Asenapine maleate是5-HT和D2的拮抗剂，Ki值分别为 0.03-4.0 nM, 1.3 nM。它也是抗精神病药物，用于治疗与双相 1 型障碍相关的精神分裂症和躁狂或混合发作。

Asenapine is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

Asenapine（0.01 mg/kg,i.v.）与NAc核相比,壳内优先增加多巴胺的流出量,而高剂量(0.05 mg/kg, i.v.)则无差异.在内侧前额叶皮质的锥体细胞中,Asenapine对NMDA诱导的应答有显著增强作用.在自由移动的大鼠中,Asenapine（0.05-0.2 mg/kg,皮下注射）诱导剂量依赖性CAR抑制（无逃避失败记录）,且未诱发强直性昏厥.在大鼠在内侧前额叶皮质和伏隔核中,Asenapine（0.05-0.2 mg/kg,皮下注射）同时增加多巴胺流出.

相对于其D2受体亲和力,Asenapine对5-HT 2C,5-HT 2A,5-HT 2B,5-HT 7,5-HT 6,alpha2B和D3受体的亲和力更高,说明在治疗剂量下其与这些靶标联系更紧密。Asenapine是一种对5-HT 1A（7.4）,5-HT1B（8.1）,5-HT 2A（9.0）,5-HT 2B（9.3）,5-HT 2C（9.0）,5-HT 6（8.0 ）,5-HT 7（8.5）,D2（9.1）,D3（9.1）,alpha2A（7.3）,alpha2B（8.3）,alpha2C（6.8）和H 1受体（8.4）有效的拮抗剂（pKB）。

In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service.

85650-56-2

C21H20ClNO5

401.84

马来酸阿塞那平;阿塞那平马来酸盐;Org 5222 maleate;Org 5222

H2O:<1 mgml
DMSO:74 mg/mL (184.2 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years