Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

D3 receptor:7.1 nM(ki), D4 receptor:25 nM(ki)

Iloperidone 对去甲肾上腺素alpha(1)-肾上腺素能受体、多巴胺 D(3) 及血清素 5-HT(2A) 受体表现出高亲和力（Ki < 10 nM）。[1] 对于多巴胺 D3 受体（Ki = 7.1 nM）的亲和力高于对多巴胺 D4 受体（Ki = 25 nM）。此外，Iloperidone 对 5-HT6 和 5-HT7 受体也显示出高亲和力（分别为 Ki = 42.7 nM 和 21.6 nM），并且发现其对 5-HT2A（Ki = 5.6 nM）的亲和力高于 5-HT2C 受体（Ki = 42.8 nM）。[2] 在大鼠纹状体中应用 0.3 mg/kg 至 10 mg/kg 剂量和在伏隔核中应用 1 mg/kg 至 10 mg/kg 剂量时，Iloperidone 显著增加了多巴胺积累，这是对 D2 受体阻断反应的多巴胺转化指标。[3]

Iloperidone在药理学大鼠模型中展现出与“非典型”抗精神病药物一致的行为效应，这些效应通过拮抗多巴胺和去甲肾上腺素受体介导，与感觉运动门控失调相关。Iloperidone（1及3 mg/kg）可防止1 mg/kg PCP治疗导致的PPI破坏效应。Iloperidone（0.3 mg/kg）能够防止Cirazoline引起的PPI缺陷，其机制并不依赖于对惊跳反应幅度的影响。[4]Iloperidone（10 mg/kg）和Melperone（10 mg/kg）在大鼠伏隔核（NAC）中引起的DA释放量相比于mPFC要小或相等，但它们均不增加NAC中乙酰胆碱（ACh）的释放。[5]

Immunoblotting for the mTOR kinase assay: HEK293 cells are plated at 2-2.5×105 cells/well of a 12-well plate and serum-starved for 24 hours in DMEM. Cells are treated with increasing concentrations of Rapamycin (0.05-50 nM) for 15 minutes at 37 °C. Serum is added to a final concentration of 20% for 30 minutes at 37 °C. Cells are lysed, and cell lysates are separated by SDS-PAGE. Resolved proteins are transferred to a polyvinylidene difluoride membrane and immunoblotted with a phosphospecific primary antibody against Thr-389 of p70 S6 kinase. Data are analyzed using ImageQuant and KaleidaGr