"目录号: HY-15204
Cytoskeleton-
Tonabersat 是一种gap-junction调节剂。
Gap Junction Protein
相关产品
GAP-134 Hydrochloride-Gap 27-
生物活性
Description
Tonabersat is agap-junctionmodulator.
IC50& Target
Gap-junction[1]
In Vitro
Tonabersat, a novel benzopyran derivative, inhibits cortical spreading depression (CSD) and therefore might be able to inhibit the early migraine mechanisms[1].
In Vivo
Treatment with either Tonabersat (10 mg/kg) or Meclofenamate (20 mg/kg) as single agents significantly inhibit progression of metastatic lesions. Addition of carboplatin to either agent profoundly inhibits brain metastasis[2].
Clinical Trial
NCT00311662
Minster Research Ltd
Migraine Without Aura-Migraine With Aura
April 2006
Phase 2
NCT00534560
Minster Research Ltd
Migraine Without Aura-Migraine With Aura
October 2007
Phase 2
NCT00332007
Minster Research Ltd-University of Copenhagen
Migraine With Aura
May 2006
Phase 2
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References
[1].Silberstein SD, et al. Tonabersat, a gap-junction modulator: efficacy and safety in two randomized, placebo-controlled, dose-ranging studies of acute migraine. Cephalalgia. 2009 Nov;29 Suppl 2:17-27.
[2].Chen Q, et al. Carcinoma-astrocyte gap junctions promote brain metastasis by cGAMP transfer. Nature. 2016 May 18;533(7604):493-8.
[3].Kim Y, et al. Tonabersat Prevents Inflammatory Damage in the Central Nervous System by Blocking Connexin43 Hemichannels. Neurotherapeutics. 2017 May 30.