| Bioactivity | 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]. |
| Invitro | 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]。 |
| 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]。 Animal Model: |
| Name | Antipsychotic agent-2 |
| Formula | C22H26FN5O |
| Molar Mass | 395.47 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Stępnicki P, et al. Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents - Design, synthesis, structural studies and pharmacological profiling. Eur J Med Chem. 2023 Apr 5;252:115285. |