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Dantrolene

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https://www.readbyqxmd.com/read/28209803/correlation-between-membrane-protein-concentrations-and-transcellular-transport-activity-for-breast-cancer-resistance-protein
#1
Houfu Liu, Liang Huang, Yi Li, Tingting Fu, Xueying Sun, Yan-Yan Zhang, Ruina Gao, Qingfang Chen, Wandong Zhang, Jasminder Sahi, Scott Summerfield, Kelly Dong
Emerging evidence indicates an important role for breast cancer resistance protein (BCRP) in limiting brain penetration of substrate drugs. While in vitro Transwell® assays can provide an indication of BCRP substrate potential, the predictability of these to in vivo brain penetration is still under debate. The present study examines the correlation of BCRP protein concentration and transcellular transport activity across MDCKII monolayers. We expressed human BCRP or murine Bcrp1 in MDCKII wild-type cells using BacMam2 virus transduction...
February 16, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28181698/calcium-uptake-via-mitochondrial-uniporter-contributes-to-palmitic-acid-induced-apoptosis-in-mouse-podocytes
#2
Zeting Yuan, Aili Cao, Hua Liu, Henjiang Guo, Yingjun Zang, Yi Wang, Yunman Wang, Hao Wang, Peihao Yin, Wen Peng
Podocytes are component cells of the glomerular filtration barrier, and their loss by apoptosis is the main cause of proteinuria that leads to diabetic nephropathy (DN). Therefore, insights into podocyte apoptosis mechanism would allow a better understanding of DN pathogenesis and thus help develop adequate therapeutic strategies. Here, we investigated the molecular mechanism of palmitic acid-inhibited cell death in mouse podocytes, and found that palmitic acid increased cell death in a dose- and time-dependent manner...
February 9, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28166109/whether-to-proceed-with-deep-brain-stimulator-battery-change-in-a-patient-with-signs-of-potential-sepsis-and-parkinson-hyperpyrexia-syndrome-a-case-report
#3
Chyong-Jy Joyce Liu, Anica Crnkovic, John Dalfino, Leina Yoko Singh
Parkinsonism-hyperpyrexia syndrome (PHS) is a neurologic emergency associated with anti-Parkinson medication withdrawal; however, its clinical presentation mimics sepsis. We describe the case of a 69-year-old man with advanced Parkinson disease who presented for exchange of the depleted battery in his subthalamic deep brain stimulator. The patient's preoperative symptoms of fever, rigidity, altered consciousness, and autonomic instability presented a dilemma whether to proceed with battery exchange to treat PHS or postpone surgery due to potential sepsis...
February 3, 2017: A & A Case Reports
https://www.readbyqxmd.com/read/28149827/a-case-of-rapid-progression-of-postoperative-hyperthermia-dantrolene-or-not-dilemma
#4
Marzieh R Honardar, Jesus Rubio, Sanjay M Bhananker
Malignant hyperthermia (MH) is an extremely rare and life-threatening differential diagnosis of postoperative fever. We present an 8-month-old child scheduled for elective outpatient procedure who rapidly developed high fever, tachycardia, and respiratory acidosis shortly after transfer to the postanesthesia care unit. MH hotline expert recommended administering dantrolene, but there was no evidence of hypermetabolism or lactic acidosis. The patient remained clinically stable after admission to the pediatric intensive care unit and was discharged home the next day...
October 2016: International Journal of Critical Illness and Injury Science
https://www.readbyqxmd.com/read/28138998/current-and-prospective-sights-in-mechanism-of-deoxynivalenol-induced-emesis-for-future-scientific-study-and-clinical-treatment
#5
REVIEW
Liangkai Chen, Zhao Peng, Andreas K Nüssler, Liegang Liu, Wei Yang
Deoxynivalenol (DON), one of trichothecene mycotoxins produced by the fungus Fusarium, is commonly detected in cereal foods and in secondary food production across the world. Lower concentrations of DON induce a dose-related feed refusal (anorexia), whereas it acts as a potent emetic agent at higher levels. DON-induced emesis in humans and livestock can be observed and recorded in both undeveloped and developed regions such as Lixian, Guide and Huangzhong in China and Illinois in the USA. Some studies with different animal models (pigs and minks) suggested that DON could change expressions of 5-hydroxytryptamine, peptide YY, neuropeptide Y2 receptor and nucleobindin-2/nesfatin-1 in plasma and different areas of the brain...
January 31, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/28132918/ciproxifan-a-histamine-h3-receptor-antagonist-and-inverse-agonist-presynaptically-inhibits-glutamate-release-in-rat-hippocampus
#6
Cheng-Wei Lu, Tzu-Yu Lin, Chia-Ying Chang, Shu-Kuei Huang, Su-Jane Wang
Ciproxifan is an H3 receptor antagonist and inverse agonist with antipsychotic effects in several preclinical models; its effect on glutamate release has been investigated in the rat hippocampus. In a synaptosomal preparation, ciproxifan reduced 4-aminopyridine (4-AP)-evoked Ca(2+)-dependent glutamate release and cytosolic Ca(2+) concentration elevation but did not affect the membrane potential. The inhibitory effect of ciproxifan on 4-AP-evoked glutamate release was prevented by the Gi/Go-protein inhibitor pertussis toxin and Cav2...
January 27, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28111173/cardiac-expression-of-ryanodine-receptor-subtype-3-a-strategic-component-in-the-intracellular-ca-2-release-system-of-purkinje-fibers-in-large-mammalian-heart
#7
Rebecca E Daniels, Kazi T Haq, Lawson S Miller, Elizabeth W Chia, Masahito Miura, Vincenzo Sorrentino, John J McGuire, Bruno D Stuyvers
BACKGROUND: Three distinct Ca(2+) release channels were identified in dog P-cells: the ryanodine receptor subtype 2 (RyR2) was detected throughout the cell, while the ryanodine receptor subtype 3 (RyR3) and inositol phosphate sensitive Ca(2+) release channel (InsP3R) were found in the cell periphery. How each of these channels contributes to the Ca(2+) cycling of P-cells is unclear. Recent modeling of Ca(2+) mobilization in P-cells suggested that Ca(2+) sensitivity of Ca(2+)induced Ca(2+)release (CICR) was larger at the P-cell periphery...
January 20, 2017: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/28098197/dantrolene-versus-amiodarone-for-cardiopulmonary-resuscitation-a-randomized-double-blinded-experimental-study
#8
Thomas Wiesmann, Dennik Freitag, Wolfgang Dersch, Daphne Eschbach, Marc Irqsusi, Thorsten Steinfeldt, Hinnerk Wulf, Carsten Feldmann
Dantrolene was introduced for treatment of malignant hyperthermia. It also has antiarrhythmic properties and may thus be an alternative to amiodarone for the treatment of ventricular fibrillation (VF). Aim of this study was to compare the return of spontaneous circulation (ROSC) with dantrolene and amiodarone in a pig model of cardiac arrest. VF was induced in anesthetized pigs. After 8 min of untreated VF, chest compressions and ventilation were started and one of the drugs (amiodarone 5 mg kg(-1), dantrolene 2...
January 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28079659/suspected-malignant-hyperthermia-in-the-setting-of-hypothermic-circulatory-arrest-for-type-a-aortic-dissection-repair-a-case-report
#9
Bryant Bunting, Joshua Knight, Stephen M McHugh
Malignant Hyperthermia (MH) is a life-threatening biochemical process of hypermetabolism brought about in susceptible individuals by a triggering drug or event. Type A aortic dissections are surgical emergencies requiring cardiopulmonary bypass and frequently deep hypothermic circulatory arrest. We present a case of suspected MH in a patient undergoing emergent repair of a type A aortic dissection. Upon arrival at our institution, the patient had multiple signs of MH. However, no known triggering agent had been administered...
January 11, 2017: A & A Case Reports
https://www.readbyqxmd.com/read/28079567/cardiac-calcium-release-channel-ryanodine-receptor-2-regulation-by-halogenated-anesthetics
#10
Derek R Laver, John Attia, Christopher Oldmeadow, Anthony W Quail
BACKGROUND: Halogenated anesthetics activate cardiac ryanodine receptor 2-mediated sarcoplasmic reticulum Ca release, leading to sarcoplasmic reticulum Ca depletion, reduced cardiac function, and providing cell protection against ischemia-reperfusion injury. Anesthetic activation of ryanodine receptor 2 is poorly defined, leaving aspects of the protective mechanism uncertain. METHODS: Ryanodine receptor 2 from the sheep heart was incorporated into artificial lipid bilayers, and their gating properties were measured in response to five halogenated anesthetics...
March 2017: Anesthesiology
https://www.readbyqxmd.com/read/28035645/reflex-arc-of-the-teeth-clenching-induced-pressor-response-in-rats
#11
Ichiro Shoji, Takehito Kemuriyama, Megumi Tandai-Hiruma, Satoshi Maruyama, Akimasa Tashiro, Hidetaka Yokoe, Yasuhiro Nishida
Although "teeth clenching" induces pressor response, the reflex tracts of the response are unknown. In this study, dantrolene administration inhibited teeth clenching generated by electrical stimulation of the masseter muscles and completely abolished the pressor response. In addition, trigeminal ganglion block or hexamethonium administration completely abolished the pressor response. Local anesthesia of molar regions significantly reduced the pressor response to 27 ± 10%. Gadolinium (mechanoreceptor blocker of group III muscle afferents) entrapment in masticatory muscles also significantly reduced the pressor response to 62 ± 7%...
December 29, 2016: Journal of Physiological Sciences: JPS
https://www.readbyqxmd.com/read/28027523/preparation-characterization-and-in-vivo-evaluation-of-a-formulation-of-dantrolene-sodium-with-hydroxypropyl-%C3%AE-cyclodextrin
#12
Mengmeng Chen, Qijuan Wu, Juan Jiang, Xin Jin, Shuang Liu, Miao Wang, Chunjie Zhao
Dantrolene sodium (Da) is an effective skeletal muscle relaxant. However, its pharmacological effects are severely limited owing to its poor solubility and low oral bioavailability. In order to solve these problems, an inclusion complex using hydroxypropyl-β-cyclodextrin (HP-β-CD) to improve the oral bioavailability of Da was prepared successfully by freeze-drying. The prepared complex was characterized by Powder X-ray diffractometry (PXRD), Fourier transform infrared spectroscopy (FTIR) and evaluated by a dissolution test and a pharmacokinetic study...
December 19, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27984222/succinylcholine-for-emergency-airway-rescue-in-class-b-ambulatory-facilities-the-society-for-ambulatory-anesthesia-position-statement
#13
Girish P Joshi, Meena S Desai, Steven Gayer, Hector Vila
Procedures in class B ambulatory facilities are performed exclusively with oral or IV sedative-hypnotics and/or analgesics. These facilities typically do not stock dantrolene because no known triggers of malignant hyperthermia (ie, inhaled anesthetics and succinylcholine) are available. This article argues that, in the absence of succinylcholine, the morbidity and mortality from laryngospasm can be significant, indeed, higher than the unlikely scenario of succinylcholine-triggered malignant hyperthermia. The Society for Ambulatory Anesthesia (SAMBA) position statement for the use of succinylcholine for emergency airway management is presented...
December 15, 2016: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/27939335/calcium-signalling-induced-by-in-vitro-exposure-to-silicium-dioxide-nanoparticles-in-rat-pulmonary-artery-smooth-muscle-cells
#14
Virginie Dubes, Thibaud Parpaite, Thomas Ducret, Jean-François Quignard, Stéphane Mornet, Nora Reinhardt, Isabelle Baudrimont, Mathilde Dubois, Véronique Freund-Michel, Roger Marthan, Bernard Muller, Jean-Pierre Savineau, Arnaud Courtois
The development and use of nanomaterials, especially engineered nanoparticles (NP), is expected to provide many benefits. But at the same time the development of such materials is also feared because of their potential human health risks. Indeed, NP display some characteristics similar to ultrafine environmental particles which are known to exert deleterious cardiovascular effects including pro-hypertensive ones. In this context, the effect of NP on calcium signalling, whose deregulation is often involved in hypertensive diseases, remain poorly described...
January 15, 2017: Toxicology
https://www.readbyqxmd.com/read/27918309/intraoperative-presentation-of-malignant-hyperthermia-confirmed-by-ryr1-gene-mutation-c-7522c-t-p-r2508c-leads-to-diagnosis-of-king-denborough-syndrome-in-a-child-with-hypotonia-and-dysmorphic-features-a-case-report
#15
Mark R Joseph, Mary C Theroux, James J Mooney, Shawn Falitz, Barbara W Brandom, Debra L Byler
We present the novel case report of a child with hypotonia and dysmorphic features who developed malignant hyperthermia (MH) intraoperatively. Neurology workup revealed the presence of a known causative ryanodine receptor (RYR1) mutation for MH, c.7522C>T; p.R2508C. Furthermore, the neurology workup diagnosed the child with King-Denborough syndrome (KDS). This particular mutation has never been documented in a patient with KDS. Atypical presentation of MH is more likely in patients with RYR1-related myopathy...
February 1, 2017: A & A Case Reports
https://www.readbyqxmd.com/read/27889824/erratum-to-counter-flow-suggests-transport-of-dantrolene-and-5-oh-dantrolene-by-the-organic-anion-transporters-2-oat2-and-3-oat3
#16
Birgitta C Burckhardt, Maja Henjakovic, Yohannes Hagos, Gerhard Burckhardt
No abstract text is available yet for this article.
November 2016: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/27882090/clinical-treatment-of-malignant-hyperthermia-in-three-cases
#17
Tao Pan, Wenli Ji, Mengqi Nie, Yang Li
Malignant hyperthermia (MH) is a rare life threatening inherited disorder that is triggered by drugs used for general anesthesia in susceptible persons. The symptoms include rapid increase of body temperature and severe muscle contractions. The present study includes 3 cases of MH and highlights the timely identification of symptoms for rescuing the patient. In case I, a 7-year-old male child underwent surgery with ketamine at a dose of 250 mg. After 4 h of operation, the child went through convulsions, high fever and succumbed within a few hours...
November 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27854207/long-term-oral-dantrolene-improved-muscular-symptoms-in-a-malignant-hyperthermia-susceptible-individual
#18
Brian N Butala, Audry Kang, Jasmeen Guron, Barbara W Brandom
This case report describes a female with p.Lys4876Arg amino acid change in the ryanodine receptor type 1 (RYR1) and a sibling who died of malignant hyperthermia (MH) during anesthesia. After her diagnosis as MH susceptible, this patient was administered low-dose dantrolene daily for greater than 25 years for treatment of chronic muscle spasm and pain in her lower extremities and back limiting sleep. Her creatine phosphokinase (CPK) was as high as 2390 IU/L during labor and 900 IU at rest. With 25 mg dantrolene daily, muscle cramps were eliminated, and sleep was improved...
March 3, 2016: Journal of Neuromuscular Diseases
https://www.readbyqxmd.com/read/27832686/dantrolene-a-selective-ryanodine-receptor-antagonist-protects-against-pentylenetetrazole-induced-seizure-in-mice
#19
Mojtaba Keshavarz, Morteza Fotouhi, Alireza Rasti
Ryanodine receptor abnormalities has implicated in the generation and maintenance of seizure. Dantrolene, a selective ryanodine receptor antagonist, may be a potential drug for the prevention of seizure. Therefore, we aimed to clarify the protective effects of dantrolene against pentylenetetrazole seizure in mice. Male albino mice were received an intra-peritoneal injection of pentylenetetrazole (80 mg/kg) in seven separate groups (n=8). We used dantrolene (10,20 and 40 mg/kg), caffeine (200 mg/kg), dantrolene (40 mg/kg) + caffeine (200 mg/kg), diazepam (5 mg/kg as a positive control) and vehicle 30 minutes before the injection of pentylenetetrazole...
September 2016: Acta Medica Iranica
https://www.readbyqxmd.com/read/27812757/counter-flow-suggests-transport-of-dantrolene-and-5-oh-dantrolene-by-the-organic-anion-transporters-2-oat2-and-3-oat3
#20
Birgitta C Burckhardt, Maja Henjakovic, Yohannes Hagos, Gerhard Burckhardt
Dantrolene is the only available drug for the treatment of malignant hyperthermia, a life-threatening inborn sensitivity of the ryanodine receptor (RyR1) in skeletal muscles to volatile anesthetics. Dantrolene is metabolized in the liver to 5-OH dantrolene. Both compounds are zwitterions or net negatively charged. Here, we investigated interactions of dantrolene and 5-OH dantrolene with solute carrier (SLC) family members occurring in skeletal muscle cells, hepatocytes, and renal proximal tubule cells. SLC22A8 (organic anion transporter 3, OAT3) was very sensitive to both compounds exhibiting IC50 values of 0...
November 2016: Pflügers Archiv: European Journal of Physiology
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