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2-[(3-氯苯基)氨基]-N-(4-吡啶基甲基)-4-(三氟甲基)-5-嘧啶甲酰胺盐酸盐

用途

GW 833972A是一种选择性CB2受体激动剂。GW 833972A抑制动物模型中诱导的神经去极化和柠檬酸诱导的咳嗽[1]。

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名称

[ CAS 号 ]:
1092502-33-4

[ 中文名 ]:
2-[(3-氯苯基)氨基]-N-(4-吡啶基甲基)-4-(三氟甲基)-5-嘧啶甲酰胺盐酸盐

[ 英文名 ]:
GW 833972A

[英文别名 ]:

生物活性

[ 描述 ]:

GW 833972A是一种选择性CB2受体激动剂。GW 833972A抑制动物模型中诱导的神经去极化和柠檬酸诱导的咳嗽[1]。

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 大麻素受体

[ 靶点 ]

hCB2-R:7.3 (pEC50)

rat CB2-R:7.5 (pEC50)

[体外研究]

GW 833972A(0.3-300μM；10分钟)抑制辣椒素诱导的人和豚鼠去极化,还抑制前列腺素 E(2)和高渗盐水诱导的豚鼠离体迷走神经去极化[1]。

[体内研究]

GW 833972A(30 mg/kg,2 mL/kg；腹腔注射; 单次剂量, 试验开始前 30分钟注射) 能够抑制柠檬酸诱导的有意识豚鼠的咳嗽症状。它还抑制辣椒素引起的主支气管血浆蛋白渗出现象[1]。

[参考文献]

[1]. Belvisi MG, et al. Inhibitory activity of the novel CB2 receptor agonist, GW833972A, on guinea-pig and human sensory nerve function in the airways. Br J Pharmacol. 2008 Oct;155(4):547-57.

物理化学性质

[ 分子式 ]:
C₁₈H₁₄Cl₂F₃N₅O

[ 分子量 ]:
444.23800

[ 精确质量 ]:
443.05300

[ PSA ]:
83.29000

[ LogP ]:
5.66720

[ 储存条件 ]:
2-8°C

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H315-H319-H335-H413

[ 警示性声明 ]:
P261-P301 + P310-P305 + P351 + P338

[ 危害码 (欧洲) ]:
T+

[ 风险声明 (欧洲) ]:
25-36/37/38

[ 安全声明 (欧洲) ]:
26-45

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

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