產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg
CAS	175013-84-0
別名	SB-220453;SB 220453;SB220453
化學(xué)名	N-[(3S,4S)-6-acetyl-3-hydroxy-2,2-dimethyl-3,4-dihydrochromen-4-yl]-3-chloro-4-fluorobenzamide
分子式	C20H19ClFNO4
分子量	391.82
溶解度	DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml,Ethanol: 20 mg/ml
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Migraine is a common, recurrent and primary headache disorder. Optimisation of novel cis- and trans-4-(substituted-anfido)benzopyran-3-ol derivatives has led to the identification of Tonabersat (SB-220453) with potential antimigraine activity.

In vitro: Topiramate targets multiple cortical and subcortical loci, altering voltage-gated ion channels and chemical transmission to decrease abnormal brain excitability. Preclinical studies have identified four properties that may account for the drug’s efficacy in epilepsy and migraine prophylaxis: (i) blockage of voltage-dependent sodium channels; (ii) augmentation of the activity of the neurotransmitter g-aminobutyric acid (GABA) at some subtypes of the GABA-A receptor; (iii) antagonism of the AMPA/kainate subtype of the glutamate receptor; and (iv) inhibition of the carbonic anhydrase enzymes, particularly isozymes II and IV [1].

In vivo: Tonabersat binds selectively to a unique site in the brain. Moreover, tonabersat could markedly reduce cortical spreading depression (CSD) and CSD-associated events and inhibite gap-junction communication between neurons and satellite glial cells in the trigeminal ganglion. Together, these findings indicate that tonabersat should have clinical application in preventing migraine attacks [2].

Clinical trial: Tonabersat showed a preventive eff ect on attacks of migraine aura but no efficacy on non-aura attacks, in keeping with its known inhibitory eff ect on CSD. The results support the theory that auras are caused by CSD and that this phenomenon is not involved in attacks without aura [3].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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