N-乙基-1,6-二氢-1,2-二甲基-6-(甲基亚氨基)-N-苯基-4-嘧啶胺盐酸盐
| 中文名称 | N-乙基-1,6-二氢-1,2-二甲基-6-(甲基亚氨基)-N-苯基-4-嘧啶胺盐酸盐 |
|---|---|
| 中文同义词 | N-乙基-1,6-二氢-1,2-二甲基-6-(甲基亚氨基)-N-苯基-4-嘧啶胺盐酸盐;N-乙基-1,6-二氢-1,2-二甲基-6-(甲基亚氨基)-N-苯基-4-嘧啶胺盐酸盐97;化合物ZD7288;ZD7288,窦房结功能调节器 |
| 英文名称 | ZD7288 |
| 英文同义词 | ICI D2788;N-ethyl-1,6-dihydro-1,2-dimethyl-6-(methylimino)-N-phenyl-4-Pyrimidinamine hydrochloride;N-Ethyl-1,6-dihydro-1,2-diMethyl-6-(MethyliMino)- N-phenyl-4-pyriMidinaMine Monohydrochloride;N-ethyl-1,2-dimethyl-6-methylimino-N-phenyl-pyrimidin-4-amine hydrochl oride;ICI D7288;inhibit,ICI D-7288,Hyperpolarization activated cyclic nucleotide gated channels,ICI D 7288,ZD 7288,HCN Channel,ZD7288,Inhibitor,ZD-7288 |
| CAS号 | 133059-99-1 |
| 分子式 | C15H21ClN4 |
| 分子量 | 0 |
| EINECS号 | |
| 相关类别 | Ion Channels;Amines;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 133059-99-1.mol |
| 结构式 |  |
N-乙基-1,6-二氢-1,2-二甲基-6-(甲基亚氨基)-N-苯基-4-嘧啶胺盐酸盐 性质
| 储存条件 | Desiccate at +4°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 结晶固体 |
| 颜色 | 白色至米白色 |
HCN channel
ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker. ZD7288 inhibits glutamate release in a concentration-dependent manner. After incubation with 1, 5 and 50 µM ZD7288 for 24 hours, glutamate content in extracellular fluid is decreased to 69.0±2.8%, 31.4±2.0% and 4.4±0.3%, respectively (P<0.01, vs. DMEM/F12 group [100.2±4.2%]). After incubation with ZD7288 (25, 50, or 100 µM) for 20 minutes, 50 µM glutamate-induced [Ca 2+ ] i rises are attenuated to 59.2±2.7%, 41.4±2.3% and 21.0±1.4%, respectively glutamate (P<0.01, vs. 50 µM glutamate group).
Application of ZD7288 0.1 µM at 5 minutes before high-frequency stimulation significantly decreases the amplitude of field excitatory postsynaptic potentials (fEPSPs), and this inhibitory effect is maintained throughout the recording period. Application of 0.1 µM ZD7288 30 minutes after high-frequency stimulation almost completely reverses the established long-term potentiation (LTP). Following application of ZD7288 (0.1 µM) 5 minutes before high-frequency stimulation, glutamate content is reduced to 74.9±8.0% (P<0.05, vs. normal saline group). Furthermore, application of 0.1 µM ZD7288 30 minutes after high-frequency stimulation markedly decreases the glutamate content to 77.0%±9.4% (P<0.05, vs. normal saline group).