阿塞那平马来酸盐 T1951

Product Introduction
Bioactivity


英文名: Asenapine Maleate

描述: Asenapine Maleate (Org 5222 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。

激酶实验: 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.

体外活性: 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.

体内活性: 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）。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 74 mg/mL (184.2 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | Asenapine Maleate | Org5222 | Inhibitor | Org-5222 | Org 5222 Maleate | 5-HT Receptor | 5-hydroxytryptamine Receptor | Serotonin Receptor | Asenapine

相关产品: AMI-193 | Serotonin hydrochloride | Facinicline hydrochloride | 8-Hydroxy-DPAT hydrobromide | Iprindole | PRX-07034 hydrochloride | SKF-83566 | BMY 7378 dihydrochloride | Desmethyl cariprazine | Paroxetine hydrochloride

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

阿塞那平马来酸盐 T1951信息由TargetMol中国为您提供，如您想了解更多关于阿塞那平马来酸盐 T1951报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途