克他命
中文名称 | 克他命 |
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中文同义词 | 2-(3-羧基丙基)-3-氨基-6-(4-甲氧苯基)吡啶溴化物;4-(6-亚氨基-3-(4-甲氧苯基)哒嗪-1(6H)-基)丁酸氢溴酸盐;SR-95531,GABA A拮抗剂 |
英文名称 | SR-95531 |
英文同义词 | Gabazine, 2-(3-Carboxypropyl)-3-amino-6-(4 methoxyphenyl)pyridazinium bromide;1(6H)-Pyridazinebutanoic acid, 6-imino-3-(4-methoxyphenyl)-, monohydrobromide;6-Amino-5-methyl-3-(4-methoxyphenyl)-1-pyridaziniumbutyric acid br;6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid monohydrobromide;Gabazine Hydrobromide;4-(6-Imino-3-(4-methoxyphenyl)pyridazin-1(6H)-yl)butanoic acid hydrobromide;GABAZINE BROMIDE;2-(3-CARBOXYPROPYL)-3-AMINO-6-(4-METHOXYPHENYL)PYRIDAZINIUM |
CAS号 | 104104-50-9 |
分子式 | C15H18BrN3O3 |
分子量 | 368.23 |
EINECS号 | |
相关类别 | GABA/Glycine receptor |
Mol文件 | 104104-50-9.mol |
结构式 | ![]() |
克他命 性质
熔点 | 200 °C(Solv: ethanol (64-17-5)) |
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储存条件 | Store at RT |
溶解度 | 在DMSO中的溶解度为30 毫克/毫升 |
形态 | 固体 |
颜色 | 白色 |
0.2 μM (GABA receptor).
Both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA binding to the GABA A receptor. Gabazine is more potent than bicuculline at blocking currents elicited by GABA, with an IC 50 for currents elicited by 3 μM GABA of ~0.2 μM and a Hill coefficient of 1.0. Gabazine reduces the currents elicited by 10 μM alphaxalone by ~30%, for responses of receptors containing wildtype β2 subunits. The concentration of Gabazine requires producing half the maximal block is ~0.2 μM. Gabazine also could only produce a partial block of currents gated by 300 μM pentobarbital. The maximal reduction, again, is ~30%, and the concentration of Gabazine required to produce half the maximal block is ~0.15 μM.
安全信息
WGK Germany | 3 |
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提供商 | 语言 |
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英文
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