AMPA受体选择性阻断剂前体结构式
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常用名 | AMPA受体选择性阻断剂前体 | 英文名 | 1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride |
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CAS号 | 192065-56-8 | 分子量 | 329.78 | |
密度 | N/A | 沸点 | N/A | |
分子式 | C17H16ClN3O2 | 熔点 | N/A | |
MSDS | 美版 | 闪点 | N/A | |
符号 |
GHS07 |
信号词 | Warning |
AMPA受体选择性阻断剂前体用途GYKI 52466 hydrochloride 是一种具有口服活性、高选择性和非竞争性的 AMPA/Kainate 受体拮抗剂,其 IC50 值分别为 7.5 和 11 μM。GYKI 52466 hydrochloride 具有良好的血脑屏障通透性和抗惊厥作用,可用于帕金森病的研究。 |
中文名 | GYKI 52466盐酸盐 |
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英文名 | 4-(8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl)aniline,hydrochloride |
英文别名 | 更多 |
描述 | GYKI 52466 hydrochloride 是一种具有口服活性、高选择性和非竞争性的 AMPA/Kainate 受体拮抗剂,其 IC50 值分别为 7.5 和 11 μM。GYKI 52466 hydrochloride 具有良好的血脑屏障通透性和抗惊厥作用,可用于帕金森病的研究。 |
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相关类别 | |
体外研究 | GYKI 52466盐酸盐(0.3-100μM)抑制培养的大鼠海马神经元中AMPA和Kainate受体激活的内向电流[1]。 |
体内研究 | GYKI 52466盐酸盐(腹膜内注射;1.76-13.2 mg/kg;一次)治疗对DBA/2小鼠的声音诱导的癫痫发作提供了强有力的抗惊厥保护[2]。 |
参考文献 |
分子式 | C17H16ClN3O2 |
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分子量 | 329.78 |
精确质量 | 329.09300 |
PSA | 69.20000 |
LogP | 3.02130 |
储存条件 | 室温 |
符号 |
GHS07 |
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信号词 | Warning |
危害声明 | H315-H319-H335 |
警示性声明 | P261-P305 + P351 + P338 |
个人防护装备 | dust mask type N95 (US);Eyeshields;Gloves |
危害码 (欧洲) | Xn |
风险声明 (欧洲) | 36/37/38 |
安全声明 (欧洲) | 22-26-36 |
危险品运输编码 | NONH for all modes of transport |
海关编码 | 2934999090 |
海关编码 | 2934999090 |
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中文概述 | 2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0% |
申报要素 | 品名, 成分含量, 用途 |
Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
Activation of GluR6-containing kainate receptors induces ubiquitin-dependent Bcl-2 degradation via denitrosylation in the rat hippocampus after kainate treatment.
J. Thorac. Cardiovasc. Surg. 286 , 7669-80, (2011) We previously showed that Bcl-2 (B-cell lymphoma 2) is down-regulated in a kainate (KA)-induced rat epileptic seizure model. The underlying mechanism had remained largely unknown, but we here report f... |
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GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses.
Neuron 10 , 51, (1993) In whole-cell voltage-clamp recordings from cultured rat hippocampal neurons, the 2,3-benzodiazepine GYKI 52466 was a potent antagonist of kainate- and AMPA-activated currents (IC50 values, 7.5 and 11... |
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Differential antagonism of alpha-amino-3-hydroxy-5-methyl-4- isoxazolepropionic acid-preferring and kainate-preferring receptors by 2,3-benzodiazepines.
Mol. Pharmacol. 47 , 582, (1995) Whole-cell recordings were used to study the antagonism of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-preferring and kainate-preferring receptors by 2,3-benzodiazepines. Current t... |
1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride |