1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Dopamine Receptor
  3. Antipsychotic agent-2

Antipsychotic agent-2 (Compound 11) 是一种有效的抗精神病剂。Antipsychotic agent-2 对 5-HT1A5-HT2A5-HT2CD2 和 H1 受体具有亲和力,Ki 分别为 56.6、66.7、552、596 和 1140 nM。Antipsychotic agent-2 可以透过血脑屏障。

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Antipsychotic agent-2 Chemical Structure

Antipsychotic agent-2 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1 receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability[1].

IC50 & Target

5-HT1A Receptor

160 nM (EC50)

5-HT2A Receptor

96.4 nM (Kb)

D2 Receptor

45.7 nM (Kb)

体外研究
(In Vitro)

Antipsychotic agent-2 (Compound 11) 拮抗 10-6 M 多巴胺在稳定表达人 D2 受体的 CHO-K1 细胞中抑制 Forskolin (HY-15371) 刺激的 cAMP 产生,这表明了对 D2 的拮抗作用 (Kb=45.7 nM)[1]
Antipsychotic agent-2 在浓度依赖的方式下抑制在稳定表达 5-HT1A 受体的 HEK293 细胞中由 Forskolin 刺激的 cAMP 产生,这表明了对 5-HT1A 的激动剂活性 (EC50=160 nM),而它表现为 5-HT2A 拮抗剂,对抗 10-6 M 5-HT 在表达 5-HT2A 受体的 CHO-K1 细胞中刺激的肌醇磷酸产生 (Kb=96.4 nM)[1]
Antipsychotic agent-2 (0.1-10 μM) 是一种相对低效的 CYP3A4 诱导剂[1]
Antipsychotic agent-2 (0.3-30 μM; 72 h) 表现出良好的安全性,并且只在 30 μM 的浓度下显示出对 SH-SY5Y 显著的细胞毒性[1]

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

体内研究
(In Vivo)

Antipsychotic agent-2 (Compound 11; 20-80 mg/kg; i.p.; once) 诱导小鼠自发运动活动发生统计学显著变化[1]
Antipsychotic agent-2 (40 mg/kg; i.p.; once) 降低安非他明 (amphetamine) 引起的小鼠多动症[1]

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

Animal Model: Naive Swiss male mice, amphetamine-induced hyperactivity[1]
Dosage: 40 mg/kg
Administration: IP, once
Result: Decreased amphetamine-induced hyperactivity.
分子量

395.47

Formula

C22H26FN5O

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
  • 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.

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Antipsychotic agent-2
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HY-149247
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