2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB357134

SB-357134 是一种具有高效选择性、脑渗透以及口服活性的 5-HT6 受体拮抗剂。SB-357134 可增强大鼠的记忆力和学习能力并增加癫痫发作阈值。

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SB357134 Chemical Structure

SB357134 Chemical Structure

CAS No. : 219963-52-7

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SB357134 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

体外研究
(In Vitro)

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[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SB357134 相关抗体:
体内研究
(In Vivo)

SB-357134 剂量依赖性地抑制特异性 [125I]SB-258585 结合[1]。
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 [1]。
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[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague–Dawley rats[1]
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[1]
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.
分子量

523.21

Formula

C17H18Br2FN3O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SB357134 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB357134219963-52-7SB 357134SB-3571345-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorRatbrain penetrant5-HT6 receptorInhibitorinhibitorinhibit

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产品名称：
SB357134
目录号：
HY-119061
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