2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. 5-HT7R antagonist 3

5-HT7R antagonist 3 (Compound 6.4) 是一种选择性的 5-HT7R 拮抗剂，Ki为 8 nM，而针对D2R、5-HT1AR、5-HT2AR 的 Ki 分别为 511 nM、8930 nM 和 5786 nM。 5-HT7R antagonist 3 在小鼠中具有抗抑郁和焦虑活性。

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5-HT7R antagonist 3 Chemical Structure

5-HT7R antagonist 3 Chemical Structure

CAS No. : 1887043-58-4

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5-HT7R antagonist 3 相关抗体

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5-HT7R antagonist 3 (Compound 6.4) is a selective 5-HT7R antagonist (Ki: 8 nM), with Ki of 511 nM (D2), 8930 nM (5-HT1A) and 5786 nM (5-HT2A), respectively. 5-HT7R antagonist 3 possesses antidepressant and anxiolytic effects in mice[1].

IC50 & Target[1]

5-HT7 Receptor

8 nM (Ki)

5-HT1A Receptor

8930 nM (Ki)

5-HT2A Receptor

5786 nM (Ki)

D2 Receptor

511 nM (Ki)

体外研究
(In Vitro)

5-HT7R antagonist 3 (1 pM-1 μM) 可抑制稳定表达人 5-HT 的细胞中 cAMP 产生，其IC50 为 113 nM，Kb 为 14 nM[1]。

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

5-HT7R antagonist 3 相关抗体:
体内研究
(In Vivo)

5-HT7R antagonist 3 (1.25-10 mg/kg，腹腔注射，测试前 60 min) 在雄性 BalbC 小鼠 (20-25 g) 中发挥显著的抗焦虑和抗抑郁作用[1]。

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

Animal Model: Male BalbC mice weighing 20-25 g[1]
Dosage: 0, 0.63, 1.25, 2.5, 5, 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Showed significant antidepressant effects in forced swim test (FST) at a dose of 2.5 mg/kg, reducing immobility time by 29%.
Showed anxiolytic activity in four-plate test (FPT) at doses of 1.25, 2.5 and 10 mg/kg.
Reduced spontaneous locomotion during the 60-minute observation period.
分子量

516.61

Formula

C30H33FN4O3
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

5-HT7R antagonist 3 相关分类

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  • 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:

5-HT7R antagonist 31887043-58-45-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorDepressionAnxiolyticcAMPCHO cellsBalbCFSTInhibitorinhibitorinhibit

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