Loreclezole
产品说明书
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同义名 : | R 72063 |
| CAS号 : | 117857-45-1 | |
| 货号 : | A1001459 | |
| 分子式 : | C10H6Cl3N3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 274.53 | |
| MDL号 : | MFCD00865331 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors. When applied to GABARs that contained a beta2 or beta3 subunit subtype， loreclezole potentiated the peak current evoked by sub-maximal concentrations of GABA. Loreclezole also increased the rate and degree of apparent desensitization of GABAR whole-cell currents, an effect that was independent of the beta subunit subtype, suggesting that potentiation and inhibition of GABAR current by loreclezole occurred through separate sites[1]. Loreclezole (10, 25, 50 or 75 mg/kg, i.p. 60 min before measurement of seizure threshold ) results in a dose-dependent rise in seizure threshold as measured by the dose of pentylenetetrazol required to produce a convulsion 60 min later[2]. Loreclezole (5 mg/kg) exerted a significant protective action against amygdala-kindled rats, reducing both seizure and afterdischarge (AD) durations. Also, the concomitant treatment of loreclezole (2.5 mg/kg) with clonazepam (0.05 mg/kg) resulted in a significant decrease of seizure and afterdischarge durations[3]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.64mL 0.73mL 0.36mL |
18.21mL 3.64mL 1.82mL |
36.43mL 7.29mL 3.64mL |
| 参考文献 |
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