An anti-migraine agent; binds to connexin43 hemichannels and inhibits ATP release in vitro during injury and reperfusion in a dose-dependent manner; blocks trigeminal ganglion neuronal-satellite glial cell signaling and cortical spreading depression; in vivo (10 mg/kg) increases the seizure threshold in MEST mice and rats (143 and 1192%

Tonabersat – 5 mg

Brand:
Cayman
CAS:
175013-84-0
Storage:
-20
UN-No:
Non-Hazardous - /

Tonabersat is an anti-migraine agent.{40037,40034} It binds to connexin43 hemichannels and inhibits ATP release in vitro during injury and reperfusion in a dose-dependent manner.{40033} This inhibition blocks trigeminal ganglion neuronal-satellite glial cell signaling and cortical spreading depression, a trigger of migraine pain.{40033,40034,40035} In vivo, tonabersat (10 mg/kg) increases the seizure threshold in maximal electroshock seizure threshold (MEST) mice and rats (143 and 1192%, respectively) and completely blocks neurogenic plasma extravasation, a marker of migraine pain, in a rat trigeminal nerve migraine model.{40036} Formulations containing tonabersat are in clinical trials for acute treatment of migraine.{40037}  

 

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Description

An anti-migraine agent; binds to connexin43 hemichannels and inhibits ATP release in vitro during injury and reperfusion in a dose-dependent manner; blocks trigeminal ganglion neuronal-satellite glial cell signaling and cortical spreading depression; in vivo (10 mg/kg) increases the seizure threshold in MEST mice and rats (143 and 1192%, respectively); blocks neurogenic plasma extravasation in a rat trigeminal nerve migraine model,

Formal name: N-[(3S,4S)-6-acetyl-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-4-yl]-3-chloro-4-fluoro-benzamide

Synonyms:  SB-220453

Molecular weight: 391.8

CAS: 175013-84-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Neuroscience|Pain Research

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