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克他命

克他命用途

Gabazine是 GABAA 受体的选择性竞争性拮抗剂,其对 GABA 受体的 IC50 值为 ~0.2 μM。

克他命名称

[ CAS 号 ]:
104104-50-9

[ 中文名 ]:
2-(3-羧基丙基)-3-氨基-6-(4-甲氧苯基)吡啶溴化物

[ 英文名 ]:
SR-95531

[中文别名 ]:

克他命

[英文别名 ]:

MFCD00055135
Gabazine
SR-95531

克他命生物活性

[ 描述 ]:

Gabazine是 GABAA 受体的选择性竞争性拮抗剂,其对 GABA 受体的 IC50 值为 ~0.2 μM。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

信号通路 >> 神经信号通路 >> GABA受体

研究领域 >> 神经疾病

[ 靶点 ]

0.2 μM (GABA receptor)[1].

[体外研究]

荷包牡丹碱和Gabazine(SR 95531)已被表征为GABA与GABAA受体结合的竞争性抑制剂。在阻断GABA引起的电流时,Gabazine比荷包牡丹碱更有效,3μMGABA引起的电流IC50为~0.2μM,Hill系数为1.0。对于含有野生型β2亚基的受体的反应,Gabazine将10μMαxalone引起的电流降低约30％。 Gabazine的浓度需要产生最大块的一半是~0.2μM。 Gabazine也只能产生由300μM戊巴比妥门控的部分电流。再次,最大降低约为30％,产生一半最大块所需的Gabazine浓度为~0.15μM[1]。

[参考文献]

[1]. Ueno S, et al. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J Neurosci. 1997 Jan 15;17(2):625-34.

[相关活性小分子]

克他命物理化学性质

[ 沸点 ]:
474.4ºC at 760 mmHg

[ 熔点 ]:
200 ºC (ethanol )

[ 分子式 ]:
C₁₅H₁₈BrN₃O₃

[ 分子量 ]:
368.226

[ 闪点 ]:
240.7ºC

[ 精确质量 ]:
367.053131

[ PSA ]:
89.32000

[ 外观性状 ]:
solid white

[ 蒸汽压 ]:
8.33E-10mmHg at 25°C

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
DMSO: 30 mg/mL

克他命安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

克他命文献

Effect of gabazine on sensory stimulation train evoked response in mouse cerebellar Purkinje cells.

Pharmazie 70(2) , 129-34, (2015)

Cerebellar Purkinje cells (PCs) respond to sensory stimulation via climbing fiber and mossy fiber-granule cell pathways, and generate motor-related outputs according to internal rules of integration a...

A hard-wired priority map in the superior colliculus shaped by asymmetric inhibitory circuitry.

J. Neurophysiol. 114 , 662-76, (2015)

The mammalian superior colliculus (SC) is a laminar midbrain structure that translates visual signals into commands to shift the focus of attention and gaze. The SC plays an integral role in selecting...

Neurotransmission to parasympathetic cardiac vagal neurons in the brain stem is altered with left ventricular hypertrophy-induced heart failure.

Am. J. Physiol. Heart Circ. Physiol. 309 , H1281-7, (2015)

Hypertension, cardiac hypertrophy, and heart failure (HF) are widespread and debilitating cardiovascular diseases that affect nearly 23 million people worldwide. A distinctive hallmark of these cardio...

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克他命