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编 号：F277370
分子式：C17H18Br2FN3O3S
分子量：523.21
分子式：C17H18Br2FN3O3S
分子量：523.21
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CAS No: 219963-52-7
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生物活性：
SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats.
体内研究：
SB-357134 剂量依赖性地抑制特异性 [125I]SB-258585 结合。SB-357134（0.03–30 mg/kg；0-24 小时；口服；单剂量）在大鼠 MEST 模型中产生有效的剂量相关抗惊厥作用，最小显著有效剂量为 0.1 mg/kg 。SB-357134（10 mg/kg；口服；每天两次；7 天）长期给药与对照组和SB-357134 急性给药相比，显著缩短路径长度。Animal Model:Sprague–Dawley rats
Dosage:0.03–30 mg/kg
Administration:0-24 h; p.o.; 0.03–30 mg/kg
Result:Produced a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg. Increased seizure threshold up to 123±12% at the highest dose tested of 30 mg/kg. At 10 mg/kg, exhibited a rapid onset of action, significantly increasing seizure threshold from a control value of 21.7 to 26.7 mA at 1 h postdose. Observed Peak activity within 4–6 h postdose. With the exception of an unexplained loss of activity at 12 h, had a long duration of action of 21 h in this model.
Animal Model:Sprague–Dawley rats
Dosage:10 mg/kg
Administration:10 mg/kg; p.o.; twice daily; 7 days
Result:Significantly shortened path length when administered chronically compared to vehicle and administered acutely.
体外研究：
SB-357134（0.1、0.3、1 和 3 μM）浓度依赖性地抑制 5-HT 介导的 cAMP 水平升高，这在高 5-HT 浓度下是可以克服的，与竞争性拮抗作用一致。
SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats.
体内研究：
SB-357134 剂量依赖性地抑制特异性 [125I]SB-258585 结合。SB-357134（0.03–30 mg/kg；0-24 小时；口服；单剂量）在大鼠 MEST 模型中产生有效的剂量相关抗惊厥作用，最小显著有效剂量为 0.1 mg/kg 。SB-357134（10 mg/kg；口服；每天两次；7 天）长期给药与对照组和SB-357134 急性给药相比，显著缩短路径长度。Animal Model:Sprague–Dawley rats
Dosage:0.03–30 mg/kg
Administration:0-24 h; p.o.; 0.03–30 mg/kg
Result:Produced a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg. Increased seizure threshold up to 123±12% at the highest dose tested of 30 mg/kg. At 10 mg/kg, exhibited a rapid onset of action, significantly increasing seizure threshold from a control value of 21.7 to 26.7 mA at 1 h postdose. Observed Peak activity within 4–6 h postdose. With the exception of an unexplained loss of activity at 12 h, had a long duration of action of 21 h in this model.
Animal Model:Sprague–Dawley rats
Dosage:10 mg/kg
Administration:10 mg/kg; p.o.; twice daily; 7 days
Result:Significantly shortened path length when administered chronically compared to vehicle and administered acutely.
体外研究：
SB-357134（0.1、0.3、1 和 3 μM）浓度依赖性地抑制 5-HT 介导的 cAMP 水平升高，这在高 5-HT 浓度下是可以克服的，与竞争性拮抗作用一致。
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