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104104-50-9

中文名稱(chēng) 克他命
英文名稱(chēng) 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 2024/12/22 16:36:08
104104-50-9 結(jié)構(gòu)式 104104-50-9 結(jié)構(gòu)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

物理化學(xué)性質(zhì)

熔點(diǎn)200 °C(Solv: ethanol (64-17-5))
儲(chǔ)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

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P280-P305+P351+P338
WGK Germany3
WGK Germany3

常見(jiàn)問(wèn)題列表

生物活性
Gabazine是 GABAA 受體 的選擇性競(jìng)爭(zhēng)性拮抗劑,其對(duì) GABA 受體的 IC50 值為 ~0.2 μM。
靶點(diǎn)

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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