|3-氨基-2-(4-氯苯基)丙烷-1-磺酸|CsnPharm

CAS No.: 125464-42-8

Synonyms: N/A

Saclofen is a selective antagonist of GABAB receptors.

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400-920-2911

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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].

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技术信息

CAS号	125464-42-8	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C9H12ClNO3S	运输	蓝冰
分子量	249.71	别名	N/A

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