ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.

A2AR:1.4 nM (Ki)

ZM 241385对A2a受体具有高亲和力。在大鼠嗜铬细胞瘤细胞膜中，ZM 241385通过具有9.52[3]的pIC50，置换了标记的5'-N-ethylcarboxamidoadenosine (NECA)的结合。ZM241385延迟了缺氧去极化（AD）的出现，这种现象与细胞损伤和死亡密切相关，保护CA1神经元和星形胶质细胞免受严重的（7分钟）OGD期间引起的突触活动抑制和损伤[4]。

ZM-241385 明显减弱了 CCPA 和 NECA 引起的降压效应，但并不改变这些激动剂所引起的心动过缓。它阻断了这两种不同腺苷受体激动剂所具有的减小梗死面积（心脏保护作用）的效应[1]。

Nitric oxide (NO) production is assessed by measuring the amount of nitrite, a stable metabolic product of NO that provides an indirect measurement of NO, by using the Griess diazotization reaction. Briefly, 24 h after incubation with 1.0 µM CG21680 or 1.0 µM ZM241385 or exposure to SMF, samples of medium (150 µl) are collected from cells and mixed with 130 µl dWater and with 20 µl Griess reagent using instruction supplied by the manufacturer. After a 30 min incubation period at room temperature, the samples are evaluated spectrophotometrically at 548 nm and OD values-in comparison with a standard curve is determined in culture medium by using serial dilutions of sodium nitrite-represented total stable metabolites of NO. (Only for Reference)