| Description | Dilazep dihydrochloride is an adenosine uptake inhibitor. Dilazep dihydrochloride also inhibits the ischemic damage, membrane transport of nucleosides and platelet aggregation. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. |
| In vitro | Dilazep、NBI 与 Dipyridamole 被报道可以抑制不同细胞对腺苷的吸收。这一吸收机制已经在体外被广泛研究。在这些化合物中，Dilazep 和 NBI 的效果几乎是 Dipyridamole 的十倍。只有 Dilazep 是水溶的，且在制备水溶液时不需要辅助的有机溶剂[1]。 |
| In vivo | Dilazep抑制再灌注心脏线粒体中的磷脂酶活化，同时也抑制了因脑缺血及再灌注引起的脂质过氧化。Dilazep可能通过增加脑血流量和/或其对血管内皮细胞膜的保护作用，预防缺血性脑损伤。Dilazep给药后，即使低剂量(0.04-0.1 mg/kg/min)的外源性腺苷也能显著增加优势肠系膜动脉导通性(SMAC)并提高动脉血浆腺苷浓度。腺苷水平的增加与SMAC变化百分比的增加以及Rmax和EC50值(分别为193.4%的SMAC变化和2.8 μM)高度相关。8-phenyltheophylline的脉冲剂量的给药消除了Dilazep增强血管舒张能力的作用，但不影响异丙肾上腺素引起的松弛[1]。 |
| molecular weight | 677.61 |
| Molecular formula | C31H46Cl2N2O10 |
| CAS | 20153-98-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 65 mg/mL (95.93 mM), Sonication is recommended. H2O: 80 mg/mL (118.06 mM) |
| References | 1. Zhang Y, et al. Dilazep potentiation of adenosine-mediated superior mesenteric arterial vasodilation. J Pharmacol Exp Ther. 1991 Sep;258(3):767-71. 2. Kawagoe J, et al. Effect of dilazep dihydrochloride against ischemia and reperfusion-induced disruption of blood-brain barrier in rats: a quantitative study. Naunyn Schmiedebergs Arch Pharmacol. 1992 Apr;345(4):485-8. |