Product Introduction
Bioactivity


英文名: Isradipine

描述: Isradipine (PN 200-110) 是一种二氢吡啶类钙通道阻滞剂，具有抗高血压和血管扩张活性。它是一种具有口服活性的 L 型钙通道阻滞剂，也是一种潜在可行的帕金森病神经保护剂。

体外活性: 在易吸收乙醇的大鼠体内,Isradipine（1 mg/kg,3次/天）减少超过70%的乙醇摄入,减少的乙醇以成比例的水消耗补偿,且在处理的5天中该作用一直存在.在小鼠体内,Isradipine抑制可卡因和吗啡的戒断症状,也许可以成为针对海洛因和可卡因滥用的有效药物疗法.在自发性高血压大鼠体内,Isradipine使两种菌株中动脉管壁胶原蛋白含量显著减少,使颈动脉中弹性蛋白含量显著增加,但对主动脉壁中弹性蛋白的含量没有影响.Isradipine使低氧诱导的钙依赖型黄嘌呤氧化酶,胞质磷脂酶A(2),单胺氧化酶和环氧合酶-2的活化减少,并伴随细胞色素C释放和自由基产生的减少.Isradipine可预防低压缺氧伴随的神经病变增加,并预防caspase 3与钙蛋白酶表达增加诱导的记忆障碍.

体内活性: 体内摄氧量(I50 = 31.1 mM)和生长培养(I50 = 20.8 mM)测定显示Isradipine是效果最好的衍生物。在微摩尔浓度下,Isradipine对克氏锥虫Tulahuen菌株短膜型的耗氧量和生长培养即有抑制作用。

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

溶解度: Ethanol : 7.4 mg/mL (20 mM)
DMSO : 50 mg/mL (134.63 mM)


关键字: vasodilator | channel | selective peripheral | Ca2+ channels | circulation | Autophagy | Parkinson's | dihydropyridine | inhibit | calcium | Calcium Channel | Inhibitor | powerful | neuroprotective | Isradipine | L-type | Ca channels | peripheral

相关产品: Darodipine | Semotiadil recemate fumarate | 9-Hydroxycanthin-6-one | Turkesterone | Menthol | Manidipine dihydrochloride | (R)-Lercanidipine hydrochloride | Mibefradil | TTA-Q6 | Amlodipine maleate

相关库: Anti-Aging Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Autophagy Compound Library | NO PAINS Compound Library