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104104-50-9

中文名稱 克他命
英文名稱 SR-95531
CAS 104104-50-9
分子式 C15H18BrN3O3
分子量 368.23
MOL 文件 104104-50-9.mol
更新日期 2026/06/04 14:21:33
104104-50-9 結構式 104104-50-9 結構式

基本信息

中文別名
2-(3-羧基丙基)-3-氨基-6-(4-甲氧苯基)吡啶溴化物
英文別名
GABAZINE
SR-95531
GABAZINE BROMIDE
Gabazine Hydrobromide
SR 95531 HYDROBROMIDE
SR 95531 hydrobromide NEW
2-(3-CARBOXYPROPYL)-3-AMINO-6-(4-METHOXYPHENYL)PYRIDAZINIUM
6-Amino-5-methyl-3-(4-methoxyphenyl)-1-pyridaziniumbutyric acid br
2-(3-CARBOXYPROPYL)-3-AMINO-6-(4 METHOXYPHENYL)PYRIDAZINIUM BROMIDE
6-IMINO-3-(4-METHOXYPHENYL)-1(6H)-PYRIDAZINEBUTANOIC ACID HYDROBROMIDE
所屬類別
生物:拮抗劑

物理化學性質(zhì)

熔點200 °C(Solv: ethanol (64-17-5))
儲存條件Store at RT
溶解度DMSO: 30 mg/mL
溶解度在DMSO中的溶解度為30 毫克/毫升
形態(tài)solid
顏色white
水溶解性water: 25mM
InChI1S/C15H17N3O3.BrH/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20;/h4-9,16H,2-3,10H2,1H3,(H,19,20);1H
InChIKeyGFZHNFOGCMEYTA-UHFFFAOYSA-N
SMILES[Br-].COc1ccc(cc1)-c2ccc(N)[n+](CCCC(O)=O)n2

安全數(shù)據(jù)

危險性符號(GHS)有害 (GHS07)
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
WGK Germany3
WGK Germany3
存儲類別11 - Combustible Solids

常見問題列表

生物活性
Gabazine是 GABAA 受體 的選擇性競爭性拮抗劑,其對 GABA 受體的 IC50 值為 ~0.2 μM。
靶點

0.2 μM (GABA receptor).

體外研究

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.

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