双哌嗪类化合物的合成及钙通道阻滞活性

Synthesis and calcium channel blocking activities of dipiperazine compounds

摘要: 为寻求活性更好、毒性更低的新结构类型钙通道阻滞剂，以氟桂利嗪为先导化合物，设计合成了一系列双哌嗪类新化合物，并经光谱证明其结构。初步药理实验结果表明，9个新化合物在⁴⁵Ca²⁺跨膜内流动药理实验中，对大鼠主动脉电压依赖型钙离子通道（PDC）均有钙阻滞活性，且部分化合物的活性强于阳性对照药硝苯吡啶。
- 双哌嗪化合物 /
- 合成 /
- 钙通道阻滞活性 /
- 放射性核素⁴⁵Ca /
- 跨膜内流技术
Abstract: With using flunarizine as a lead compund to search for calcium channel blockers with fewer side effects and improved potency,a series of dipiperazine compounds were prepared with their structures being confirmed by spectrometry.Their inhibitory effect on potential-dependent calcium channels(PDC) and Ca²⁺ antagonistic effect in rat aorta were determined by ⁴⁵Ca²⁺ transmembrane influx technique.Preliminary results showed that all the nine new compounds possessed calcium channel blocking activities.Some compounds exhibited stronger inhibitory effect on PDC than nifedipine.
- dipiperazine compounds /
- synthesis /
- calcium channel blocking activity /
- radionuclide ⁴⁵Ca²⁺ /
- ⁴⁵Ca²⁺ transmembrane influx technique