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133059-99-1

中文名稱 N-乙基-1,6-二氫-1,2-二甲基-6-(甲基亞氨基)-N-苯基-4-嘧啶胺鹽酸鹽
英文名稱 ZD7288
CAS 133059-99-1
分子式 C15H21ClN4
MOL 文件 133059-99-1.mol
133059-99-1 結(jié)構(gòu)式 133059-99-1 結(jié)構(gòu)式

基本信息

中文別名
N-乙基-1,6-二氫-1,2-二甲基-6-(甲基亞氨基)-N-苯基-4-嘧啶胺鹽酸鹽
N-乙基-1,6-二氫-1,2-二甲基-6-(甲基亞氨基)-N-苯基-4-嘧啶胺鹽酸鹽97
英文別名
ICI D2788
ICI D7288
N-ethyl-1,2-dimethyl-6-methylimino-N-phenyl-pyrimidin-4-amine hydrochl oride
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

物理化學性質(zhì)

儲存條件Desiccate at +4°C
溶解度溶于二甲基亞砜
形態(tài)結(jié)晶固體
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
ZD7288 (ICI D7288) 是一種有選擇性的超極化激活的環(huán)核苷酸門控 (HCN) 通道阻斷劑。
靶點

HCN channel

體外研究

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).

體內(nèi)研究

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).

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