| 名稱 | Asenapine Maleate |
| 描述 | Asenapine Maleate (Org 5222 maleate) 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. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | Asenapine（0.01 mg/kg,i.v.）與NAc核相比,殼內(nèi)優(yōu)先增加多巴胺的流出量,而高劑量(0.05 mg/kg, i.v.)則無(wú)差異.在內(nèi)側(cè)前額葉皮質(zhì)的錐體細(xì)胞中,Asenapine對(duì)NMDA誘導(dǎo)的應(yīng)答有顯著增強(qiáng)作用.在自由移動(dòng)的大鼠中,Asenapine（0.05-0.2 mg/kg,皮下注射）誘導(dǎo)劑量依賴性CAR抑制（無(wú)逃避失敗記錄）,且未誘發(fā)強(qiáng)直性昏厥.在大鼠在內(nèi)側(cè)前額葉皮質(zhì)和伏隔核中,Asenapine（0.05-0.2 mg/kg,皮下注射）同時(shí)增加多巴胺流出. |
| 體內(nèi)活性 | 相對(duì)于其D2受體親和力,Asenapine對(duì)5-HT 2C,5-HT 2A,5-HT 2B,5-HT 7,5-HT 6,alpha2B和D3受體的親和力更高,說明在治療劑量下其與這些靶標(biāo)聯(lián)系更緊密。Asenapine是一種對(duì)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受體（8.4）有效的拮抗劑（pKB）。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (149.31 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
|
| 關(guān)鍵字 | inhibit | Asenapine Maleate | Org5222 | Inhibitor | Org-5222 | Org 5222 Maleate | 5-HT Receptor | 5-hydroxytryptamine Receptor | Serotonin Receptor | Asenapine |
| 相關(guān)產(chǎn)品 | Cinchonidine | Cloperastine hydrochloride | Alverine citrate | Amitriptyline hydrochloride | Dapoxetine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Serotonin hydrochloride | CLOZAPINE N-OXIDE |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | EMA 上市藥物庫(kù) | FDA 上市藥物庫(kù) | GPCR靶點(diǎn)分子庫(kù) | 膜蛋白靶向化合物庫(kù) | 疼痛相關(guān)化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌藥物庫(kù) |