riluzole

Summary

Summary: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.

Top Publications

  1. ncbi Riluzole for amyotrophic lateral sclerosis (ALS)/motor neuron disease (MND)
    R G Miller
    Department of Neurology, California Pacific Medical Center, San Francisco, USA
    Amyotroph Lateral Scler Other Motor Neuron Disord 4:191-206. 2003
  2. pmc Riluzole treatment, survival and diagnostic criteria in Parkinson plus disorders: the NNIPPS study
    Gilbert Bensimon
    Departement de Pharmacologie Clinique, Hopital de la Pitie Salpetriere, Assistance Publique Hôpitaux de Paris and UPMC University Paris 06, UMR 7087, Paris, France
    Brain 132:156-71. 2009
  3. ncbi Metabotropic glutamate receptor 1 and glutamate signaling in human melanoma
    Jin Namkoong
    Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers University, 164 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Cancer Res 67:2298-305. 2007
  4. ncbi Microglial SK3 and SK4 currents and activation state are modulated by the neuroprotective drug, riluzole
    B S Liu
    Toronto Western Research Institute, University Health Network, MC9 417, 399 Bathurst Street, Toronto, Ontario M5T 2S8, Canada
    J Neuroimmune Pharmacol 8:227-37. 2013
  5. pmc The glutamate release inhibitor Riluzole decreases migration, invasion, and proliferation of melanoma cells
    Maithao N Le
    Division of Surgical Oncology, Department of Surgery, UMDNJ Robert Wood Johnson Medical School, Piscataway, New Jersey 08854, USA
    J Invest Dermatol 130:2240-9. 2010
  6. pmc Glial pathology in an animal model of depression: reversal of stress-induced cellular, metabolic and behavioral deficits by the glutamate-modulating drug riluzole
    M Banasr
    Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06437, USA
    Mol Psychiatry 15:501-11. 2010
  7. pmc A phase 0 trial of riluzole in patients with resectable stage III and IV melanoma
    Dana Yip
    Division of Surgical Oncology, Department of Surgery, UMDNJ Robert Wood Johnson Medical School, USA
    Clin Cancer Res 15:3896-902. 2009
  8. ncbi Differential neuroprotective effects of a minocycline-based drug cocktail in transient and permanent focal cerebral ischemia
    Yuan Cheng Weng
    Faculty of Medicine, Laval University, Centre de Recherche du CHUL CHUQ, Department of Anatomy and Physiology, T3 67, 2705, Boul Laurier, Quebec, QC, Canada G1V 4G2
    Exp Neurol 204:433-42. 2007
  9. ncbi Riluzole suppresses motor cortex facilitation in correlation to its plasma level. A study using transcranial magnetic stimulation
    P Schwenkreis
    Department of Neurology, Buerkle de la Camp Platz 1, Ruhr University Bochum, BG Kliniken Bergmannsheil, 44789 Bochum, Germany
    Exp Brain Res 135:293-9. 2000
  10. ncbi Riluzole enhances the activity of glutamate transporters GLAST, GLT1 and EAAC1
    Elena Fumagalli
    Istituto di Ricerche Farmacologiche Mario Negri, Via La Masa 19, 20156 Milan, Italy
    Eur J Pharmacol 578:171-6. 2008

Detail Information

Publications267 found, 100 shown here

  1. ncbi Riluzole for amyotrophic lateral sclerosis (ALS)/motor neuron disease (MND)
    R G Miller
    Department of Neurology, California Pacific Medical Center, San Francisco, USA
    Amyotroph Lateral Scler Other Motor Neuron Disord 4:191-206. 2003
    b>Riluzole 100 mg probably prolongs survival in patients with amyotrophic lateral sclerosis by about two months and the safety of the drug is not a major concern...
  2. pmc Riluzole treatment, survival and diagnostic criteria in Parkinson plus disorders: the NNIPPS study
    Gilbert Bensimon
    Departement de Pharmacologie Clinique, Hopital de la Pitie Salpetriere, Assistance Publique Hôpitaux de Paris and UPMC University Paris 06, UMR 7087, Paris, France
    Brain 132:156-71. 2009
    ..We designed a double-blind randomized placebo-controlled trial of riluzole as a potential disease-modifying agent in Parkinson plus disorders (NNIPPS: Neuroprotection and Natural History ..
  3. ncbi Metabotropic glutamate receptor 1 and glutamate signaling in human melanoma
    Jin Namkoong
    Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers University, 164 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Cancer Res 67:2298-305. 2007
    ..human melanoma cells with a GRM1 antagonist (LY367385 or BAY36-7620) or a glutamate release inhibitor (riluzole) leads to a suppression of cell proliferation as well as a decrease in levels of extracellular glutamate...
  4. ncbi Microglial SK3 and SK4 currents and activation state are modulated by the neuroprotective drug, riluzole
    B S Liu
    Toronto Western Research Institute, University Health Network, MC9 417, 399 Bathurst Street, Toronto, Ontario M5T 2S8, Canada
    J Neuroimmune Pharmacol 8:227-37. 2013
    ..Here, we assessed actions of the neuroprotective drug, riluzole, on two Ca(2+)- activated K channels in microglia - SK3 (KCa2.3, KCNN3) and SK4 (KCa3...
  5. pmc The glutamate release inhibitor Riluzole decreases migration, invasion, and proliferation of melanoma cells
    Maithao N Le
    Division of Surgical Oncology, Department of Surgery, UMDNJ Robert Wood Johnson Medical School, Piscataway, New Jersey 08854, USA
    J Invest Dermatol 130:2240-9. 2010
    ..Using the glutamate-release inhibitor Riluzole or the non-competitive GRM1 antagonist BAY 36-7620 we were able to induce considerable inhibition of colony ..
  6. pmc Glial pathology in an animal model of depression: reversal of stress-induced cellular, metabolic and behavioral deficits by the glutamate-modulating drug riluzole
    M Banasr
    Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06437, USA
    Mol Psychiatry 15:501-11. 2010
    ..Furthermore, we analyzed the effects of riluzole, a Food and Drug Administration-approved drug for the treatment of amyotrophic laterosclerosis, known to modulate ..
  7. pmc A phase 0 trial of riluzole in patients with resectable stage III and IV melanoma
    Dana Yip
    Division of Surgical Oncology, Department of Surgery, UMDNJ Robert Wood Johnson Medical School, USA
    Clin Cancer Res 15:3896-902. 2009
    ..Furthermore, a xenograft model of melanoma treated with riluzole, an oral GRM1 blocking agent, showed decreased tumor growth compared with the untreated controls...
  8. ncbi Differential neuroprotective effects of a minocycline-based drug cocktail in transient and permanent focal cerebral ischemia
    Yuan Cheng Weng
    Faculty of Medicine, Laval University, Centre de Recherche du CHUL CHUQ, Department of Anatomy and Physiology, T3 67, 2705, Boul Laurier, Quebec, QC, Canada G1V 4G2
    Exp Neurol 204:433-42. 2007
    ..It consists of minocycline--an antibiotic with anti-inflammatory properties, riluzole--a glutamate antagonist, and nimodipine--a blocker of voltage-gated calcium channels...
  9. ncbi Riluzole suppresses motor cortex facilitation in correlation to its plasma level. A study using transcranial magnetic stimulation
    P Schwenkreis
    Department of Neurology, Buerkle de la Camp Platz 1, Ruhr University Bochum, BG Kliniken Bergmannsheil, 44789 Bochum, Germany
    Exp Brain Res 135:293-9. 2000
    The aim of our study was to measure the effects of the glutamate antagonist riluzole on different parameters of motor excitability, using transcranial magnetic stimulation (TMS) during 7 days of riluzole administration, and to correlate ..
  10. ncbi Riluzole enhances the activity of glutamate transporters GLAST, GLT1 and EAAC1
    Elena Fumagalli
    Istituto di Ricerche Farmacologiche Mario Negri, Via La Masa 19, 20156 Milan, Italy
    Eur J Pharmacol 578:171-6. 2008
    b>Riluzole exerts a neuroprotective effect through different mechanisms, including action on glutamatergic transmission...
  11. pmc Metabotropic glutamate receptor-1: a potential therapeutic target for the treatment of breast cancer
    Cecilia L Speyer
    Breast Cancer Biology Program, Barbara Ann Karmanos Cancer Institute, Detroit, MI, USA
    Breast Cancer Res Treat 132:565-73. 2012
    ..mGluR1 inhibitors (Riluzole or BAY36-7620) inhibited the proliferation of triple negative breast cancer cells in a time- and dose-dependent ..
  12. pmc Chemical-genetic screen identifies riluzole as an enhancer of Wnt/β-catenin signaling in melanoma
    Travis L Biechele
    Howard Hughes Medical Institute, Department of Pharmacology, and Institute for Stem Cell and Regenerative Medicine, University of Washington School of Medicine, Box 357370, Seattle, WA 98195, USA
    Chem Biol 17:1177-82. 2010
    ..This identified 44 unique compounds, including the FDA-approved drug riluzole, which is presently in clinical trials for treating melanoma...
  13. ncbi Riluzole for amyotrophic lateral sclerosis (ALS)/motor neuron disease (MND)
    Robert G Miller
    Forbes Norris ALS Research Center, California PacificMedical Center, San Francisco, USA
    Cochrane Database Syst Rev 3:CD001447. 2012
    b>Riluzole is approved for the treatment of amyotrophic lateral sclerosis in most countries. Questions persist about its clinical utility because of high cost and modest efficacy.
  14. ncbi Creatine supplementation and riluzole treatment provide similar beneficial effects in copper, zinc superoxide dismutase (G93A) transgenic mice
    R J Snow
    School of Health Sciences, Deakin University, Victoria, 3125, Burwood, Australia
    Neuroscience 119:661-7. 2003
    This study investigated the effects of riluzole (Ril), creatine (Cr) and a combination of these treatments on the onset and progression of clinical signs and neuropathology in an animal model of familial amyotrophic lateral sclerosis, the ..
  15. pmc Glutamatergic pathway targeting in melanoma: single-agent and combinatorial therapies
    Hwa Jin Lee
    Department of Biological Science, Sookmyung Women s University, Seoul, South Korea
    Clin Cancer Res 17:7080-92. 2011
    ..preclinical efficacy of combining the multikinase inhibitor sorafenib or the mutated B-RAF inhibitor PLX4720 with riluzole, an inhibitor of glutamate release that antagonizes metabotropic glutamate receptor 1 (GRM1) signaling in ..
  16. pmc Diagnosis and management of motor neurone disease
    Christopher J McDermott
    Sheffield Care and Research Centre for Motor Neurone Disorders Academic Neurology Unit, Section of Neuroscience, University of Sheffield, Sheffield S10 2RX
    BMJ 336:658-62. 2008
  17. ncbi Evaluation of the benzothiazole aggregation inhibitors riluzole and PGL-135 as therapeutics for Huntington's disease
    Emma Hockly
    King s College London, Department of Medical and Molecular Genetics, GKT School of Medicine, 8th Floor Guy s Tower, Guy s Hospital, London SE1 9RT, UK
    Neurobiol Dis 21:228-36. 2006
    ..To further explore the therapeutic potential of the benzothiazole aggregation inhibitors, we assessed PGL-135 and riluzole in hippocampal slice cultures derived from the R6/2 mouse, confirming their ability to inhibit aggregation with ..
  18. ncbi Secondary injury mechanisms of spinal cord trauma: a novel therapeutic approach for the management of secondary pathophysiology with the sodium channel blocker riluzole
    Gwen Schwartz
    Toronto Western Research Institute, Division of Cell and Molecular Biology, Division of Neurosurgery, University of Toronto, Toronto, Canada
    Prog Brain Res 137:177-90. 2002
    ..This review describes the evolution of acute spinal cord injury and provides a rationale for the clinical utility of sodium channel blockers, particularly riluzole, in the management of spinal cord trauma.
  19. ncbi Delayed neuroprotection by riluzole against excitotoxic damage evoked by kainate on rat organotypic spinal cord cultures
    G L Mazzone
    Neurobiology Sector and IIT Unit, International School for Advanced Studies SISSA, Trieste, Italy
    Neuroscience 190:318-27. 2011
    ..Using such cultures, the putative neuroprotective agent riluzole applied at 5 μM (plasma therapeutic concentration) was studied for its ability to prevent neurotoxicity evoked ..
  20. pmc Neuroprotective drug riluzole amplifies the heat shock factor 1 (HSF1)- and glutamate transporter 1 (GLT1)-dependent cytoprotective mechanisms for neuronal survival
    Alice Y C Liu
    Department of Cell Biology and Neuroscience, Division of Life Sciences, Rutgers State University of New Jersey, Piscataway, New Jersey 08854, USA
    J Biol Chem 286:2785-94. 2011
    ..We show that the neuroprotective drug riluzole increased the amount of HSF1 in NG108-15 neuroprogenitor cells by slowing the specific turnover of HSF1 and ..
  21. ncbi Effects of riluzole on cortical excitability in patients with amyotrophic lateral sclerosis
    K Stefan
    Department of Neurology, University of Rostock, Germany
    Ann Neurol 49:536-9. 2001
    Using transcranial magnetic stimulation, the effect of riluzole (RLZ) on cortical excitability was studied in patients with amyotrophic lateral sclerosis (ALS)...
  22. ncbi CSF from amyotrophic lateral sclerosis patients produces glutamate independent death of rat motor brain cortical neurons: protection by resveratrol but not riluzole
    Matilde Yáñez
    Instituto Teófilo Hernando and Departamento de Farmacología y Terapéutica, Universidad Autonoma de Madrid, Madrid, Spain
    Brain Res 1423:77-86. 2011
    ..However, riluzole did not afford protection and antagonized the resveratrol-elicited neuroprotective effects...
  23. ncbi Mechanisms underlying the riluzole inhibition of glutamate release from rat cerebral cortex nerve terminals (synaptosomes)
    S J Wang
    School of Medicine, Fu Jen Catholic University, 510 Chung Cheng Road, Hsin Chuang, Taipei Hsien, Taiwan 24205
    Neuroscience 125:191-201. 2004
    We have examined the effect of riluzole, a neuroprotective agent with anticonvulsant properties, on the release of endogenous glutamate from rat cerebrocortical synaptosomes using an on-line enzyme-coupled fluorometric assay...
  24. pmc Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling
    Mark E McDonnell
    Fox Chase Chemical Diversity Center, Inc, 3805 Old Easton Road, Doylestown, PA 18902, USA
    Bioorg Med Chem 20:5642-8. 2012
    b>Riluzole (1) is an approved therapeutic for the treatment of ALS and has also demonstrated anti-melanoma activity in metabotropic glutamate GRM1 positive cell lines, a mouse xenograft assay and human clinical trials...
  25. ncbi Protective effects of riluzole on dopamine neurons: involvement of oxidative stress and cellular energy metabolism
    A Storch
    Department of Neurology, University of Ulm Medical School, Ulm, Germany
    J Neurochem 75:2259-69. 2000
    b>Riluzole is neuroprotective in patients with amyotrophic lateral sclerosis and may also protect dopamine (DA) neurons in Parkinson's disease...
  26. ncbi Differential effects of riluzole on subpopulations of adult rat dorsal root ganglion neurons in vitro
    V H L Leinster
    Queen Mary University of London, Barts and the London School of Medicine and Dentistry, Neuroscience and Trauma Centre, Blizard Institute of Cell and Molecular Science, Turner Street, London, E1 2AD, UK
    Neuroscience 166:942-51. 2010
    b>Riluzole is clinically approved for the treatment of motoneuron disease...
  27. ncbi Glutamate release inhibition ineffective in levodopa-induced motor complications
    William Bara-Jimenez
    Experimental Therapeutics Branch, National Institute of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, Maryland, USA
    Mov Disord 21:1380-3. 2006
    ..In a 3-week, double-blind, proof-of-concept study, riluzole (200 mg/day) failed to alter parkinsonian or levodopa-induced motor complication severity...
  28. pmc Increased survival and reinnervation of cervical motoneurons by riluzole after avulsion of the C7 ventral root
    Sandor Pinter
    Laboratory of Neuromorphology, Department of Ophthalmology, Faculty of General Medicine, University of Szeged, Szeged, Hungary
    J Neurotrauma 27:2273-82. 2010
    ..in very low numbers of surviving motoneurons (65 ± 8 SEM), while treatment of the injured motoneurons with riluzole resulted in high numbers of surviving motoneurons (637 ± 26 SEM)...
  29. ncbi Glutamatergic approaches in major depressive disorder: focus on ketamine, memantine and riluzole
    R T Owen
    Drugs Today (Barc) 48:469-78. 2012
    ..Trials with memantine and riluzole, agents with actions broadly similar to and different from ketamine on the glutamatergic system, are also ..
  30. pmc Riluzole elevates GLT-1 activity and levels in striatal astrocytes
    Marica Carbone
    King s College London, Wolfson Centre for Age Related Diseases, Guy s Campus, London SE1 1UL, UK
    Neurochem Int 60:31-8. 2012
    ..The neuroprotective compound riluzole (100 μM) upregulated GLT-1 levels and activity, through a mechanism that was not dependent on blockade of ..
  31. ncbi Riluzole prolongs survival time and alters nuclear inclusion formation in a transgenic mouse model of Huntington's disease
    Johannes Schiefer
    University Hospital RWTH Aachen, Department of Neurology, Aachen, Germany
    Mov Disord 17:748-57. 2002
    Glutamate excitotoxicity has been suggested to contribute to the pathogenesis of Huntington's disease (HD). Riluzole is a substance with glutamate antagonistic properties that is used for neuroprotective treatment in amyotrophic lateral ..
  32. ncbi Riluzole reduces brain lesions and improves neurological function in rats after a traumatic brain injury
    F Wahl
    Rhone Poulenc Rorer, Pharmaceuticals Discovery, Neurodegenerative Diseases Department, Vitry sur Seine, France
    Brain Res 756:247-55. 1997
    b>Riluzole (2-amino 6-trifluoromethoxy-benzothiazole) was studied in a rat model of traumatic brain injury (TBI) induced by a fluid percussion applied laterally to the right parietal cortex...
  33. ncbi Effect of riluzole on dyskinesia and duration of the on state in Parkinson disease patients: a double-blind, placebo-controlled pilot study
    Claudia A Braz
    Movement Disorders Unit, Department of Neurology, Universidade Federal de Sao Paulo, Brazil
    Clin Neuropharmacol 27:25-9. 2004
    The objective of this study was to evaluate the effect of riluzole on dyskinesia and the duration of the ON state in patients with Parkinson disease (PD). The authors studied 16 PD patients with levodopa-induced dyskinesia...
  34. pmc Comparative effects of glibenclamide and riluzole in a rat model of severe cervical spinal cord injury
    J Marc Simard
    Department of Neurosurgery, University of Maryland School of Medicine, Baltimore, MD 21201 1595, USA
    Exp Neurol 233:566-74. 2012
    Both glibenclamide and riluzole reduce necrosis and improve outcome in rat models of spinal cord injury (SCI)...
  35. ncbi Riluzole, neuroprotection and amyotrophic lateral sclerosis
    B C Cheah
    Prince of Wales Medical Research Institute, Barker Street, Randwick, NSW 2031, Australia
    Curr Med Chem 17:1942-199. 2010
    ..theory of ALS gave rise to the development of therapeutic approaches and ultimately clinical trials involving riluzole, initially thought to act solely as an inhibitor of glutamate release...
  36. ncbi A double-blind, placebo-controlled and longitudinal study of riluzole in early Parkinson's disease
    J Jankovic
    Parkinson s Disease Center and Movement Disorders Clinic, Baylor College of Medicine, 6550 Fannin Smith 1801, Houston, TX 77030, USA
    Parkinsonism Relat Disord 8:271-6. 2002
    ....
  37. ncbi Sodium and calcium current-mediated pacemaker neurons and respiratory rhythm generation
    Christopher A Del Negro
    Systems Neurobiology Laboratory, Department of Neurobiology, David Geffen School of Medicine at the University of California Los Angeles, Los Angeles, California 90095 1763, USA
    J Neurosci 25:446-53. 2005
    ..I(NaP)-mediated bursting was voltage dependent and blocked by 20 mum riluzole (RIL). We found Ca2+ current (I(Ca))-dependent bursting in 7...
  38. pmc Review of the use of the glutamate antagonist riluzole in psychiatric disorders and a description of recent use in childhood obsessive-compulsive disorder
    Paul Grant
    Pediatrics and Developmental Neuroscience PDN Branch, National Institute of Mental Health, Bethesda, Maryland 20892, USA
    J Child Adolesc Psychopharmacol 20:309-15. 2010
    The antiglutamatergic drug riluzole (Rilutek) is presently being used off label in the treatment of psychiatric conditions in adult patients and, increasingly, in children...
  39. ncbi Riluzole normalizes early-life stress-induced visceral hypersensitivity in rats: role of spinal glutamate reuptake mechanisms
    Romain Daniel Gosselin
    Laboratory of Neurogastroenterology, Alimentary Pharmabiotic Centre, University College Cork, Cork, Ireland
    Gastroenterology 138:2418-25. 2010
    ..Because alterations in spinal non-neuronal (astrocytic) glutamate reuptake are suspected to participate in chronic pain, we asked whether such processes occur in visceral hypersensitivity...
  40. pmc Inhibition of Navβ4 peptide-mediated resurgent sodium currents in Nav1.7 channels by carbamazepine, riluzole, and anandamide
    Jonathan W Theile
    Department of Pharmacology and Toxicology, Stark Neurosciences Research Institute, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Mol Pharmacol 80:724-34. 2011
    ..Here we examined whether carbamazepine and two other sodium channel inhibitors, riluzole and anandamide, exhibit differential inhibition of resurgent currents...
  41. ncbi Riluzole slows the progression of neuromuscular dysfunction in the wobbler mouse motor neuron disease
    Takeo Ishiyama
    Sumitomo Pharmaceuticals Research Division, 1 98 Kasugadenaka 3 chome, Konohanaku, Osaka 554 0022, Japan
    Brain Res 1019:226-36. 2004
    In the wobbler mouse motor neuron disease (MND), we firstly evaluated the effect of riluzole, the only approved drug for amyotrophic lateral sclerosis, and compared it with that of brain-derived neurotrophic factor (BDNF)...
  42. ncbi Early excitability changes in lumbar motoneurons of transgenic SOD1G85R and SOD1G(93A-Low) mice
    Arnaud Pambo-Pambo
    Laboratoire de Plasticité et Physio Pathologie de la Motricité, Unité Mixte de Recherche 6196 Centre National de la Recherche Scientifique, Aix Marseille Universite, Marseille, France
    J Neurophysiol 102:3627-42. 2009
    ....
  43. pmc Mechanisms underlying the early phase of spike frequency adaptation in mouse spinal motoneurones
    G B Miles
    Department of Anatomy and Neurobiology, Dalhousie University, Halifax, NS, Canada
    J Physiol 566:519-32. 2005
    ..iberiotoxin), voltage-activated Ca2+ channels (CdCl2), M-current (linopirdine) and persistent Na+ currents (riluzole) are all unnecessary for SFA...
  44. ncbi Comparative neuroprotective effect of sodium channel blockers after experimental spinal cord injury
    Ozkan Ates
    Inonu University, School of Medicine, Department of Neurosurgery, Turgut Ozal Medical Center, 44069 Malatya, Turkey
    J Clin Neurosci 14:658-65. 2007
    ..study was to compare the neuroprotective effect of three sodium channel blockers-mexiletine, phenytoin and riluzole--after SCI...
  45. ncbi Differential contribution of pacemaker properties to the generation of respiratory rhythms during normoxia and hypoxia
    Fernando Pena
    Department of Organismal Biology and Anatomy, The University of Chicago, Chicago, IL 60637, USA
    Neuron 43:105-17. 2004
    ..We propose that respiratory rhythm generation in normoxia depends on a heterogeneous population of pacemaker neurons, while during hypoxia the respiratory rhythm is driven by only one type of pacemaker...
  46. ncbi Lamotrigine derivatives and riluzole inhibit INa,P in cortical neurons
    Francesca Spadoni
    IRCCS Fondazione Santa Lucia, Roma, Italy
    Neuroreport 13:1167-70. 2002
    ..Two lamotrigine derivatives (sipatrigine and 202W92) and riluzole inhibited the persistent sodium current at low, therapeutic concentrations...
  47. ncbi Increased persistent sodium current determines cortical hyperexcitability in a genetic model of amyotrophic lateral sclerosis
    Massimo Pieri
    Department of Neuroscience, University of Rome Tor Vergata, Via Montpellier 1, 00133 Rome, Italy
    Exp Neurol 215:368-79. 2009
    ..Finally, Riluzole, a selective blocker of the persistent sodium current at low concentrations, decreased the firing frequency in ..
  48. ncbi Riluzole induces apoptotic cell death in human prostate cancer cells via endoplasmic reticulum stress
    Kanako Akamatsu
    Department of Anatomy and Cell Biology, Division of Life Sciences, Osaka Medical College, Takatsuki, Osaka 569 8686, Japan
    Anticancer Res 29:2195-204. 2009
    ..Ion channel modulators have been previously associated with cell proliferation and cell death in human cancer cell lines...
  49. pmc Safety and efficacy of lithium in combination with riluzole for treatment of amyotrophic lateral sclerosis: a randomised, double-blind, placebo-controlled trial
    Swati P Aggarwal
    Neurology Clinical Trials Unit, Massachusetts General Hospital, Charlestown, MA, USA
    Lancet Neurol 9:481-8. 2010
    ..In a pilot study, lithium treatment slowed progression of amyotrophic lateral sclerosis (ALS). We aimed to confirm or disprove these findings by assessing the safety and efficacy of lithium in combination with riluzole in patients with ALS.
  50. ncbi Brain and plasma riluzole pharmacokinetics: effect of minocycline combination
    Aline Milane
    Laboratoire de Barrières et Passage des Médicaments, EA 2706, Faculty of Pharmacy, Universite Paris Sud XI, Chatenay Malabry, Chatenay Malabry, France
    J Pharm Pharm Sci 12:209-17. 2009
    ..The only drug approved is riluzole. Minocycline is an antibiotic with numerous neuroprotective properties...
  51. pmc Riluzole enhances ionizing radiation-induced cytotoxicity in human melanoma cells that ectopically express metabotropic glutamate receptor 1 in vitro and in vivo
    Atif J Khan
    Department of Radiation Oncology, UMDNJ Robert Wood Johnson Medical School, Piscataway, New Jersey, USA
    Clin Cancer Res 17:1807-14. 2011
    ..human GRM1 (hGRM1) expressing melanoma cells release excess extracellular glutamate and are growth inhibited by riluzole, an inhibitor of glutamate release...
  52. ncbi Rasagiline alone and in combination with riluzole prolongs survival in an ALS mouse model
    Stefan Waibel
    Department of Neurology, University of Ulm, Oberer Eselsberg 45, 89081, Ulm, Germany
    J Neurol 251:1080-4. 2004
    ..We examined its neuroprotective effect alone and in combination with the putative glutamate release blocker riluzole in the G93A model of familial amyotrophic lateral sclerosis (fALS)...
  53. ncbi Molecular dissection of lubeluzole use-dependent block of voltage-gated sodium channels discloses new therapeutic potentials
    Jean Francois Desaphy
    Section of Pharmacology, Department of Pharmacy, University of Bari Aldo Moro, Bari, Italy
    Mol Pharmacol 83:406-15. 2013
    ..The lubeluzole structure contains a benzothiazole moiety [N-methyl-1,3-benzothiazole-2-amine (R-like)] related to riluzole and a phenoxy-propranol-amine moiety [(RS)-1-(3,4-difluorophenoxy)-3-(piperidin-1-yl)propan-2-ol (A-core)] ..
  54. ncbi Riluzole is a potent drug to protect neonatal rat hypoglossal motoneurons in vitro from excitotoxicity due to glutamate uptake block
    Alessandra Cifra
    Neurobiology Sector, International School for Advanced Studies SISSA, via Bonomea 265, 34136 Trieste, Italy
    Eur J Neurosci 33:899-913. 2011
    ..b>Riluzole is the only drug licensed for symptomatic ALS treatment and is proposed to delay disease progression...
  55. ncbi Activation of TREK currents by the neuroprotective agent riluzole in mouse sympathetic neurons
    Alba Cadaveira-Mosquera
    Department of Functional Biology and Biochemistry, University of Vigo, Campus Lagoas Marcosende, 36310 Vigo, Spain
    J Neurosci 31:1375-85. 2011
    ..Whole-cell experiments revealed a riluzole-activated current (I(RIL)), transported by potassium, in mouse superior cervical ganglion (mSCG) neurons...
  56. ncbi Intracerebroventricular administration of riluzole prevents morphine-induced apoptosis in the lumbar region of the rat spinal cord
    Kambiz Hassanzadeh
    Department of Physiology and Pharmacology, Faculty of Medicine, Kurdistan University of Medical Sciences, Pasdaran Street, Sanandaj, Iran, 66177 13446
    Pharmacol Rep 62:664-73. 2010
    ..The aim of this study is to evaluate the effects of intracerebroventricular (i.c.v.) administration of riluzole, an anti-glutamatergic drug, on morphine-induced apoptosis in the lumbar region of the rat spinal cord...
  57. ncbi Riluzole augmentation for treatment-resistant depression
    Gerard Sanacora
    Am J Psychiatry 161:2132. 2004
  58. ncbi Norepinephrine differentially modulates different types of respiratory pacemaker and nonpacemaker neurons
    Jean Charles Viemari
    Department of Organismal Biology and Anatomy, The University of Chicago, 1027 East 57th Street, Chicago, IL 60637, USA
    J Neurophysiol 95:2070-82. 2006
    ..b>Riluzole blocked the FM of isolated cadmium-insensitive pacemakers...
  59. ncbi Co-treatment with riluzole and GDNF is necessary for functional recovery after ventral root avulsion injury
    Astrid Bergerot
    Department of Anatomy and Developmental Biology, University College London, WC1 6BT London, UK
    Exp Neurol 187:359-66. 2004
    ..VRI) or intrathecal glial cell line-derived neurotrophic factor (GDNF) delivery or intraperitoneal injection of riluzole for 2 weeks ameliorates motoneuron death to 80% of control but combining the different treatment paradigms did ..
  60. pmc Delayed post-injury administration of riluzole is neuroprotective in a preclinical rodent model of cervical spinal cord injury
    Yongchao Wu
    Toronto Western Research Institute and Krembil Neuroscience Centre, University Health Network, University of Toronto, Toronto, Ontario, Canada
    J Neurotrauma 30:441-52. 2013
    b>Riluzole, a sodium/glutamate antagonist has shown promise as a neuroprotective agent. It is licensed for amyotrophic lateral sclerosis and is in clinical trial development for spinal cord injury (SCI)...
  61. pmc Electrophysiologic biomarkers for assessing disease progression and the effect of riluzole in SOD1 G93A ALS mice
    Jia Li
    Department of Neurology, Harvard Medical School, Beth Israel Deaconess Medical Center, Boston, Massachusetts, United States of America
    PLoS ONE 8:e65976. 2013
    To compare electrical impedance myography (EIM) 50 kHz phase to weight, motor score, paw grip endurance (PGE), CMAP amplitude, and MUNE for the identification of disease progression and the effect of riluzole in the SOD1 G93A mouse.
  62. pmc Riluzole and prognostic factors in amyotrophic lateral sclerosis long-term and short-term survival: a population-based study of 1149 cases in Taiwan
    Charles Tzu Chi Lee
    Department of Public Health, Kaohsiung Medical University, Kaohsiung, Taiwan
    J Epidemiol 23:35-40. 2013
    ..Amyotrophic lateral sclerosis (ALS) is a rare disease in Taiwan; thus, estimation of ALS mortality is difficult. We evaluated factors associated with ALS survival in Taiwan...
  63. pmc Riluzole-triggered GSH synthesis via activation of glutamate transporters to antagonize methylmercury-induced oxidative stress in rat cerebral cortex
    Yu Deng
    Department of Enviromental Health, School of Public Health, China Medical University, Liaoning, Shenyang 110001, China
    Oxid Med Cell Longev 2012:534705. 2012
    This study was to evaluate the effect of riluzole on methylmercury- (MeHg-) induced oxidative stress, through promotion of glutathione (GSH) synthesis by activating of glutamate transporters (GluTs) in rat cerebral cortex.
  64. ncbi Co-treatment with riluzole, a neuroprotective drug, ameliorates the 3-acetylpyridine-induced neurotoxicity in cerebellar Purkinje neurones of rats: behavioural and electrophysiological evidence
    Mahyar Janahmadi
    Neuroscience Research Center and Department of Physiology, Faculty of Medicine, Shahid Beheshti University Medical Campus, PO Box 19835 181, Evin, Tehran, Iran
    Neurotoxicology 30:393-402. 2009
    b>Riluzole has been shown to possess neuroprotective effects in a variety of neurological and animal model of diseases, including motor diseases...
  65. pmc Blockade of persistent sodium currents contributes to the riluzole-induced inhibition of spontaneous activity and oscillations in injured DRG neurons
    Rou Gang Xie
    Institute of Neuroscience, Xi Jing Hospital, The Fourth Military Medical University, Xi an, People s Republic of China
    PLoS ONE 6:e18681. 2011
    ..large-diameter fibers isolated from the compressed DRG in Sprague-Dawley rats, we show that local application of riluzole, which blocks the I(NaP), also inhibits the spontaneous activity of A-type DRG neurons in a dose-dependent manner...
  66. pmc Antidepressant-like properties of oral riluzole and utility of incentive disengagement models of depression in mice
    Shannon L Gourley
    Department of Psychiatry, Division of Molecular Psychiatry, Yale University, New Haven, CT 06511, USA
    Psychopharmacology (Berl) 219:805-14. 2012
    The neuroprotective agent riluzole has antidepressant-like properties in humans, but its mechanisms of action are unclear...
  67. ncbi The protective effect of riluzole on manganese caused disruption of glutamate-glutamine cycle in rats
    Yu Deng
    Department of Environmental Health, School of Public Health, China Medical University, Shenyang, 110001, People s Republic of China
    Brain Res 1289:106-17. 2009
    ..In addition, the effect of 21.35 micromol/kg riluzole (Na(+) channel blocker) was studied at 200 micromol/kg MnCl(2)...
  68. ncbi The effects of riluzole on neurological, brain biochemical, and histological changes in early and late term of sepsis in rats
    Hale Z Toklu
    Department of Pharmacology, Marmara University School of Pharmacy, Istanbul, Turkey
    J Surg Res 152:238-48. 2009
    ..b>Riluzole, a glutamate release inhibitor, has been shown to have neuroprotective effects in several animal models...
  69. ncbi Central administration of minocycline and riluzole prevents morphine-induced tolerance in rats
    Bohlool Habibi-asl
    Department of Pharmacology and Toxicology, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
    Anesth Analg 109:936-42. 2009
    ..In this study, we evaluated the effects of central administration of minocycline (a tetracycline derivative) and riluzole (an antiglutamatergic drug) on morphine-induced tolerance in rats.
  70. ncbi Riluzole-induced block of voltage-gated Na+ current and activation of BKCa channels in cultured differentiated human skeletal muscle cells
    Ya Jean Wang
    Institute of Basic Medical Sciences, National Cheng Kung University Medical College, Tainan, Taiwan
    Life Sci 82:11-20. 2008
    b>Riluzole is known to be of therapeutic use in the management of amyotrophic lateral sclerosis. In this study, we investigated the effects of riluzole on ion currents in cultured differentiated human skeletal muscle cells (dHSkMCs)...
  71. ncbi Toward more efficient clinical trials for amyotrophic lateral sclerosis
    Merit E Cudkowicz
    Massachusetts General Hospital, Boston, Massachusetts, USA
    Amyotroph Lateral Scler 11:259-65. 2010
    More than 30 phase II or III clinical trials have been carried out in amyotrophic lateral sclerosis (ALS). Only riluzole, however, has been shown to extend survival and/or time to tracheostomy...
  72. pmc Riluzole and D-amphetamine interactions in humans
    Mehmet Sofuoglu
    Yale University, School of Medicine, Department of Psychiatry and VA Connecticut Healthcare System, 950 Campbell Ave, Bldg 36 116A4, West Haven, CT 06516, United States
    Prog Neuropsychopharmacol Biol Psychiatry 32:16-22. 2008
    ..One such medication is riluzole, marketed for the treatment of Amyotrophic Lateral Sclerosis (ALS)...
  73. ncbi A study of the potential neuroprotective effect of riluzole on locomotor networks of the neonatal rat spinal cord in vitro damaged by excitotoxicity
    C Sámano
    Neuroscience Department, International School for Advanced Studies SISSA, Trieste, Italy
    Neuroscience 222:356-65. 2012
    ..05-0.1 mM) to produce limited excitotoxicity, the present study investigated whether riluzole, a drug inhibiting glutamate release and neuronal excitability, could prevent neuronal loss and protect locomotor ..
  74. pmc A pilot study of hippocampal volume and N-acetylaspartate (NAA) as response biomarkers in riluzole-treated patients with GAD
    Chadi G Abdallah
    Division of Neuropsychopharmacology, Department of Psychiatry, SUNY Downstate Medical Center, Brooklyn, NY, USA
    Eur Neuropsychopharmacol 23:276-84. 2013
    Anxiolytic benefit following chronic treatment with the glutamate modulating agent riluzole in patients with generalized anxiety disorder (GAD) was previously associated with differential changes in hippocampal NAA concentrations...
  75. ncbi Riluzole exerts central and peripheral modulating effects in amyotrophic lateral sclerosis
    Steve Vucic
    Neuroscience Research Australia, Barker Street, Randwick, Sydney, NSW 2031, Australia
    Brain 136:1361-70. 2013
    b>Riluzole, a benzothiazole derivative, has been shown to be effective in prolonging survival in amyotrophic lateral sclerosis...
  76. ncbi The effect of riluzole in amyotrophic lateral sclerosis: a study with cortical stimulation
    M T Desiato
    Clinica Neurologica, Dipartimento di Neuroscienze, Universita di Roma Tor Vergata, c o Ospedale S Eugenio, Piazzale dell Umanesimo, 00143, Roma, Italy
    J Neurol Sci 169:98-107. 1999
    ..sporadic amyotrophic lateral sclerosis (ALS) was selected for a prospective open study based on treatment with riluzole. A neurophysiological evaluation was performed by means of single and paired transcranial magnetic stimulation (..
  77. ncbi Riluzole suppresses experimental autoimmune encephalomyelitis: implications for the treatment of multiple sclerosis
    Yossi Gilgun-Sherki
    Laboratory of Neurosciences, Felsenstein Medical Research Center and Department of Neurology, Rabin Medical Center Beilinson Campus, The Sackler School of Medicine, Tel Aviv University, Petah Tikva 49100, Israel
    Brain Res 989:196-204. 2003
    ..Therefore, we examined whether riluzole, an inhibitor of glutamate transmission, affects the pathogenesis and clinical features of MS-like disease in ..
  78. ncbi Riluzole enhances glutamate uptake in rat astrocyte cultures
    Marcos Emilio dos Santos Frizzo
    Departamento de Bioquimica, Instituto de Ciencias Basicas da Saude, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil
    Cell Mol Neurobiol 24:123-8. 2004
    1. Riluzole is used for the treatment of amyotrophic lateral sclerosis and reported to have neuroprotective effects in animal models of Parkinson's disease, Huntington's disease, and brain ischemia...
  79. ncbi Interaction of the neuroprotective drug riluzole with GABA(A) and glycine receptor channels
    B Mohammadi
    Neurological Department, Medical School Hannover, Carl-Neuberg-Str. 1, 30625, Hannover, Germany
    Eur J Pharmacol 415:135-40. 2001
    b>Riluzole is used as therapeutic agent in amyotrophic lateral sclerosis...
  80. ncbi A riluzole- and valproate-sensitive persistent sodium current contributes to the resting membrane potential and increases the excitability of sympathetic neurones
    J Antonio Lamas
    Department of Functional Biology, Faculty of Biology, Section of Physiology, University of Vigo, Lagoas Marcosende, Vigo, Spain
    Pflugers Arch 458:589-99. 2009
    ..I(NaP) was inhibited by riluzole and valproate with an IC(50) of 2.7 and 3...
  81. ncbi The metabotropic glutamate receptor subtype 5 antagonist MPEP and the Na+ channel blocker riluzole show different neuroprotective profiles in reversing behavioral deficits induced by excitotoxic prefrontal cortex lesions
    C Risterucci
    Laboratoire de Neurobiologie de la Cognition, CNRS UMR 6155, Universite de Provence, Case C, 3 Place Victor Hugo, 13331 Marseille Cedex 3, France
    Neuroscience 137:211-20. 2006
    ..antagonist of metabotropic glutamate receptor subtype 5, and 2-amino-6-trifluoro methoxy-benzothiole (riluzole), a Na+ channel blocker exhibiting anti-glutamatergic properties, on the ibotenate-induced damage to the rat ..
  82. pmc Course of improvement in depressive symptoms to a single intravenous infusion of ketamine vs add-on riluzole: results from a 4-week, double-blind, placebo-controlled study
    Lobna Ibrahim
    Experimental Therapeutics and Pathophysiology Branch, Division of Intramural Research Programs, National Institute of Mental Health NIMH, National Institutes of Health NIH, Bethesda, MD, USA
    Neuropsychopharmacology 37:1526-33. 2012
    ..b>Riluzole, a glutamatergic modulator with antidepressant and synaptic plasticity-enhancing effects, could conceivably be ..
  83. ncbi Riluzole rapidly attenuates hyperemotional responses in olfactory bulbectomized rats, an animal model of depression
    Kou Takahashi
    Department of Neuropsychopharmacology, National Institute of Mental Health, National Center of Neurology and Psychiatry, 4 1 1 Ogawahigashimachi, Kodaira, Tokyo 187 8553, Japan
    Behav Brain Res 216:46-52. 2011
    ..b>Riluzole, a drug currently used to slow the progression of amyotrophic lateral sclerosis (ALS), directly affects the ..
  84. ncbi Plasma glutamate and glycine levels in patients with amyotrophic lateral sclerosis: the effect of riluzole treatment
    Elisabeth Andreadou
    Department of Neurology, Athens National University, Aeginition Hospital, 74, Vas Sophia s Ave, 11528 Athens, Greece
    Clin Neurol Neurosurg 110:222-6. 2008
    ..Moreover, glycine (gly) has been shown to potentiate excitatory transmission. The "antiglutamatergic" agent riluzole has been shown to prolong survival in ALS...
  85. ncbi Enhanced endogenous type I interferon cell-driven survival and inhibition of spontaneous apoptosis by Riluzole
    Ammar Achour
    Laboratoire des Interferons Sarcolectine, Universite Paris Descartes, Centre Universitaire des Saint Pères, 45 Rue des Saints Pères 75006 Paris, France
    Virology 386:160-7. 2009
    ..In this study, we investigated the action of Riluzole (2-amino-6-trifuromethoxybenzothiazole) in HIV-1 infection...
  86. ncbi A pilot trial of memantine and riluzole in ALS: correlation to CSF biomarkers
    Todd D Levine
    PNA Center for Neurologic Research, 5090 N 40th St, Phoenix, AZ 85018, USA
    Amyotroph Lateral Scler 11:514-9. 2010
    ..Twenty patients on stable doses of riluzole were enrolled. Patients received memantine, 10 mg b.i.d., for 18 months...
  87. pmc Riluzole protects against cardiac ischaemia and reperfusion damage via block of the persistent sodium current
    S Weiss
    The John Curtin School of Medical Research, The Australian National University, Canberra, ACT, Australia
    Br J Pharmacol 160:1072-82. 2010
    ..Here we propose a different approach, block of the persistent sodium current (INaP)...
  88. ncbi Riluzole therapy for motor neurone disease: an early Australian experience (1996-2002)
    Margie C Zoing
    Multidisciplinary Motor Neurone Disease Service, Institute of Neurological Sciences, Prince of Wales Hospital, Sydney, New South Wales, Australia
    J Clin Neurosci 13:78-83. 2006
    b>Riluzole is the only therapy proven in clinical trials to prolong survival in patients with motor neurone disease (MND)...
  89. pmc Rapid enhancement of glutamatergic neurotransmission in bipolar depression following treatment with riluzole
    Brian P Brennan
    Biological Psychiatry Laboratory, McLean Hospital, Belmont, MA 02478, USA
    Neuropsychopharmacology 35:834-46. 2010
    Glutamatergic abnormalities may underlie bipolar disorder (BD). The glutamate-modulating drug riluzole may be efficacious in bipolar depression, but few in vivo studies have examined its effect on glutamatergic neurotransmission...
  90. ncbi Maintenance of eupnea of in situ and in vivo rats following riluzole: a blocker of persistent sodium channels
    Walter M St-John
    Department of Physiology, Dartmouth Medical School, Dartmouth Hitchcock Medical Center, Borwell Bldg, Lebanon, NH 03756, USA
    Respir Physiol Neurobiol 155:97-100. 2007
    ..Regardless of the level of CO(2) drive, riluzole (1-10 microM), a blocker of persistent sodium channels, caused increases in the frequency and reductions in peak ..
  91. ncbi Brain-targeted solid lipid nanoparticles containing riluzole: preparation, characterization and biodistribution
    Maria Luisa Bondi
    Istituto per lo Studio dei Materiali Nanostrutturati, sez di Palermo, Consiglio Nazionale delle Ricerche, Via Ugo La Malfa 153, 90146 Palermo, Italy
    Nanomedicine (Lond) 5:25-32. 2010
    ..In this study nanoparticulate systems as drug carriers for riluzole, with sufficiently high loading capacity and small particle size, were prepared to a reach therapeutic drug level ..
  92. ncbi Effects of riluzole on the electrophysiological activity of pallidal neurons in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated monkey
    T Boraud
    Basal Gang, CNRS UMR 5543, Universite Victor Segalen Bordeaux 2, 146 rue Leo Saignat, 33076 Bordeaux, Cedex, France
    Neurosci Lett 281:75-8. 2000
    The effect of riluzole administration, an antiglutamatergic compound, on the electrophysiological activity of the pallidal complex of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys is compared with those induced by ..
  93. ncbi Neuroprotective effects of riluzole in early phase Parkinson's disease on clinically relevant parameters in the marmoset MPTP model
    Peternella S Verhave
    BU CBRN Protection, TNO Defence, Security and Safety, Lange Kleiweg 137, PO Box 45, 2280 AA Rijswijk, The Netherlands
    Neuropharmacology 62:1700-7. 2012
    ..The anti-glutamatergic compound riluzole is used as a model compound for neuroprotection...
  94. pmc Riluzole in psychiatry: a systematic review of the literature
    Carlos A Zarate
    Mark O Hatfield CRC, Bethesda, Maryland 20892, USA
    Expert Opin Drug Metab Toxicol 4:1223-34. 2008
    ..b>Riluzole, a neuroprotective agent with anticonvulsant properties approved for the treatment of amyotrophic lateral ..
  95. ncbi Protective effect of combination of sulforaphane and riluzole on glutamate-mediated excitotoxicity
    Geng Chang
    Department of Neurology, The Second Hospital of Hebei Medical University, Hebei, China
    Biol Pharm Bull 33:1477-83. 2010
    ..Some drugs, including sulforaphane (SF) and riluzole, can protect motor neuron against excitotoxicity...
  96. ncbi The use of the potassium channel activator riluzole to test whether potassium channels mediate the capacity of isoflurane to produce immobility
    Yilei Xing
    Department of Anesthesia and Perioperative Care, University of California, San Francisco 94110, USA
    Anesth Analg 97:1020-4, table of contents. 2003
    ..alveolar anesthetic concentration (MAC) during 4-h intrathecal or IV infusions of the nonspecific KCNK activator riluzole in 54 Sprague-Dawley rats...
  97. ncbi Riluzole (2-amino-6-trifluoromethoxy benzothiazole) attenuates MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) neurotoxicity in mice
    T Araki
    Department of Clinical Pharmacology and Therapeutics, Tohoku University Graduate School of Pharmaceutical Science and Medicine, Aoba yama, Sendai 980 8578, Japan
    Neurosci Lett 312:50-4. 2001
    The protective effects of 2-amino-6-trifluoromethoxy benzothiazole (riluzole), a Na(+) channel blocker with antiglutamatergic activity were investigated in the model of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced depletion ..
  98. ncbi Open-label riluzole in fragile X syndrome
    Craig A Erickson
    Department of Psychiatry, Indiana University School of Medicine, James Whitcomb Riley Hospital for Children, Indianapolis, IN 46202, USA
    Brain Res 1380:264-70. 2011
    Glutamatergic dysregulation is implicated in the pathophysiology of fragile X syndrome (FXS). Riluzole is hypothesized to have an inhibitory effect on glutamate release, block excitotoxic effects of glutamate, and potentiate postsynaptic ..
  99. pmc Riluzole pharmacokinetics in young patients with spinal muscular atrophy
    Chadi Abbara
    Universite d Angers, UFR Medecine, Angers Cedex, F 49045 CHU d Angers, Service Pharmacologie Toxicologie, Angers Cedex 09, France
    Br J Clin Pharmacol 71:403-10. 2011
    The objective of the present study was to assess the pharmacokinetics of riluzole in patients with spinal muscular atrophy (SMA).
  100. pmc Hippocampal N-acetylaspartate concentration and response to riluzole in generalized anxiety disorder
    Sanjay J Mathew
    Department of Psychiatry, Mount Sinai School of Medicine, New York, New York 10029, USA
    Biol Psychiatry 63:891-8. 2008
    ..spectroscopic imaging ((1)H MRSI) to examine the acute and chronic effects of the glutamate-release inhibitor riluzole on hippocampal N-acetylaspartate (NAA), a neuronal marker, in patients with generalized anxiety disorder (GAD) ..
  101. ncbi Effectiveness of riluzole in suppressing spasticity in the spinal cord injured rat
    Patrick H Kitzman
    Department of Rehabilitation Sciences, The University of Kentucky, Lexington, KY 40536 0200, USA
    Neurosci Lett 455:150-3. 2009
    ..The present study examined the effectiveness of riluzole, an agent that has been shown to reduce glutamate release, in managing spasticity within the tail musculature...

Research Grants62

  1. The Role of the Terminal Complement Pathway in ALS
    Scott R Barnum; Fiscal Year: 2013
    ..There is currently no prophylactic therapy or cure for ALS and the only approved treatment, riluzole, extends survival only a few months and is considered ineffective...
  2. Optimization of KCa2 Channel Activators as Neuroscience Tools and Potential Drugs
    Heike Wulff; Fiscal Year: 2012
    ..Using the neuroprotective drug riluzole as a synthetic template, our laboratory recently designed SKA-31 (EC50 2 uM), the first KCa2 channel activator, ..
  3. Role of TRP channels in secondary injury after brain trauma
    VLADIMIR GERZANICH; Fiscal Year: 2013
    ..potential: brief (24-hr) TRPM4 gene suppression using IV antisense oligodeoxynucleotide (AS-ODN), and riluzole, a pleiotropic FDA-approved drug that is a potent blocker of TRPM4 channels...
  4. A Phase II Trial of Riluzole in Patients with Advanced Melanoma
    James S Goydos; Fiscal Year: 2010
    ..A murine xenograft model of melanoma treated with Riluzole, an oral Grm1 blocking agent, showed decreased tumor growth in the treated mice compared to the untreated ..
  5. NIH ALS Conference: Clinical Research to Find the Pathogenesis and Cause of ALS
    Hiroshi Mitsumoto; Fiscal Year: 2011
    ..The single approved, available medication, Riluzole, only modestly slows disease progression...
  6. Riluzole Prodrugs for Melanoma and ALS
    ALLEN BERNARD REITZ; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): We have identified a novel Type IIb prodrug of riluzole, FC-311, which has the potential to revolutionize therapy for the treatment of the devastating condition of metastatic melanoma acting via a ..
  7. Phase 2 Study of Rasagiline for Treatment of Amyotrophic Lateral Sclerosis
    Yunxia Wang; Fiscal Year: 2012
    ..Despite multiple clinical trials and advances in understanding its pathogenesis riluzole, the only FDA approved ALS drug, has only a modest neuroprotective effect and carries a high financial burden to ..
  8. Involvement of astrocytic two-pore domain K+ channels in ischemic pathology
    Min Zhou; Fiscal Year: 2013
    ..of electrophysiological response of astrocytes to CIPNJFs by neuroprotectant and TREK-1 channel modulator riluzole and sipatrigine;3) Identify specific K2P-CIPNJF interaction mechanisms by selective silencing of astrocytic K2Ps ..
  9. Effects of Stress and Glutamatergic Agents on Glutamate Cycling and Behavior
    Gerard Sanacora; Fiscal Year: 2013
    ..b>Riluzole, an FDA-approved Glu-modulating agent used to delay ALS progression, exhibits anti-glutamatergic properties via ..
  10. Nanotechnology for Amyotrophic Lateral Sclerosis
    Kenneth Hensley; Fiscal Year: 2010
    ..SPECIFIC AIM 3 will test whether CeO2 nanoparticles interact with systemically administered riluzole to either improve or diminish murine clinical outcomes...
  11. Combination Therapy that Targets Glutamate Signaling in Melanoma
    James S Goydos; Fiscal Year: 2013
    ..Importantly, pharmacologic depletion of the GRM1 ligand, glutamate, with the glutamate antagonist Riluzole suppresses melanoma cell growth and increases apoptosis in vitro, and promotes apoptosis and reduces melanoma ..
  12. High throughput assay development for Huntington?s Disease
    RONALD B WETZEL; Fiscal Year: 2010
    ..One such compound, riluzole, failed to induce a response in human clinical trials, but then it also failed in a animal model preclinical ..
  13. Targeting Glutamate in OCD: A Placebo-Controlled, Double-Blind Augmentation Trial
    CHRISTOPHER JOHN PITTENGER; Fiscal Year: 2011
    ..glutamate in OCD: a placebo-controlled, double-blind augmentation trial of the glutamate-modulating agent riluzole in treatment-refractory OCD. Obsessive-compulsive disorder (OCD) affects approximately 2...
  14. 2/2-Novel Medication Strategies Targeting Brain Mechanisms in Pediatric OCD
    Dikoma C Shungu; Fiscal Year: 2013
    ..g., riluzole, memantine) reduce OCD severity when added to SRIs...
  15. 1/2-Novel Medication Strategies Targeting Brain Mechanisms in Pediatric OCD
    Helen Blair Simpson; Fiscal Year: 2013
    ..g., riluzole, memantine) reduce OCD severity when added to SRIs...
  16. 3/3-Efficacy and Tolerability of Riluzole in Treatment-Resistant Depression
    Maurizio Fava; Fiscal Year: 2013
    ..This collaborative R01 investigates the safety and efficacy of the glutamate-modulating and neuroprotective agent riluzole in a randomized double-blind placebo-controlled clinical trial (RCT) in patients with treatment- resistant ..
  17. Characterization of KIFAP3, a Modifier of Survival in Sporadic ALS
    John E Landers; Fiscal Year: 2013
    ..0 months, a substantial improvement (~42%) that surpasses the magnitude of benefit of the single drug (riluzole) that is FDA approved for ALS in ALS...
  18. Phase 2B Trial of Memantine for the Treatment of Amyotrophic Lateral Sclerosis
    TODD DYLAN LEVINE; Fiscal Year: 2013
    ..b>Riluzole the only FDA approved agent for ALS extends a patient's lifespan by 2-3 months, and there are no proven ..
  19. Mechanism and Treatment of Manganese Toxicity
    JEROME ALLAN ROTH; Fiscal Year: 2010
    ..Interestingly, there is a drug on the market, riluzole, currently approved for treatment of amyotrophic lateral sclerosis (ALS), which mechanistically behaves in this ..
  20. A Patient Oriented Research Program for Surgical Oncologists
    James S Goydos; Fiscal Year: 2013
    ..He has just completed accrual to a phase 0 trial of the glutamate signaling pathway inhibiting compound Riluzole in patients with resectable stage III and IV melanoma and the results are very encouraging. Dr...
  21. CLINICAL TRIALS FOR PEDIATRIC SPINAL MUSCULAR ATROPHY
    Susan Iannaccone; Fiscal Year: 2005
    ..The trials will be 6 month, open label using riluzole, albuterol and sodium 4-phenylbutyrate. All pediatric age groups from birth to 18 years will be included...
  22. Drug Discovery in ALS: Opportunities and Challenges
    Lucie Bruijn; Fiscal Year: 2012
    ..Despite tremendous efforts to halt the progression of the disease, Riluzole is the only drug on the market which prolongs the survival of patients by only 2-3 months...
  23. A New Approach to ALS
    Cassie S Mitchell; Fiscal Year: 2013
    ..quantitative framework of ALS using both the literature and clinical data analysis (aim 1);assess the effects of riluzole on in vivo electrophysiology (aim 2);and generating and quantitatively assessing combination treatment strategies ..
  24. A Phase 0 Trial of Riluzole in Patients with Resectable Stage III or IV Melanoma
    James Goydos; Fiscal Year: 2007
    ..Finally, a murine xenograft model of melanoma treated with Riluzole, an oral Grm1 blocking agent, showed decreased tumor growth in the treated mice compared to the untreated ..
  25. Novel Therapeutic Agents for ALS
    DONALD KIRSCH; Fiscal Year: 2007
    ..b>Riluzole is the sole drug currently approved for the treatment of ALS and only extends the survival of ALS patients by 2-3 ..
  26. SK Channel Openers as Therapeutics for Cerebellar Ataxia
    Heike Wulff; Fiscal Year: 2007
    ..b>Riluzole, a FDA approved drug for the therapy of amyotrophic lateral sclerosis, has been reported to be a potent SK ..
  27. RILUZOLE MOA: TARGETS FOR IMPROVED NEUROPROTECTIVE DRUGS
    Ann Sluder; Fiscal Year: 2004
    ..b>Riluzole, the only drug currently approved for the treatment of ALS, provides only a modest extension of 2 to 3 months in ..
  28. RISK FACTORS AND THERAPEUTIC STRATEGIES IN ALS
    Merit Cudkowicz; Fiscal Year: 2000
    ..will be followed by a phase II double-blind efficacy trial of Procysteine compared with the anti-glutamate agent Riluzole in 80 subjects with ALS...
  29. Synaptic and intrinsic exitability in motoneurons in a mouse model of ALS.
    KATHARINA ANN QUINLAN; Fiscal Year: 2010
    ..3 Ca2+ channels which produce the persistent inward current (PIC). Riluzole, the only FDA approved drug for ALS, works in two ways, blocking NaP, and decreasing presynaptic glutamate ..
  30. Synaptic & intrinsic motoneuron excitability in ALS excitotoxicity
    Jenna E Schuster; Fiscal Year: 2010
    ..Furthermore, the effect of Riluzole, the only FDA approved drug for ALS, on both intrinsic and synaptic motoneuron excitability will also be assessed...
  31. PROTON MRS STUDIES IN GENERALIZED ANXIETY DISORDER
    Sanjay Mathew; Fiscal Year: 2008
    ..A specific long-term goal is for the candidate to develop sufficient expertise in MRS to sustain valid and creative application to problems of GAD and related conditions. ..
  32. Southeastern Michigan Parkinson's Disease Program
    Peter LeWitt; Fiscal Year: 2006
    ..This application also discusses concepts for three pharmacological agents that could be investigated in pilot studies and, if promising, in multicenter clinical trials for assessing neuroprotection. ..
  33. Nocardia: A Novel Environmental Agent For Parkinsonism?
    Peter LeWitt; Fiscal Year: 2003
    ..These outcomes will be significant because they should add to our understanding of the neurodegenerative process in PD, and could lead to improved means of diagnosis and treatment for individuals with this disorder. ..
  34. MECHANISMS AND SITES OF VENTILATORY NEUROGENESIS
    WALTER ST JOHN; Fiscal Year: 2008
    ..Such information might provide insights into dysfunctions of the control of ventilation in humans, such as in "sleep apnea" or the "sudden infant death syndrome." [unreadable] [unreadable] [unreadable]..
  35. Phase III Trial of Minocycline in ALS-II Data Center
    Robert Miller; Fiscal Year: 2007
    ..The details of data management are described, including the methods for quality control, security and information technology. Finally, the analytic plan is described in full. ..
  36. QUANTITATIVE FUNCTION IN MOTOR NEURON DISEASE
    Eric Sorenson; Fiscal Year: 2004
    ..This will become increasingly important as our population ages, increasing demands for medical and social resources. ..
  37. IGF-I/ALS Trial
    Eric Sorenson; Fiscal Year: 2007
    ..Except for a very small minority of cases, the cause is unknown. The disease is incurable and only riluzole has proven to be effective in slowing the disease...
  38. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2004
    ..The results of this study will have profound public health implications by improving our understanding of the efficacy of SJW and standard antidepressants for the treatment of MinorD. ..
  39. CLINICAL TRIAL OF TOPIRAMATE IN ALS
    Merit Cudkowicz; Fiscal Year: 2003
    ..Secondary outcome measures include grip strength, forced vital capacity, the ALS functional rating scale, and the safety and tolerability of topiramate in this population. ..
  40. Metabolomic Signatures in ALS
    Merit Cudkowicz; Fiscal Year: 2005
    ..abstract_text> ..
  41. A Scientific Meeting of ALS Clinical Trials
    Hiroshi Mitsumoto; Fiscal Year: 2003
    ..Approved since 1996, Riluzole is the only drug available for ALS, but its benefit is limited...
  42. Substituted Amphetamines: NO-Dependent Mechanisms
    Yossef Itzhak; Fiscal Year: 2005
    ....
  43. Divalent Metal Transporter: Role in Manganese Toxicity
    JEROME ROTH; Fiscal Year: 2004
    ....
  44. BOSTON UNIVERSITY CRU FOR ALCOHOLISM TREATMENT
    Domenic Ciraulo; Fiscal Year: 2004
    ..However, each study site has provided site-specific information on the budget, budget justifications, listing of key personnel, consultant/consortium agreements, and human subjects sections of their respective proposals. ..
  45. Creatine Therapy for Huntington's Disease
    Steven Hersch; Fiscal Year: 2004
    ..These studies are intended to provide the basis of a subsequent phase III trial of creatine in HD. ..
  46. Neuropathic Pain Modulation by Cannabinoids
    Jianren Mao; Fiscal Year: 2006
    ..A better understanding of cannabinoid actions in neuropathic pain states could open a new avenue to developing novel pharmacological tools for the improved management of often intractable and debilitating neuropathic pain syndromes. ..
  47. Coenzyme Q10 in Huntington's Disease
    Merit Cudkowicz; Fiscal Year: 2007
    ..abstract_text> ..
  48. GABA Medications for Tobacco Addiction
    Mehmet Sofuoglu; Fiscal Year: 2009
    ..The findings of this study will provide valuable information to develop new pharmacotherapies for smoking cessation. ..
  49. OPIOID-INDUCED PAIN SENSITIVITY: CLINICAL DIAGNOSIS AND MANAGEMENT
    Jianren Mao; Fiscal Year: 2010
    ....
  50. Adolescent Exposure to Psychostimulants: Role of nNOS
    Yossef Itzhak; Fiscal Year: 2008
    ..Results of these studies would provide new information on mechanisms that underlie the development of hypersensitivity to these drugs from adolescence through adulthood. ..
  51. Cocaine Withdrawal and Pharmacotherapy Response
    Mehmet Sofuoglu; Fiscal Year: 2010
    ..This proposal, by testing the efficacy of carvedilol and investigating the influence of withdrawal severity on carvedilol's efficacy, may result in development of more effective treatments for cocaine addiction. ..
  52. Improving Outcomes in Pharmacotherapy of Social Phobia
    Mark Pollack; Fiscal Year: 2009
    ..It thus directly addresses a critical public health issue that adversely affects a substantial proportion of the population. ..
  53. Background sodium currents in respiratory pacemakers
    ANDREW TRYBA; Fiscal Year: 2009
    ..This research will lead to better understanding of the ionic mechanisms behind the generation of regular versus irregular rhythmic respiratory activity. ..
  54. Properties of Ion Channels that Control Secretion
    JOHN ENYEART; Fiscal Year: 2008
    ..abstract_text> ..
  55. 13C Measurement of GABA Synthesis in Depression
    Gerard Sanacora; Fiscal Year: 2009
    ..In addition, we will continue to investigate the potential association between cortical GABA concentrations and both the various clinical subtypes of depression and allelic variants of the GAD65 gene. ..
  56. IDENTIFICATION OF GENES THAT DELAY ALS ONSET
    Catherine Kunst; Fiscal Year: 2008
    ..have a modest 13 day increase in mean survival that is similar to the protection conferred by the ALS drug riluzole in similar transgenic lines...
  57. Coupling & Reconfiguration of Rhythmic Motor Networks
    Stephen Johnson; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  58. Impact of Trauma of Terroist Attack on Bipolar Patients
    Mark Pollack; Fiscal Year: 2003
    ..abstract_text> ..
  59. HUNTINGTON PROTEIN AND THE HUNTINGTON'S DISEASE MUTATION
    Steven Hersch; Fiscal Year: 2003
    ..In Specific Aim 4, we will examine apoptosis as a mechanism of cell death in transgenic HD animals by direct examination and by crossing tem with transgenic animal lines relevant to apoptotic death. ..
  60. Glutamate Uptake & the Pathogenesis of Neuropathic Pain
    Jianren Mao; Fiscal Year: 2007
    ..abstract_text> ..