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AMPA受体选择性阻断剂前体

更新时间:2024-01-08 19:08:19

AMPA受体选择性阻断剂前体结构式
AMPA受体选择性阻断剂前体结构式
品牌特惠专场
常用名 AMPA受体选择性阻断剂前体 英文名 1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride
CAS号 192065-56-8 分子量 329.78
密度 N/A 沸点 N/A
分子式 C17H16ClN3O2 熔点 N/A
MSDS 美版 闪点 N/A
符号 GHS07
GHS07
信号词 Warning

 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

中文名 GYKI 52466盐酸盐
英文名 4-(8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl)aniline,hydrochloride
英文别名 更多

 AMPA受体选择性阻断剂前体生物活性

描述 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。
相关类别
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
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5

更多文献
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...

 AMPA受体选择性阻断剂前体英文别名

1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride