MEK162

"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

View MoreCollapse

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.