143692-48-2
中文名称 | 143692-48-2 |
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中文同义词 | 化合物 T15456 |
英文名称 | 1-(4-Aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepinehydrochloride |
英文同义词 | 1-(4-Aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepinehydrochloride;GYKI 53655 hydrochloride;5-(4-Aminophenyl)-8,9-dihydro-N,8-dimethyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide hydrochloride;GYKI-53655 hydrate;LY300168 hydrochloride hydrate |
CAS号 | 143692-48-2 |
分子式 | C19H21ClN4O3 |
分子量 | 388.85 |
EINECS号 | |
相关类别 | |
Mol文件 | 143692-48-2.mol |
结构式 | ![]() |
143692-48-2 性质
储存条件 | Desiccate at RT |
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溶解度 | H2O:>10mg/mL |
形态 | 粉末 |
颜色 | 黄色至橙色粘性至蜡状 |
AMPA
GYKI 53655 (LY300168) hydrochloride inhibits α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) (10 μM)-induced responses with IC 50 value of 5.9±0.1 μM. GYKI 53655 hydrochloride inhibits AMPA (10 μM) responses in recombinant G1uR4 expressing HEK293 cells with IC 50 value of 4.6±0.4 μM. Using 3 μM cyclothiazide the inhibition produced by GYKI 53655 hydrochloride is 79±2% (n=4 cells). GYKI 53655 hydrochloride produces only small inhibitions of kainate-induced currents at 30 μM and inhibits kainate-induced currents at a concentration of 100 μM by 12±2 (n=4) and 18±4 (n=4), respectively. GYKI 53655 hydrochloride inhibits AMPA receptor-mediated responses in cerebella Purkinje neurons with an IC 50 value of 1.5±0.1 μM.
GYKI 53655 hydrochloride (4 mg/kg) is found to have a short-lasting depressant effect on neuronal responses to iontophoretic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), with a half-recovery time of approximately 7 min. GYKI 53655 hydrochloride (4 and 8 mg/kg) substantially depresses or completely abolishes AMPA responses. Results demonstrate the dose-dependence of GYKI 53655 hydrochloride (2 to 8 mg/kg) in depressing responses to AMPA. At the highest doses tested, GYKI 53655 hydrochloride reduces AMPA responses to a comparable degree. Tonic fit and death are completely prevented by GYKI 53655 hydrochloride at dose over 5.0 mg/kg. The ED 50 value of GYKI 53655 hydrochloride is 2.2 mg/kg i.p. The maximal effects of GYKI 53655 hydrochloride lasts 3 h then the exit inhibition effect of GYKI 53655 hydrochloride falls to 20% 1 h later.
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-103228 | GYKI 53655 hydrochloride | 1 mg | 545元 | |
2024/04/30 | HY-103228 | 143692-48-2 GYKI 53655 hydrochloride | 143692-48-2 | 5mg | 1200元 |