Product Introduction
Bioactivity


英文名: ST-1535

描述: ST 1535 是有效的，具有口服活性的 A2A 腺苷受体拮抗剂。ST 1535 显示出抗帕金森病活性和抗震颤作用。

体外活性: ST-1535 在经人类A2A腺苷受体克隆的细胞中，竞争性拮抗A2A腺苷激动剂NECA对cAMP的影响（IC50=353±30 nM），并在经人类A1腺苷受体克隆的细胞中竞争性拮抗A1腺苷激动剂CHA对cAMP的影响（IC50=510±38 nM）。[1]

体内活性: ST 1535, at oral doses of 5 and 10 mg/kg, antagonizes catalepsy induced by intracerebroventricular administration of the A2A adenosine agonist CGS 21680 (10 microg/5 microl) in mice. At oral doses ranging between 5 and 20 mg/kg, ST 1535 induces hypermotility and antagonizes haloperidol-induced catalepsy in mice up to 7 h. Oral ST 1535, at 1.25 and 2.5 mg/kg, potentiates L-dopa effects in reducing haloperidol-induced catalepsy. [1]

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

溶解度: DMSO : 9 mg/mL (33.05 mM)


关键字: ST1535 | ST-1535 | ST 1535

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