Saclofen
产品说明书
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同义名 : | - |
| CAS号 : | 125464-42-8 | |
| 货号 : | A281714 | |
| 分子式 : | C9H12ClNO3S | |
| 纯度 : | 98% | |
| 分子量 : | 249.71 | |
| MDL号 : | MFCD00216817 | |
| 存储条件： |
Pure form Sealed in dry, room temperature 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 | Saclofen (the direct sulphonic analogue of baclofen) is a competitive antagonist of baclofen at GABAB receptors in guinea pig ileum and rat cortical slices (estimated pA2 = 5.3), at least twice as potent as 2-hydroxy-saclofen (pA2 = 5)[1]. 2-hydroxy-saclofen (2-OH-S), a sulphonic analogue of baclofen, slightly increased the twitch height and reversibly antagonised the GABA- and baclofen-induced depression of twitch contractions in the guinea pig vas deferens and isolated ileum, causing a parallel dextral shift in the baclofen dose-response curve in a competitive manner (pA2 = 5.0) in the latter tissue. 2-OH-S (10-50 mM) reversibly elevated the spike height and antagonised the baclofen (8-20 mM)-induced suppression of ictal discharges in rat cortical slices superfused in Mg2+-free Krebs solution, the spike height declining to control level within 15 min of washout[2]. Baclofen (2-hydroxy-saclofen) (0.5-20 mM) reduces the amplitude of excitatory postsynaptic potentials (EPSPs) recorded from hippocampal CA1 pyramidal neurons. In the presence of 200-500 mM 2-OH-S, the synaptic depressant action of baclofen is significantly reduced[3]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
4.00mL 0.80mL 0.40mL |
20.02mL 4.00mL 2.00mL |
40.05mL 8.01mL 4.00mL |
| 参考文献 |
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