known to alter physiological parameters in GPs (Cavia porcellus, GPs). This study investigated the effects of repeated anaesthesia with either medetomidine-midazolam-fentanyl (MMF) or isoflurane (Iso) on physiological parameters in the GP. Twelve GPs were repeatedly administered with MMF or Iso in two anaesthesia sets. One set consisted of six 40-min anaesthesias, performed over 3 weeks (2 per week); the anaesthetic used first was randomized...
2017: PloS One
https://www.readbyqxmd.com/read/28301629/antidote-availability-in-the-municipality-of-campinas-s%C3%A3-o-paulo-brazil
#3
Luciane Cristina Rodrigues Fernandes, Taís Freire Galvão, Adriana Safioti Toledo Ricardi, Eduardo Mello De Capitani, Stephen Hyslop, Fábio Bucaretchi
CONTEXT AND OBJECTIVE: The lack of availability of antidotes in emergency services is a worldwide concern. The aim of the present study was to evaluate the availability of antidotes used for treating poisoning in Campinas (SP). DESIGN AND SETTING: This was a cross-sectional study of emergency services in Campinas, conducted in 2010-2012. METHODS: The availability, amount in stock, place of storage and access time for 26 antidotal treatments was investigated...
March 13, 2017: São Paulo Medical Journal, Revista Paulista de Medicina
https://www.readbyqxmd.com/read/28292021/antinociceptive-pharmacological-profile-of-dysphania-graveolens-in-mouse
#4
Myrna Déciga-Campos, Rachel Mata, Isabel Rivero-Cruz
This work evaluates the potential antinociceptive activity of Dysphania graveolens, traditional medicinal plant used in Mexico to treat stomach pain. A CH2Cl2-MeOH extract, infusion and essential oil from aerial parts of Dysphania graveolens were evaluated in hot plate and writhing tests in mice. The metabolites pinostrobin, pinocembrin and chrysin were isolated from the Dysphania graveolens infusion; next, they were evaluated in both nociceptive tests. To confirm the antinociceptive activity and explore the possible participation of opioid, GABA and serotonin receptors in the pharmacological mechanism, a formalin test was used...
March 7, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28265839/achyranthes-aspera-attenuates-epilepsy-in-experimental-animals-possible-involvement-of-gabaergic-mechanism
#5
Gollapalle Lakshminarayanashastry Viswanatha, Marikunte V Venkataranganna, Nunna Bheema Lingeswara Prasad, Ashok Godavarthi
The present study was aimed to examine the possible anticonvulsant property of aerial parts of Achyranthes aspera using various experimental models of epilepsy in mice. Petroleum ether extract of aerial parts of A. aspera (PeAA), methanolic eAA (MeAA) and aqueous eAA (AeAA) was initially evaluated against six-hertz seizure model in mice, based on the outcomes the effective extract was further evaluated against maximal electroshock (MES) and pentylenetetrazole (PTZ) models in mice. In addition, the potent extract was evaluated against the PTZ model by co-administering with flumazenil (FMZ), and also evaluated for its effect on GABA levels in brain and NMDA-induced lethality in mice...
March 6, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28259526/review-of-intranasally-administered-medications-for-use-in-the-emergency-department
#6
Abby M Bailey, Regan A Baum, Karolyn Horn, Tameka Lewis, Kate Morizio, Amy Schultz, Kyle Weant, Stephanie N Justice
BACKGROUND: Intranasal (IN) medication delivery is a viable alternative to other routes of administration, including intravenous (IV) and intramuscular (IM) administration. The IN route bypasses the risk of needle-stick injuries and alleviates the emotional trauma that may arise from the insertion of an IV catheter. OBJECTIVE: This review aims to evaluate published literature on medications administered via the IN route that are applicable to practice in emergency medicine...
March 1, 2017: Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28255314/anticonvulsant-activity-of-dorema-ammoniacum-gum-evidence-for-the-involvement-of-benzodiazepines-and-opioid-receptors
#7
Manijeh Motevalian, Saeed Mehrzadi, Samira Ahadi, Asie Shojaii
This study investigated the anticonvulsant activity and possible mechanism of action of an aqueous solution of Dorema ammoniacum gum (DAG) which has been used traditionally in the treatment of convulsions. In this study, the anticonvulsant activity of DAG was examined using the pentylentetrazole (PTZ) model in mice. Thirty male albino mice were divided randomly and equally to 5 groups, and pretreated with normal saline, diazepam, or various doses of DAG (500, 700, and 1000 mg/kg, i.p.), prior to the injection of PTZ (60 mg/kg, i...
February 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28255031/progressive-cortical-neuronal-damage-and-extracranial-intracranial-bypass-surgery-in-patients-with-misery-perfusion
#8
H Yamauchi, S Kagawa, Y Kishibe, M Takahashi, T Higashi
BACKGROUND AND PURPOSE: Misery perfusion may cause selective neuronal damage in atherosclerotic ICA or MCA disease. Bypass surgery can improve misery perfusion and may prevent neuronal damage. On the other hand, surgery conveys a risk for neuronal damage. The purpose of this retrospective study was to determine whether progression of cortical neuronal damage in surgically treated patients with misery perfusion is larger than that in surgically treated patients without misery perfusion or medically treated patients with misery perfusion...
March 2, 2017: AJNR. American Journal of Neuroradiology
https://www.readbyqxmd.com/read/28229437/pharmacokinetic-modeling-of-11-c-flumazenil-kinetics-in-the-rat-brain
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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...
April 3, 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
#17
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
#18
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
#19
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
#20
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
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