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Tonabersat

Names

[ CAS No. ]:
175013-84-0

[ Name ]:
Tonabersat

[Synonym ]:
Tonabersat
Tonabersat [BAN,INN]
UNII-2XD9773ZMN
USL-260

Biological Activity

[Description]:

Tonabersat is a gap-junction modulator.

[Related Catalog]:

Signaling Pathways >> Cytoskeleton >> Gap Junction Protein
Research Areas >> Neurological Disease

[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].

[Animal admin]

Mice[2] Athymic NCR nu/nu mice, Cr:NIH bg-nu-xid mice, B6129SF1/J, C57BL/6J-Tmem173gt/J 'golden ticket', and C57/Bl/6J mice are used at 5-6 weeks of age. For inducible knockdown experiments, mice are given doxycycline hyclate in the drinking water (2 mg/mL) and the diet 14 days after injection of cancer cells. For drug treatment experiments, mice are intraperitoneally injected with Carboplatin (5 mg/kg per 5 days), Tonabersat (MedChem Express) (10 mg/kg per day), or meclofenamic acid sodium salt (20 mg/kg per day). Vehicle (10% DMSO in polyethylene glycol 400) is used in control mice. Quantification of tumour burden is by Bio-luminescent imaging (BLI), performed using an IVIS Spectrum Xenogen instrument and analysed using Living Image software v.2.50.

[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.


[Related Small Molecules]

GAP-134 (Hydrochloride) | GAP 27 acetate salt | GAP 26 trifluoroacetate salt

Chemical & Physical Properties

[ Density]:
1.38g/cm3

[ Boiling Point ]:
554.5ºC at 760 mmHg

[ Molecular Formula ]:
C20H19ClFNO4

[ Molecular Weight ]:
391.82100

[ Flash Point ]:
289.2ºC

[ Exact Mass ]:
391.09900

[ PSA ]:
75.63000

[ LogP ]:
4.07560

[ Vapour Pressure ]:
3.94E-13mmHg at 25°C

[ Index of Refraction ]:
1.612

[ Storage condition ]:
2-8℃

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H400

[ Precautionary Statements ]:
P273-P280-P305 + P351 + P338-P337 + P313-P391

[ RIDADR ]:
UN 3077 9 / PGIII

Related Compounds