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Chemical Compound Review

Distraneurin     5-(2-chloroethyl)-4-methyl- 1,3-thiazole

Synonyms: Somnevrin, Emineurina, Clometiazol, Clomethiazol, Clometiazole, ...
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Disease relevance of Clomethiazole


Psychiatry related information on Clomethiazole


High impact information on Clomethiazole


Chemical compound and disease context of Clomethiazole


Biological context of Clomethiazole


Anatomical context of Clomethiazole


Associations of Clomethiazole with other chemical compounds

  • 3. Administration of a single dose of chlormethiazole (100 mg kg-1) 20 min after the MDMA also provided complete protection to the hippocampus but not the cortex [26].
  • 1. The effect of chlormethiazole, and other drugs which potentiate gamma-aminobutyric acid (GABA) function on delayed neuronal death in the hippocampus has been examined in the gerbil [24].
  • 6. This conclusion was supported by the observation that the enhanced efflux of glutamate from slices of cerebral cortex which had been induced by incubation of the slices in an hypoxic medium was unaltered by the presence of a high concentration of chlormethiazole (1 mM) in the medium.(ABSTRACT TRUNCATED AT 250 WORDS)[25]
  • Injection of chlormethiazole (100 mg kg-1, i.p.) or dizocilpine (1 mg kg-1, i.p.) 5 min before and 55 min after the PCA failed to protect against the neurotoxicity, nor was protection afforded by chlormethiazole when a lower dose of PCA (2.5 mg kg-1, i.p.) was given which produced only a 30% loss of 5-HT content.(ABSTRACT TRUNCATED AT 250 WORDS)[26]
  • If muscimol, dizocilpine, or the adenosine A1 receptor agonist R-N6-phenylisopropyl-adenosine were administered together with chlormethiazole at their respective ED25 doses, a potentiation was apparent in the degree of neuroprotection [27].

Gene context of Clomethiazole

  • Anti-CYP2E1 reactivity showed positive correlation with the levels of hepatic CYP2E1 and was inhibited by the CYP2E1 transcriptional inhibitor chlormethiazole [28].
  • OBJECTIVE: To assess the safety of tissue-type plasminogen activator (t-PA) plus clomethiazole in patients with acute ischemic stroke and determine the feasibility of combination stroke therapy [29].
  • The Clomethiazole Acute Stroke Study in tissue-type plasminogen activator-treated stroke (CLASS-T): final results [29].
  • Here the authors suggested that chlormethiazole has anti-inflammatory properties because it potently and selectively inhibited p38 mitogen-activated protein (MAP) kinase in primary cortical glial cultures [30].
  • We investigated zonal differences of cytokine expression in rat liver and how these are affected by alcohol exposure and by chlormethiazole (CMZ), a transcriptional and posttranslational inhibitor of hepatic CYP2E1 [11].

Analytical, diagnostic and therapeutic context of Clomethiazole


  1. Results in 95 hemorrhagic stroke patients included in CLASS, a controlled trial of clomethiazole versus placebo in acute stroke patients. Wahlgren, N.G., Díez-Tejedor, E., Teitelbaum, J., Arboix, A., Leys, D., Ashwood, T., Grossman, E. Stroke (2000) [Pubmed]
  2. Clomethiazole (Zendra) in acute ischemic stroke: basic pharmacology and biochemistry and clinical efficacy. Green, A.R. Pharmacol. Ther. (1998) [Pubmed]
  3. Severe toxic hepatitis related to chlormethiazole. Gallardo-Caballero, E., Lucena, M.I., Andrade, R.J., Rodrigo, L., Pérez-Martínez, J., García-Ruiz, E. J. Hepatol. (2003) [Pubmed]
  4. Functional benefit from clomethiazole treatment after focal cerebral ischemia in a nonhuman primate species. Marshall, J.W., Cross, A.J., Ridley, R.M. Exp. Neurol. (1999) [Pubmed]
  5. Letter: Chlormethiazol and delirium tremens. Muller, C., Fadda, S. The American journal of psychiatry. (1975) [Pubmed]
  6. Physiological dependence on, and symptoms of withdrawal from, chlormethiazole. Reilly, T.M. The British journal of psychiatry : the journal of mental science. (1976) [Pubmed]
  7. The interaction of AR-A008055 and its enantiomers with the GABA(A) receptor complex and their sedative, muscle relaxant and anticonvulsant activity. Green, A.R., Hainsworth, A.H., Misra, A., Debens, T.A., Jackson, D.M., Murray, T.K., Nelson, R.M., Cross, A.J. Neuropharmacology (2001) [Pubmed]
  8. Clinical trial of the neuroprotectant clomethiazole in coronary artery bypass graft surgery: a randomized controlled trial. Kong, R.S., Butterworth, J., Aveling, W., Stump, D.A., Harrison, M.J., Hammon, J., Stygall, J., Rorie, K.D., Newman, S.P. Anesthesiology (2002) [Pubmed]
  9. Two-stage infusion of chlormethiazole for basal sedation. Seow, L.T., Roberts, J.G., Mather, L.E., Cousins, M.J. British journal of anaesthesia. (1981) [Pubmed]
  10. Induction of cytochrome P450 2E1 increases hepatotoxicity caused by Fas agonistic Jo2 antibody in mice. Wang, X., Lu, Y., Cederbaum, A.I. Hepatology (2005) [Pubmed]
  11. Zonated expression of cytokines in rat liver: effect of chronic ethanol and the cytochrome P450 2E1 inhibitor, chlormethiazole. Fang, C., Lindros, K.O., Badger, T.M., Ronis, M.J., Ingelman-Sundberg, M. Hepatology (1998) [Pubmed]
  12. Chlormethiazole inhibition of cytochrome P450 2E1 as assessed by chlorzoxazone hydroxylation in humans. Gebhardt, A.C., Lucas, D., Ménez, J.F., Seitz, H.K. Hepatology (1997) [Pubmed]
  13. Inhibition of ethanol-induced liver disease in the intragastric feeding rat model by chlormethiazole. Gouillon, Z., Lucas, D., Li, J., Hagbjork, A.L., French, B.A., Fu, P., Fang, C., Ingelman-Sundberg, M., Donohue, T.M., French, S.W. Proc. Soc. Exp. Biol. Med. (2000) [Pubmed]
  14. Review of the pharmacology and clinical pharmacology of 3,4-methylenedioxymethamphetamine (MDMA or "Ecstasy"). Green, A.R., Cross, A.J., Goodwin, G.M. Psychopharmacology (Berl.) (1995) [Pubmed]
  15. Diazepam and chlormethiazole attenuate the development of hyperthermia in an animal model of the serotonin syndrome. Nisijima, K., Shioda, K., Yoshino, T., Takano, K., Kato, S. Neurochem. Int. (2003) [Pubmed]
  16. Alcohol withdrawal: effects of clonidine treatment on sympathetic activity, the renin-aldosterone system, and clinical symptoms. Manhem, P., Nilsson, L.H., Moberg, A.L., Wadstein, J., Hökfelt, B. Alcohol. Clin. Exp. Res. (1985) [Pubmed]
  17. Successful treatment of alcohol withdrawal with trazodone. Borras, L., Timary, P., Constant, E.L., Huguelet, P., Eytan, A. Pharmacopsychiatry (2006) [Pubmed]
  18. Kinetics of chlormethiazole in patients with alcohol withdrawal manifestations. Jostell, K.G., Agurell, S., Hollister, L.E., Wermuth, B. Clin. Pharmacol. Ther. (1978) [Pubmed]
  19. Alcohol intoxication and hangover: modification of hangover by chlormethiazole. Myrsten, A.L., Rydberg, U., Ideström, C.M., Lamble, R. Psychopharmacology (Berl.) (1980) [Pubmed]
  20. Modeling drug- and system-related changes in body temperature: application to clomethiazole-induced hypothermia, long-lasting tolerance development, and circadian rhythm in rats. Visser, S.A., Sällström, B., Forsberg, T., Peletier, L.A., Gabrielsson, J. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  21. Chlormethiazole attenuates the derangement of sensory evoked potential (SEP) induced by ICV administration of NMDA. Thoren, P., Sjölander, M. Psychopharmacology (Berl.) (1993) [Pubmed]
  22. The protective action of chlormethiazole against ischaemia-induced neurodegeneration in gerbils when infused at doses having little sedative or anticonvulsant activity. Cross, A.J., Jones, J.A., Snares, M., Jostell, K.G., Bredberg, U., Green, A.R. Br. J. Pharmacol. (1995) [Pubmed]
  23. The effect of chlormethiazole on neuronal damage in a model of transient focal ischaemia. Sydserff, S.G., Cross, A.J., West, K.J., Green, A.R. Br. J. Pharmacol. (1995) [Pubmed]
  24. Neuroprotective activity of chlormethiazole following transient forebrain ischaemia in the gerbil. Cross, A.J., Jones, J.A., Baldwin, H.A., Green, A.R. Br. J. Pharmacol. (1991) [Pubmed]
  25. Attenuation by chlormethiazole administration of the rise in extracellular amino acids following focal ischaemia in the cerebral cortex of the rat. Baldwin, H.A., Williams, J.L., Snares, M., Ferreira, T., Cross, A.J., Green, A.R. Br. J. Pharmacol. (1994) [Pubmed]
  26. 5-HT loss in rat brain following 3,4-methylenedioxymethamphetamine (MDMA), p-chloroamphetamine and fenfluramine administration and effects of chlormethiazole and dizocilpine. Colado, M.I., Murray, T.K., Green, A.R. Br. J. Pharmacol. (1993) [Pubmed]
  27. The attenuation of kainate-induced neurotoxicity by chlormethiazole and its enhancement by dizocilpine, muscimol, and adenosine receptor agonists. MacGregor, D.G., Graham, D.I., Stone, T.W. Exp. Neurol. (1997) [Pubmed]
  28. Autoantibodies against cytochromes P-4502E1 and P-4503A in alcoholics. Lytton, S.D., Helander, A., Zhang-Gouillon, Z.Q., Stokkeland, K., Bordone, R., Aricò, S., Albano, E., French, S.W., Ingelman-Sundberg, M. Mol. Pharmacol. (1999) [Pubmed]
  29. The Clomethiazole Acute Stroke Study in tissue-type plasminogen activator-treated stroke (CLASS-T): final results. Lyden, P., Jacoby, M., Schim, J., Albers, G., Mazzeo, P., Ashwood, T., Nordlund, A., Odergren, T. Neurology (2001) [Pubmed]
  30. Neuroprotective agent chlomethiazole attenuates c-fos, c-jun, and AP-1 activation through inhibition of p38 MAP kinase. Simi, A., Ingelman-Sundberg, M., Tindberg, N. J. Cereb. Blood Flow Metab. (2000) [Pubmed]
  31. Status dystonicus: the syndrome and its management. Manji, H., Howard, R.S., Miller, D.H., Hirsch, N.P., Carr, L., Bhatia, K., Quinn, N., Marsden, C.D., Bahtia, K. Brain (1998) [Pubmed]
  32. Effect of starvation and chlormethiazole on cytochrome P450s of rat nasal mucosa. Longo, V., Ingelman-Sundberg, M., Amato, G., Salvetti, A., Gervasi, P.G. Biochem. Pharmacol. (2000) [Pubmed]
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