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(±)-BAYK8644

(±)-BAYK8644用途

Bay K 8644是一种二氢吡啶化合物,是一种特殊的L型钙通道激动剂。Bay K 8644通过增加肌膜Ca2+通道的开放时间增加Ca2+内流[1]。

(±)-BAYK8644名称

[ CAS 号 ]:
71145-03-4

[ 中文名 ]:
1,4-二氢-2,6-二甲基-5-硝基-4-(2-[三氟甲基]苯基)吡啶-3-羧酸甲酯

[ 英文名 ]:
Bay K-8644

[中文别名 ]:

氟硝尼啶

[英文别名 ]:

rac-Aziridin-2-carbonitril
(+/-)-Aziridin-2-carbonitril
cyano-2 aziridine
2-aziridinecarbonitrile
MFCD00036697
2-cyano-2-aziridine
(.+/-.)-Bay K 8644
nitrile of aziridine-2-carboxylic acid
Bay K-8644

(±)-BAYK8644生物活性

[ 描述 ]:

Bay K 8644是一种二氢吡啶化合物,是一种特殊的L型钙通道激动剂。Bay K 8644通过增加肌膜Ca2+通道的开放时间增加Ca2+内流[1]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 神经疾病

[体外研究]

在新生大鼠心室肌细胞中,Bay K 8644(1μM)处理增加了2天龄细胞中的L型钙电流密度。Bay K 8644在2天龄培养细胞中比在7天龄培养细胞中增加的L型钙电流密度更高,这可以解释为每个发育阶段钙通道磷酸化水平的差异[2]。

[体内研究]

一次剂量低至10μg/kg的Bay K 8644可显著提高内毒素治疗的低血压大鼠的平均动脉压(MAP),而对正常大鼠的影响最小。Bay K 8644还可导致内毒素治疗组大鼠心率降低37%,对照组大鼠心率降低39%[1]。

[参考文献]

[1]. H Satoh, et al. Bay K 8644 increases resting Ca2+ spark frequency in ferret ventricular myocytes independent of Ca influx: contrast with caffeine and ryanodine effects. Circ Res. 1998 Dec 14-28;83(12):1192-204.

[2]. J P Gomez, et al. Effects of Bay K 8644 on L-type calcium current from newborn rat cardiomyocytes in primary culture. J Mol Cell Cardiol. 1996 Oct;28(10):2217-29.

[3]. N Ives,et al. BAY k 8644, a calcium channel agonist, reverses hypotension in endotoxin-shocked rats. Eur J Pharmacol. 1986 Nov 4;130(3):169-75.

(±)-BAYK8644物理化学性质

[ 密度 ]:
1.37g/cm3

[ 沸点 ]:
404.3ºC at 760 mmHg

[ 分子式 ]:
C₁₆H₁₅F₃N₂O₄

[ 分子量 ]:
356.29700

[ 闪点 ]:
198.3ºC

[ 精确质量 ]:
356.09800

[ PSA ]:
84.15000

[ LogP ]:
4.19940

[ 外观性状 ]:
黄色粉末

[ 折射率 ]:
1.545

[ 储存条件 ]:
-20℃

(±)-BAYK8644MSDS

(±)-BAYK8644安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319

[ 警示性声明 ]:
P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/38

[ 安全声明 (欧洲) ]:
26-36

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

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(±)-BAYK8644文献

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J. Surg. Res. 184(2) , 944-50, (2013)

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J. Physiol. 586(7) , 1963-75, (2008)

The regulation of neuromediator expression by neuronal activity in the enteric nervous system (ENS) is currently unknown. Using primary cultures of ENS derived from rat embryonic intestine, we have ch...

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