13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
標簽:Tonabersat
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 5mg 10mg 50mg |
| CAS | 175013-84-0 |
| 別名 | SB-220453;SB 220453;SB220453 |
| 化學名 | 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 |
產品描述：
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].
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原創作者：上海莼試生物技術有限公司
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賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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