AMPA受体选择性阻断剂前体

AMPA受体选择性阻断剂前体用途

GYKI 52466 hydrochloride 是一种具有口服活性、高选择性和非竞争性的 AMPA/Kainate 受体拮抗剂,其 IC50 值分别为 7.5 和 11 μM。GYKI 52466 hydrochloride 具有良好的血脑屏障通透性和抗惊厥作用,可用于帕金森病的研究。

AMPA受体选择性阻断剂前体名称

[ CAS 号 ]:
192065-56-8

[ 中文名 ]:
GYKI 52466盐酸盐

[ 英文名 ]:
1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride

[英文别名 ]:

AMPA受体选择性阻断剂前体生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> iGluR

[体外研究]

GYKI 52466盐酸盐(0.3-100μM)抑制培养的大鼠海马神经元中AMPA和Kainate受体激活的内向电流[1]。

[体内研究]

GYKI 52466盐酸盐(腹膜内注射；1.76-13.2 mg/kg；一次)治疗对DBA/2小鼠的声音诱导的癫痫发作提供了强有力的抗惊厥保护[2]。

[参考文献]

[1]. S D Donevan, et al. GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses. Neuron. 1993 Jan;10(1):51-9.

[2]. A G Chapman, et al. The anticonvulsant effect of the non-NMDA antagonists, NBQX and GYKI 52466, in mice. Epilepsy Res. 1991 Jul;9(2):92-6.

AMPA受体选择性阻断剂前体物理化学性质

[ 分子式 ]:
C₁₇H₁₆ClN₃O₂

[ 分子量 ]:
329.78

[ 精确质量 ]:
329.09300

[ PSA ]:
69.20000

[ LogP ]:
3.02130

[ 储存条件 ]:
室温

AMPA受体选择性阻断剂前体安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
22-26-36

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

[ 海关编码 ]:
2934999090

AMPA受体选择性阻断剂前体海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

AMPA受体选择性阻断剂前体文献

Activation of GluR6-containing kainate receptors induces ubiquitin-dependent Bcl-2 degradation via denitrosylation in the rat hippocampus after kainate treatment.

J. Thorac. Cardiovasc. Surg. 286 , 7669-80, (2011)

We previously showed that Bcl-2 (B-cell lymphoma 2) is down-regulated in a kainate (KA)-induced rat epileptic seizure model. The underlying mechanism had remained largely unknown, but we here report f...

GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses.

Neuron 10 , 51, (1993)

In whole-cell voltage-clamp recordings from cultured rat hippocampal neurons, the 2,3-benzodiazepine GYKI 52466 was a potent antagonist of kainate- and AMPA-activated currents (IC50 values, 7.5 and 11...

Differential antagonism of alpha-amino-3-hydroxy-5-methyl-4- isoxazolepropionic acid-preferring and kainate-preferring receptors by 2,3-benzodiazepines.

Mol. Pharmacol. 47 , 582, (1995)

Whole-cell recordings were used to study the antagonism of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-preferring and kainate-preferring receptors by 2,3-benzodiazepines. Current t...

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