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. Cifra A, Nani F, Nistri A. Riluzole is a potent drug to protect neonatal rat hypoglossal motoneurons in vitro from excitotoxicity due to glutamate uptake block. Eur J Neurosci. 2011;33:899-913 pubmed publisher
    ..b>Riluzole is the only drug licensed for symptomatic ALS treatment and is proposed to delay disease progression...
  2. Miles G, Dai Y, Brownstone R. Mechanisms underlying the early phase of spike frequency adaptation in mouse spinal motoneurones. J Physiol. 2005;566:519-32 pubmed
    ..iberiotoxin), voltage-activated Ca2+ channels (CdCl2), M-current (linopirdine) and persistent Na+ currents (riluzole) are all unnecessary for SFA...
  3. Weiss S, Benoist D, White E, Teng W, Saint D. Riluzole protects against cardiac ischaemia and reperfusion damage via block of the persistent sodium current. Br J Pharmacol. 2010;160:1072-82 pubmed publisher
    ..hearts from adult rats, subjected to 30 min global ischaemia and reperfusion with vehicle only (control) or riluzole (1-10 microM) in the perfusate...
  4. Li J, Sung M, Rutkove S. Electrophysiologic biomarkers for assessing disease progression and the effect of riluzole in SOD1 G93A ALS mice. PLoS ONE. 2013;8:e65976 pubmed publisher
    ..grip endurance (PGE), CMAP amplitude, and MUNE for the identification of disease progression and the effect of riluzole in the SOD1 G93A mouse...
  5. Lamanauskas N, Nistri A. Riluzole blocks persistent Na+ and Ca2+ currents and modulates release of glutamate via presynaptic NMDA receptors on neonatal rat hypoglossal motoneurons in vitro. Eur J Neurosci. 2008;27:2501-14 pubmed publisher
    The neuroprotective agent riluzole is used for the symptomatic treatment of motoneuron disease, which strongly affects the brainstem nucleus hypoglossus...
  6. Wang J, Dib M, Lenoir M, Vago P, Eybalin M, Hameg A, et al. Riluzole rescues cochlear sensory cells from acoustic trauma in the guinea-pig. Neuroscience. 2002;111:635-48 pubmed
    ..Whatever the mechanisms, a common feature of noise damage to hair cells was mitochondrial alteration. Riluzole (2-amino-6-trifluoromethoxy benzothiazole) is a neuroprotective agent that prevents apoptosis- and necrosis-..
  7. Meininger V, Asselain B, Guillet P, Leigh P, Ludolph A, Lacomblez L, et al. Pentoxifylline in ALS: a double-blind, randomized, multicenter, placebo-controlled trial. Neurology. 2006;66:88-92 pubmed
    ..and safety of pentoxifylline, a US Food and Drug Administration-approved drug, in patients with ALS treated with riluzole. The authors conducted a double-blind, randomized, placebo-controlled, multicenter trial...
  8. Ishiyama T, Okada R, Nishibe H, Mitsumoto H, Nakayama C. Riluzole slows the progression of neuromuscular dysfunction in the wobbler mouse motor neuron disease. Brain Res. 2004;1019:226-36 pubmed
    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)...
  9. Bensimon G, Lacomblez L, Delumeau J, Bejuit R, Truffinet P, Meininger V. A study of riluzole in the treatment of advanced stage or elderly patients with amyotrophic lateral sclerosis. J Neurol. 2002;249:609-15 pubmed
    Treatment with the neuroprotective drug riluzole has previously been shown to increase the probability of survival in patients with amyotrophic lateral sclerosis...

More Information

Publications88

  1. Kitzman P. Effectiveness of riluzole in suppressing spasticity in the spinal cord injured rat. Neurosci Lett. 2009;455:150-3 pubmed publisher
    ..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...
  2. Sámano C, Nasrabady S, Nistri A. A study of the potential neuroprotective effect of riluzole on locomotor networks of the neonatal rat spinal cord in vitro damaged by excitotoxicity. Neuroscience. 2012;222:356-65 pubmed publisher
    ..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 ..
  3. Vucic S, Lin C, Cheah B, Murray J, Menon P, Krishnan A, et al. Riluzole exerts central and peripheral modulating effects in amyotrophic lateral sclerosis. Brain. 2013;136:1361-70 pubmed publisher
    b>Riluzole, a benzothiazole derivative, has been shown to be effective in prolonging survival in amyotrophic lateral sclerosis...
  4. Tripathi V, Al Chalabi A. Molecular insights and therapeutic targets in amyotrophic lateral sclerosis. CNS Neurol Disord Drug Targets. 2008;7:11-9 pubmed
    ..The causes of ALS are largely unknown, but the only disease-modifying therapy, riluzole, was designed based on one hypothesis of disease causation, the excitotoxic hypothesis...
  5. Del Signore S, Amante D, Kim J, Stack E, Goodrich S, Cormier K, et al. Combined riluzole and sodium phenylbutyrate therapy in transgenic amyotrophic lateral sclerosis mice. Amyotroph Lateral Scler. 2009;10:85-94 pubmed publisher
    ..Since many patients are already on riluzole, it is important to ensure that any proposed therapy does not result in negative synergy with riluzole...
  6. Cheah B, Vucic S, Krishnan A, Kiernan M. Riluzole, neuroprotection and amyotrophic lateral sclerosis. Curr Med Chem. 2010;17:1942-199 pubmed
    ..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...
  7. Namkoong J, Shin S, Lee H, MARIN Y, Wall B, Goydos J, et al. Metabotropic glutamate receptor 1 and glutamate signaling in human melanoma. Cancer Res. 2007;67:2298-305 pubmed
    ..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...
  8. Akamatsu K, Shibata M, Ito Y, Sohma Y, Azuma H, Otsuki Y. Riluzole induces apoptotic cell death in human prostate cancer cells via endoplasmic reticulum stress. Anticancer Res. 2009;29:2195-204 pubmed
    ..The effects of riluzole, an ion channel modulator, on cell proliferation, apoptosis and the apoptotic pathway in the LNCaP and C4-2 ..
  9. Chang G, Guo Y, Jia Y, Duan W, Li B, Yu J, et al. Protective effect of combination of sulforaphane and riluzole on glutamate-mediated excitotoxicity. Biol Pharm Bull. 2010;33:1477-83 pubmed
    ..Some drugs, including sulforaphane (SF) and riluzole, can protect motor neuron against excitotoxicity...
  10. Owen R. Glutamatergic approaches in major depressive disorder: focus on ketamine, memantine and riluzole. Drugs Today (Barc). 2012;48:469-78 pubmed publisher
    ..Trials with memantine and riluzole, agents with actions broadly similar to and different from ketamine on the glutamatergic system, are also ..
  11. Landwehrmeyer G, Dubois B, de Yebenes J, Kremer B, Gaus W, Kraus P, et al. Riluzole in Huntington's disease: a 3-year, randomized controlled study. Ann Neurol. 2007;62:262-72 pubmed
    We conducted a randomized double-blind trial of riluzole in Huntington's disease to investigate the efficacy of this antiexcitotoxic drug in slowing disease progression...
  12. Diguet E, Fernagut P, Scherfler C, Wenning G, Tison F. Effects of riluzole on combined MPTP + 3-nitropropionic acid-induced mild to moderate striatonigral degeneration in mice. J Neural Transm (Vienna). 2005;112:613-31 pubmed
    We investigated the potency of riluzole, an anti-glutamatergic drug, to affect ongoing neuronal death process following combined MPTP + 3-nitropropionic acid (3-NP) intoxication producing combined striatal and nigral degeneration (SND) in ..
  13. Speyer C, Smith J, Banda M, Devries J, Mekani T, Gorski D. Metabotropic glutamate receptor-1: a potential therapeutic target for the treatment of breast cancer. Breast Cancer Res Treat. 2012;132:565-73 pubmed publisher
    ..mGluR1 inhibitors (Riluzole or BAY36-7620) inhibited the proliferation of triple negative breast cancer cells in a time- and dose-dependent ..
  14. Yip D, Le M, Chan J, Lee J, Mehnert J, Yudd A, et al. A phase 0 trial of riluzole in patients with resectable stage III and IV melanoma. Clin Cancer Res. 2009;15:3896-902 pubmed publisher
    ..Furthermore, a xenograft model of melanoma treated with riluzole, an oral GRM1 blocking agent, showed decreased tumor growth compared with the untreated controls...
  15. Verhave P, Jongsma M, van den Berg R, Vanwersch R, Smit A, Philippens I. Neuroprotective effects of riluzole in early phase Parkinson's disease on clinically relevant parameters in the marmoset MPTP model. Neuropharmacology. 2012;62:1700-7 pubmed publisher
    ..The anti-glutamatergic compound riluzole is used as a model compound for neuroprotection...
  16. Carbone M, Duty S, Rattray M. Riluzole elevates GLT-1 activity and levels in striatal astrocytes. Neurochem Int. 2012;60:31-8 pubmed publisher
    ..The neuroprotective compound riluzole (100 ?M) upregulated GLT-1 levels and activity, through a mechanism that was not dependent on blockade of voltage-..
  17. Cadaveira Mosquera A, Ribeiro S, Reboreda A, Pérez M, Lamas J. Activation of TREK currents by the neuroprotective agent riluzole in mouse sympathetic neurons. J Neurosci. 2011;31:1375-85 pubmed publisher
    ..Whole-cell experiments revealed a riluzole-activated current (I(RIL)), transported by potassium, in mouse superior cervical ganglion (mSCG) neurons...
  18. Khan A, Wall B, Ahlawat S, Green C, Schiff D, Mehnert J, et al. Riluzole enhances ionizing radiation-induced cytotoxicity in human melanoma cells that ectopically express metabotropic glutamate receptor 1 in vitro and in vivo. Clin Cancer Res. 2011;17:1807-14 pubmed publisher
    ..human GRM1 (hGRM1) expressing melanoma cells release excess extracellular glutamate and are growth inhibited by riluzole, an inhibitor of glutamate release...
  19. Erickson C, Weng N, Weiler I, Greenough W, Stigler K, Wink L, et al. Open-label riluzole in fragile X syndrome. Brain Res. 2011;1380:264-70 pubmed publisher
    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 ..
  20. Gourley S, Espitia J, Sanacora G, Taylor J. Antidepressant-like properties of oral riluzole and utility of incentive disengagement models of depression in mice. Psychopharmacology (Berl). 2012;219:805-14 pubmed publisher
    The neuroprotective agent riluzole has antidepressant-like properties in humans, but its mechanisms of action are unclear...
  21. Deng Y, Xu Z, Liu W, Xu B, Yang H, Wei Y. Riluzole-triggered GSH synthesis via activation of glutamate transporters to antagonize methylmercury-induced oxidative stress in rat cerebral cortex. Oxid Med Cell Longev. 2012;2012:534705 pubmed publisher
    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...
  22. Andreadou E, Kapaki E, Kokotis P, Paraskevas G, Katsaros N, Libitaki G, et al. Plasma glutamate and glycine levels in patients with amyotrophic lateral sclerosis: the effect of riluzole treatment. Clin Neurol Neurosurg. 2008;110:222-6 pubmed
    ..The "antiglutamatergic" agent riluzole has been shown to prolong survival in ALS...
  23. Pittenger C, Coric V, Banasr M, Bloch M, Krystal J, Sanacora G. Riluzole in the treatment of mood and anxiety disorders. CNS Drugs. 2008;22:761-86 pubmed
    ..b>Riluzole, which is approved and marketed for the treatment of amyotrophic lateral sclerosis, is thought to be ..
  24. Wu N, Enomoto A, Tanaka S, Hsiao C, Nykamp D, Izhikevich E, et al. Persistent sodium currents in mesencephalic v neurons participate in burst generation and control of membrane excitability. J Neurophysiol. 2005;93:2710-22 pubmed
    ..04 s, tau(recov) = 2.21 s). Riluzole (< or =5 microM) substantially reduced I(NaP), membrane resonance, postinhibitory rebound (PIR), and ..
  25. Weng Y, Kriz J. Differential neuroprotective effects of a minocycline-based drug cocktail in transient and permanent focal cerebral ischemia. Exp Neurol. 2007;204:433-42 pubmed
    ..It consists of minocycline--an antibiotic with anti-inflammatory properties, riluzole--a glutamate antagonist, and nimodipine--a blocker of voltage-gated calcium channels...
  26. Hockly E, Tse J, Barker A, Moolman D, Beunard J, Revington A, et al. Evaluation of the benzothiazole aggregation inhibitors riluzole and PGL-135 as therapeutics for Huntington's disease. Neurobiol Dis. 2006;21:228-36 pubmed
    ..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 ..
  27. Shortland P, Leinster V, White W, Robson L. Riluzole promotes cell survival and neurite outgrowth in rat sensory neurones in vitro. Eur J Neurosci. 2006;24:3343-53 pubmed
    This study explored the effects of riluzole administration on cell survival and neurite growth in adult and neonatal rat dorsal root ganglion (DRG) neurones in vitro...
  28. McDonnell M, Vera M, Blass B, Pelletier J, King R, Fernandez Metzler C, et al. Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling. Bioorg Med Chem. 2012;20:5642-8 pubmed publisher
    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...
  29. Desaphy J, Carbonara R, Costanza T, Lentini G, Cavalluzzi M, Bruno C, et al. Molecular dissection of lubeluzole use-dependent block of voltage-gated sodium channels discloses new therapeutic potentials. Mol Pharmacol. 2013;83:406-15 pubmed publisher
    ..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)] ..
  30. Coderre T, Kumar N, Lefebvre C, Yu J. A comparison of the glutamate release inhibition and anti-allodynic effects of gabapentin, lamotrigine, and riluzole in a model of neuropathic pain. J Neurochem. 2007;100:1289-99 pubmed
    The effects of treatment with the anti-convulsant agents, lamotrigine and riluzole were compared with gabapentin in a rat experimental model of neuropathic pain...
  31. Pena F, Parkis M, Tryba A, Ramirez J. Differential contribution of pacemaker properties to the generation of respiratory rhythms during normoxia and hypoxia. Neuron. 2004;43:105-17 pubmed
    ..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. ..
  32. Dunlop J, Beal McIlvain H, She Y, Howland D. Impaired spinal cord glutamate transport capacity and reduced sensitivity to riluzole in a transgenic superoxide dismutase mutant rat model of amyotrophic lateral sclerosis. J Neurosci. 2003;23:1688-96 pubmed
    ..b>Riluzole, a neuroprotective agent used clinically to slow the progression of ALS, produced an enhancement of spinal cord ..
  33. Haddad H, Cifuentes Diaz C, Miroglio A, Roblot N, Joshi V, Melki J. Riluzole attenuates spinal muscular atrophy disease progression in a mouse model. Muscle Nerve. 2003;28:432-7 pubmed
    ..To test whether riluzole, which exhibits neurotrophic properties, might have a protective role in SMA, mutant mice were treated with it ..
  34. Irifune M, Kikuchi N, Saida T, Takarada T, Shimizu Y, Endo C, et al. Riluzole, a glutamate release inhibitor, induces loss of righting reflex, antinociception, and immobility in response to noxious stimulation in mice. Anesth Analg. 2007;104:1415-21, table of contents pubmed
    ..b>Riluzole (2-amino-6-[trifluoromethoxy]benzothiazole) is a neuroprotective drug that inhibits glutamate release from nerve ..
  35. Wu Y, Satkunendrarajah K, Teng Y, Chow D, Buttigieg J, Fehlings M. Delayed post-injury administration of riluzole is neuroprotective in a preclinical rodent model of cervical spinal cord injury. J Neurotrauma. 2013;30:441-52 pubmed publisher
    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)...
  36. Scherfler C, Sather T, Diguet E, Stefanova N, Puschban Z, Tison F, et al. Riluzole improves motor deficits and attenuates loss of striatal neurons in a sequential double lesion rat model of striatonigral degeneration (parkinson variant of multiple system atrophy). J Neural Transm (Vienna). 2005;112:1025-33 pubmed
    We investigated neuroprotective effects of riluzole, an anti-glutamatergic agent that is FDA approved for disease-modifying therapy in amyotrophic lateral sclerosis (ALS), in an established double lesion rat model of striatonigral ..
  37. Deng Y, Xu Z, Xu B, Tian Y, Xin X, Deng X, et al. The protective effect of riluzole on manganese caused disruption of glutamate-glutamine cycle in rats. Brain Res. 2009;1289:106-17 pubmed publisher
    ..In addition, the effect of 21.35 micromol/kg riluzole (Na(+) channel blocker) was studied at 200 micromol/kg MnCl(2)...
  38. Milane A, Tortolano L, Fernandez C, Bensimon G, Meininger V, Farinotti R. Brain and plasma riluzole pharmacokinetics: effect of minocycline combination. J Pharm Pharm Sci. 2009;12:209-17 pubmed
    ..The only drug approved is riluzole. Minocycline is an antibiotic with numerous neuroprotective properties...
  39. Zarate C, Manji H. Riluzole in psychiatry: a systematic review of the literature. Expert Opin Drug Metab Toxicol. 2008;4:1223-34 pubmed publisher
    ..b>Riluzole, a neuroprotective agent with anticonvulsant properties approved for the treatment of amyotrophic lateral ..
  40. McDermott C, Shaw P. Diagnosis and management of motor neurone disease. BMJ. 2008;336:658-62 pubmed publisher
  41. Abbara C, Estournet B, Lacomblez L, Lelièvre B, Ouslimani A, Lehmann B, et al. Riluzole pharmacokinetics in young patients with spinal muscular atrophy. Br J Clin Pharmacol. 2011;71:403-10 pubmed publisher
    The objective of the present study was to assess the pharmacokinetics of riluzole in patients with spinal muscular atrophy (SMA). Fourteen patients were enrolled in an open-label, nonrandomized and repeat-dose pharmacokinetic study...
  42. Bergerot A, Shortland P, Anand P, Hunt S, Carlstedt T. Co-treatment with riluzole and GDNF is necessary for functional recovery after ventral root avulsion injury. Exp Neurol. 2004;187:359-66 pubmed
    ..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 ..
  43. Lacomblez L, Bensimon G, Leigh P, Debove C, Bejuit R, Truffinet P, et al. Long-term safety of riluzole in amyotrophic lateral sclerosis. Amyotroph Lateral Scler Other Motor Neuron Disord. 2002;3:23-9 pubmed
    This international, open-label, multicentre extension of riluzole pivotal studies was designed to assess the long-term safety of riluzole in the treatment of amyotrophic lateral sclerosis (ALS)...
  44. Coric V, Taskiran S, Pittenger C, Wasylink S, Mathalon D, Valentine G, et al. Riluzole augmentation in treatment-resistant obsessive-compulsive disorder: an open-label trial. Biol Psychiatry. 2005;58:424-8 pubmed
    ..We investigated the efficacy of augmentation therapy with riluzole, a glutamate-modulating agent, in treatment-resistant OCD...
  45. Bensimon G, Doble A. The tolerability of riluzole in the treatment of patients with amyotrophic lateral sclerosis. Expert Opin Drug Saf. 2004;3:525-34 pubmed
    b>Riluzole is the only disease-modifying drug approved for the treatment of amyotrophic lateral sclerosis (ALS), in which it has been demonstrated to extend survival...
  46. Mazzone G, Nistri A. Delayed neuroprotection by riluzole against excitotoxic damage evoked by kainate on rat organotypic spinal cord cultures. Neuroscience. 2011;190:318-27 pubmed publisher
    ..Using such cultures, the putative neuroprotective agent riluzole applied at 5 ?M (plasma therapeutic concentration) was studied for its ability to prevent neurotoxicity evoked by ..
  47. Cudkowicz M, Katz J, Moore D, O NEILL G, Glass J, Mitsumoto H, et al. Toward more efficient clinical trials for amyotrophic lateral sclerosis. Amyotroph Lateral Scler. 2010;11:259-65 pubmed publisher
    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...
  48. Risterucci C, Coccurello R, Banasr M, Stutzmann J, Amalric M, Nieoullon A. 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. Neuroscience. 2006;137:211-20 pubmed
    ..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 ..
  49. Zoccolella S, Beghi E, Palagano G, Fraddosio A, Guerra V, Samarelli V, et al. Riluzole and amyotrophic lateral sclerosis survival: a population-based study in southern Italy. Eur J Neurol. 2007;14:262-8 pubmed
    b>Riluzole is to date the only treatment that prolongs amyotrophic lateral sclerosis (ALS) survival...
  50. Xing Y, Zhang Y, Stabernack C, Eger E, Gray A. The use of the potassium channel activator riluzole to test whether potassium channels mediate the capacity of isoflurane to produce immobility. Anesth Analg. 2003;97:1020-4, table of contents pubmed
    ..alveolar anesthetic concentration (MAC) during 4-h intrathecal or IV infusions of the nonspecific KCNK activator riluzole in 54 Sprague-Dawley rats...
  51. Albo F, Pieri M, Zona C. Modulation of AMPA receptors in spinal motor neurons by the neuroprotective agent riluzole. J Neurosci Res. 2004;78:200-7 pubmed
    We investigated the interaction of riluzole, a therapeutic agent used in amyotrophic lateral sclerosis (ALS), with alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor channels in mouse spinal motor neurons in culture ..
  52. Zoing M, Burke D, Pamphlett R, Kiernan M. Riluzole therapy for motor neurone disease: an early Australian experience (1996-2002). J Clin Neurosci. 2006;13:78-83 pubmed
    b>Riluzole is the only therapy proven in clinical trials to prolong survival in patients with motor neurone disease (MND)...
  53. ST JOHN W, Waki H, Dutschmann M, Paton J. Maintenance of eupnea of in situ and in vivo rats following riluzole: a blocker of persistent sodium channels. Respir Physiol Neurobiol. 2007;155:97-100 pubmed
    ..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 ..
  54. Le M, Chan J, Rosenberg S, Nabatian A, Merrigan K, Cohen Solal K, et al. The glutamate release inhibitor Riluzole decreases migration, invasion, and proliferation of melanoma cells. J Invest Dermatol. 2010;130:2240-9 pubmed publisher
    ..Using the glutamate-release inhibitor Riluzole or the non-competitive GRM1 antagonist BAY 36-7620 we were able to induce considerable inhibition of colony ..
  55. Lamas J, Romero M, Reboreda A, Sánchez E, Ribeiro S. A riluzole- and valproate-sensitive persistent sodium current contributes to the resting membrane potential and increases the excitability of sympathetic neurones. Pflugers Arch. 2009;458:589-99 pubmed publisher
    ..I(NaP) was inhibited by riluzole and valproate with an IC(50) of 2.7 and 3...
  56. Pambo Pambo A, Durand J, Gueritaud J. Early excitability changes in lumbar motoneurons of transgenic SOD1G85R and SOD1G(93A-Low) mice. J Neurophysiol. 2009;102:3627-42 pubmed publisher
  57. Russman B, Iannaccone S, Samaha F. A phase 1 trial of riluzole in spinal muscular atrophy. Arch Neurol. 2003;60:1601-3 pubmed
    ..b>Riluzole, a glutamate inhibitor, has been shown to slow the rate of decline in patients with amyotrophic lateral sclerosis,..
  58. Bellingham M. A review of the neural mechanisms of action and clinical efficiency of riluzole in treating amyotrophic lateral sclerosis: what have we learned in the last decade?. CNS Neurosci Ther. 2011;17:4-31 pubmed publisher
    ..b>Riluzole has been used as the only approved treatment for amyotrophic lateral sclerosis since 1995, but its mechanism(s) ..
  59. Reboreda A, Sánchez E, Romero M, Lamas J. Intrinsic spontaneous activity and subthreshold oscillations in neurones of the rat dorsal column nuclei in culture. J Physiol. 2003;551:191-205 pubmed
    ..The frequency of LTOs was voltage dependent and could be abolished by TTX (0.5 microM) and riluzole (30 microM), suggesting the participation of a sodium current...
  60. Ates O, Cayli S, Gurses I, Turkoz Y, Tarim O, Cakir C, et al. Comparative neuroprotective effect of sodium channel blockers after experimental spinal cord injury. J Clin Neurosci. 2007;14:658-65 pubmed
    ..study was to compare the neuroprotective effect of three sodium channel blockers-mexiletine, phenytoin and riluzole--after SCI...
  61. Abdallah C, Coplan J, Jackowski A, Sato J, Mao X, Shungu D, et al. A pilot study of hippocampal volume and N-acetylaspartate (NAA) as response biomarkers in riluzole-treated patients with GAD. Eur Neuropsychopharmacol. 2013;23:276-84 pubmed publisher
    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...
  62. Waibel S, Reuter A, Malessa S, Blaugrund E, Ludolph A. Rasagiline alone and in combination with riluzole prolongs survival in an ALS mouse model. J Neurol. 2004;251:1080-4 pubmed
    ..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)...
  63. Banasr M, Chowdhury G, Terwilliger R, Newton S, Duman R, Behar K, et al. Glial pathology in an animal model of depression: reversal of stress-induced cellular, metabolic and behavioral deficits by the glutamate-modulating drug riluzole. Mol Psychiatry. 2010;15:501-11 pubmed publisher
    ..Furthermore, we analyzed the effects of riluzole, a Food and Drug Administration-approved drug for the treatment of amyotrophic laterosclerosis, known to modulate ..
  64. Grant P, Lougee L, Hirschtritt M, Swedo S. An open-label trial of riluzole, a glutamate antagonist, in children with treatment-resistant obsessive-compulsive disorder. J Child Adolesc Psychopharmacol. 2007;17:761-7 pubmed publisher
    Obsessive-compulsive disorder (OCD) in childhood is often refractory to treatment. Riluzole, a glutamate antagonist, has theoretical support as an alternative pharmacological treatment and has demonstrated possible benefit in some open-..
  65. Braz C, Borges V, Ferraz H. Effect of riluzole on dyskinesia and duration of the on state in Parkinson disease patients: a double-blind, placebo-controlled pilot study. Clin Neuropharmacol. 2004;27:25-9 pubmed
    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...
  66. Meininger V. Clinical trials in ALS: what did we learn from recent trials in humans?. Neurodegener Dis. 2005;2:208-14 pubmed
    ..This review suggests that in these trials there is a discrepancy between drug effects on survival versus function. These results suggest that a reappraisal of strategies to identify therapeutic targets for ALS is required. ..
  67. Sofuoglu M, Waters A, Mooney M, Kosten T. Riluzole and D-amphetamine interactions in humans. Prog Neuropsychopharmacol Biol Psychiatry. 2008;32:16-22 pubmed
    ..One such medication is riluzole, marketed for the treatment of Amyotrophic Lateral Sclerosis (ALS)...
  68. Stevenson A, Yates D, Manser C, De Vos K, Vagnoni A, Leigh P, et al. Riluzole protects against glutamate-induced slowing of neurofilament axonal transport. Neurosci Lett. 2009;454:161-4 pubmed publisher
    b>Riluzole is the only drug approved for the treatment of amyotrophic lateral sclerosis (ALS) but its precise mode of action is not properly understood...
  69. Simard J, Tsymbalyuk O, Keledjian K, Ivanov A, Ivanova S, Gerzanich V. Comparative effects of glibenclamide and riluzole in a rat model of severe cervical spinal cord injury. Exp Neurol. 2012;233:566-74 pubmed publisher
    Both glibenclamide and riluzole reduce necrosis and improve outcome in rat models of spinal cord injury (SCI)...
  70. Spadoni F, Hainsworth A, Mercuri N, Caputi L, Martella G, Lavaroni F, et al. Lamotrigine derivatives and riluzole inhibit INa,P in cortical neurons. Neuroreport. 2002;13:1167-70 pubmed
    ..Two lamotrigine derivatives (sipatrigine and 202W92) and riluzole inhibited the persistent sodium current at low, therapeutic concentrations...
  71. Fumagalli E, Bigini P, Barbera S, De Paola M, Mennini T. Riluzole, unlike the AMPA antagonist RPR119990, reduces motor impairment and partially prevents motoneuron death in the wobbler mouse, a model of neurodegenerative disease. Exp Neurol. 2006;198:114-28 pubmed
    ..We carried out two parallel studies in wobbler mice, comparing the anti-glutamatergic drug riluzole and the AMPA receptor antagonist RPR119990...
  72. Liu B, Ferreira R, Lively S, Schlichter L. Microglial SK3 and SK4 currents and activation state are modulated by the neuroprotective drug, riluzole. J Neuroimmune Pharmacol. 2013;8:227-37 pubmed publisher
    ..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...
  73. Fumagalli E, Funicello M, Rauen T, Gobbi M, Mennini T. Riluzole enhances the activity of glutamate transporters GLAST, GLT1 and EAAC1. Eur J Pharmacol. 2008;578:171-6 pubmed
    b>Riluzole exerts a neuroprotective effect through different mechanisms, including action on glutamatergic transmission...
  74. Sanacora G, Kendell S, Fenton L, Coric V, Krystal J. Riluzole augmentation for treatment-resistant depression. Am J Psychiatry. 2004;161:2132 pubmed
  75. Jankovic J, Hunter C. A double-blind, placebo-controlled and longitudinal study of riluzole in early Parkinson's disease. Parkinsonism Relat Disord. 2002;8:271-6 pubmed
    ..Patients in early stages of PD, not previously treated with levodopa, were randomized to receive riluzole 50mg capsules orally, taken twice daily or a matching placebo...
  76. Viemari J, Ramirez J. Norepinephrine differentially modulates different types of respiratory pacemaker and nonpacemaker neurons. J Neurophysiol. 2006;95:2070-82 pubmed
    ..b>Riluzole blocked the FM of isolated cadmium-insensitive pacemakers...
  77. Aggarwal S, Zinman L, Simpson E, McKinley J, Jackson K, Pinto H, et al. Safety and efficacy of lithium in combination with riluzole for treatment of amyotrophic lateral sclerosis: a randomised, double-blind, placebo-controlled trial. Lancet Neurol. 2010;9:481-8 pubmed publisher
    ..aimed to confirm or disprove these findings by assessing the safety and efficacy of lithium in combination with riluzole in patients with ALS. We did a double-blind, placebo-controlled trial with a time-to-event design...
  78. Squitieri F, Orobello S, Cannella M, Martino T, Romanelli P, Giovacchini G, et al. Riluzole protects Huntington disease patients from brain glucose hypometabolism and grey matter volume loss and increases production of neurotrophins. Eur J Nucl Med Mol Imaging. 2009;36:1113-20 pubmed publisher
    ..b>Riluzole interferes with glutamatergic neurotransmission, thereby reducing excitotoxicity, enhancing neurite formation in ..
  79. Kononenko N, Shao L, Dudek F. Riluzole-sensitive slowly inactivating sodium current in rat suprachiasmatic nucleus neurons. J Neurophysiol. 2004;91:710-8 pubmed
    ..Tetrodotoxin (TTX; 1 microM) completely and reversibly blocked I(Na,S). Riluzole, an effective blocker of I(Na,P), inhibited reversibly I(Na,S) with an EC(50) of 1-2 microM...