生物活性

• 描述Ethosuximide, 2-ethyl-2-methylsuccinimide, has been used extensively for "petit mal" seizures. Commonly observed side effects of ethosuximide are dose dependent and involve the gastrointestinal tract and central nervous system. The spontaneous pacemaker oscillatory activity of thalamocortical circuitry involves low threshold T-type Ca2+ currents in the thalamus, and ethosuximide is presumed to reduce these low threshold T-type Ca2+ currents in thalamic neurons. Ethosuximide also decreases the persistent Na+ and Ca2+ -activated K+ currents in thalamic and layer V cortical pyramidal neurons^[3]. Ethosuximide and valproic acid are more effective than lamotrigine in the treatment of childhood absence epilepsy. Ethosuximide is associated with fewer adverse attentional effects^[4]. Concentrations of 2 μM or more of Ethosuximide not only are found to be less effective than 1 μM concentration of Ethosuximide, but also induce cell toxicity. The number and percentage of tubulin β-III immunopositive neurons were increased after 6 days treatment with ethosuximide. Ethosuximide may compensate damage caused by seizure attacks and possibly other neuronal loss disorders^[5]. Ethosuximide given with drinking water (300 mg/kg/day) over 45 days slightly reduced proneness to audiogenic epilepsy and increased locomotor activity of the animals at the periphery of the open field^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02205931	Epilepsy	Phase 4	Recruiting	June 2019	United Kingdom ... more >> Birmingham Children's Hospital Recruiting Birmingham, United Kingdom, B4 6NH Contact: Shakti Agrawal, MBBS    0044 1213338149    shakti.agrawal@bch.nhs.uk    Principal Investigator: Shakti Agrawal, MBBS          Bristol Royal Hospital for Children Recruiting Bristol, United Kingdom, BS2 8AE Contact: Andrew Mallick, FRCPCH          Principal Investigator: Andrew Mallick          Addenbrooke's Hospital Recruiting Cambridge, United Kingdom, CB2 0QQ Contact: Alasdair Parker, MA    0044 1223 245151    alasdair.parker@addenbrookes.nhs.uk    Principal Investigator: Alasdair Parker, MA          Lancashire Teaching Hospitals NHS Foundation Trust Recruiting Lancashire, United Kingdom Contact: Helen Basu       Helen.Basu@lthtr.nhs.uk    Principal Investigator: Helen Basu          Leeds Teaching Hospital Recruiting Leeds, United Kingdom, LS1 3EX Contact: Helen McCullagh, RCPCH    0044 113 243 2799    h.mccullagh@nhs.net    Principal Investigator: Helen McCullagh, RCPCH          Alder Hey Children's Hospital Recruiting Liverpool, United Kingdom, L12 2AP Contact: Rachel Kneen, BMBS    0044 151 2525163    rachel.kneen@liverpool.ac.uk    Principal Investigator: Rachel Kneen, BMBS          Great Ormond Street Hospital Recruiting London, United Kingdom, WC1N 3JH Contact: Christin Eltze, MD Res    0044 207 405 9200 ext 5438    christin.eltze@gosh.nhs.uk    Principal Investigator: Christin Eltze, MD Res          St George's University Hospitals NHS Foundation Trust Recruiting London, United Kingdom Contact: Penny Fallon       Penny.Fallon@stgeorges.nhs.uk    Principal Investigator: Penny Fallon          Royal Manchester Children's Hospital Recruiting Manchester, United Kingdom, M13 0JE Contact: Tim Martland, RCPCH    0044 161 276 1234    timothy.martland@cmft.nhs.uk    Principal Investigator: Tim Martland, RCPCH          The Newcastle Upon Tyne Hospitals NHS Foundation Trust Recruiting Newcastle upon Tyne, United Kingdom Contact: Anita Devlin       Anita.Devlin@nuth.nhs.uk    Principal Investigator: Anita Devlin          Sheffield Children's NHS Foundation Trust Recruiting Sheffield, United Kingdom Contact: Archana Desurkar       Archana.Desurkar@sch.nhs.uk    Principal Investigator: Archana Desurkar Collapse <<
  NCT01390909	-	-	Completed	-	-
  NCT01390909	-	-	Completed	-	-

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• 参考文献

• [1] Chen X, McCue HV, et al. Ethosuximide ameliorates neurodegenerative disease phenotypes by modulating DAF-16/FOXO target gene expression. Mol Neurodegener. 2015 Sep 29;10:51.

  [2] Collins JJ, Evason K, et al. The anticonvulsant ethosuximide disrupts sensory function to extend C. elegans lifespan. PLoS Genet. 2008 Oct;4(10):e1000230.

  [3] Gören MZ, Onat F. Ethosuximide: from bench to bedside. CNS Drug Rev. 2007 Summer;13(2):224-39

  [4] Glauser TA, Cnaan A, Shinnar S, Hirtz DG, Dlugos D, Masur D, Clark PO, Capparelli EV, Adamson PC; Childhood Absence Epilepsy Study Group. Ethosuximide, valproic acid, and lamotrigine in childhood absence epilepsy. N Engl J Med. 2010 Mar 4;362(9):790-9

  [5] Sondossi K, Majdzadeh M, Ghaeli P, Ghahremani MH, Shafaroodi H, Paknejad B, Ostad SN. Analysis of the antiepileptic, ethosuximide impacts on neurogenesis of rat forebrain stem cells. Fundam Clin Pharmacol. 2014 Oct;28(5):512-8

  [6] Fedotova IB, Perepelkina OV, Nikolaev GM, Surina NM, Poletaeva II. Effect of Ethosuximide on Audiogenic Epilepsy in Krushinsky-Molodkina Rats. Bull Exp Biol Med. 2019 Aug;167(4):464-466

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