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

5-HT7R antagonist 2 (compound 4h) 是一种 5-HT7R 拮抗剂，在 G 蛋白和 β-阻滞蛋白信号通路中起拮抗作用，对 5-HT7R 的 Ki 为 67 nM，在 cAMP 和 Tango 试验中的 IC50 值分别为 2.59 μM、39.57 μM。5-HT7R antagonist 2 对神经发生有影响，可减少自闭症谱系障碍 (ASD) 相关的重复行为，恢复 ASD 受损的神经发生。

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5-HT7R antagonist 2 Chemical Structure

5-HT7R antagonist 2 Chemical Structure

CAS No. : 1448808-50-1

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5-HT7R antagonist 2 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment[1].
Pharmacokinetic Analysis ICR Male Mice[1]

药代动力学分析[1]

Plasma Intravenous Administration Intraperitoneal Administration
Tmax (h) 0.08 0.25
T1/2 (h) 0.77 1.06
Cmax (ng/mL) 33.07 156.44
AUClast (ng·h/mL) 28.31 143.27
CL (L/h/kg) 41.61 -
Vss (L/kg) 32.43 -
MRT (h) 0.79 0.93
F (%) 50.60

IC50 & Target

5-HT7 Receptor

67 nM (Ki)

体外研究
(In Vitro)

5-HT7R antagonist 2 (compound 4h) (microsomes, 30 分钟) 具有显著的代谢稳定性，对细胞无毒性[1]。
5-HT7R antagonist 2 在 G 蛋白和 β-阻滞蛋白信号通路中都是一种竞争性拮抗剂[1]。

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

5-HT7R antagonist 2 相关抗体:

Cell Line:
Concentration:
Incubation Time:
Result:

Cell Line:
Concentration:
Incubation Time:
Result:
体内研究
(In Vivo)

5-HT7R antagonist (compound 4h) （腹腔内注射，5 mg/kg，30 分钟）在 ASD 动物模型中具有调节 ASD 重复行为的潜力，能增加 ASD 未成熟神经元的数量[1]。

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

Animal Model: ASD animal models
Dosage: 5 mg/kg
Administration: Intraperitoneal injection
Result: 4h can increase the number of immature ASD neurons
分子量

252.31

Formula

C16H16N2O
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 2 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

5-HT7R antagonist 21448808-50-15-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorASDShank3 TG miceself-groomingInhibitorinhibitorinhibit

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