六亚甲基-双-[二甲基-(3-邻苯二甲酰亚氨基丙基)氨基]二溴化物

用途

W-84(二溴化物)是M2胆碱受体的有效变构调节剂,可延缓[3H]N-甲基东莨菪碱的解离。W-84二溴化物能稳定胆碱能拮抗剂受体复合物。W-84(二溴)是一种具有变构效应的非竞争性毒蕈碱乙酰胆碱受体拮抗剂。当与阿托品[1][2][3]结合使用时,W-84(二溴)可额外防止有机磷中毒。

名称

[ CAS 号 ]:
21093-51-6

[ 中文名 ]:
六亚甲基-双-[二甲基-(3-邻苯二甲酰亚氨基丙基)氨基]二溴化物

[ 英文名 ]:
W-84 dibromide

[英文别名 ]:

Hdmppa
W-84 dibromide
W-84

生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR

研究领域 >> 其他

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

[ 靶点 ]

muscarinic acetylcholine receptors[1]

[体外研究]

W-84(二溴化物)对拮抗受体复合物的稳定作用可以解释阿托品和W-84(二溴化物)联合使用对有机磷中毒的过度加性保护作用[1]。W-84(二溴)不仅抑制放射性配体结合,而且还强烈稳定拮抗剂受体复合物[2]。

[参考文献]

[1]. Jepsen K, et al. Allosteric stabilization of 3H-N-methylscopolamine binding in guinea-pig myocardium by an antidote against organophosphate intoxication. Pharmacol Toxicol. 1988;63(3):163-168.

[2]. Mohr K, et al. Equipotent allosteric effect of W84 on [3H]NMS-binding to cardiac muscarinic receptors from guinea-pig, rat, and pig. Pharmacol Toxicol. 1992;70(3):198-200.

[3]. Grossmüller M, et al. Allosteric site in M2 acetylcholine receptors: evidence for a major conformational change upon binding of an orthosteric agonist instead of an antagonist. Naunyn Schmiedebergs Arch Pharmacol. 2006;372(4):267-276.

物理化学性质

[ 分子式 ]:
C₃₂H₄₄Br₂N₄O₄

[ 分子量 ]:
708.52400

[ 精确质量 ]:
706.17300

[ PSA ]:
74.76000

[ 储存条件 ]:
-20°C，密封，干燥

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) ]:
Xi

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

合成路线

详细合成路线

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文献

Potentiation by alcuronium of the antimuscarinic effect of N-methylscopolamine in guinea pig left atria.

Eur. J. Pharmacol. 272 , 103-106, (1995)

Alcuronium is known to stabilize allosterically the binding of the muscarinic antagonist N-methylscopolamine to muscarinic M2 receptors and thus to elevate the equilibrium binding of N-methylscopolami...

Allosteric modulation of G protein-coupled receptors: perspectives and recent developments.

Drug Discov. Today 9 , 752-758, (2004)

Allosteric modulation of G protein-coupled receptors has recently been recognized as an alternative approach to gain selectivity in drug action. In this overview, allosteric modulators that enhance or...

A stable and highly potent hexamethonium derivative which modulates muscarinic receptors allosterically in guinea-pig hearts.

J. Pharm. Pharmacol. 46(2) , 108-12, (1994)

W84 (N,N,N',N'-tetramethyl-N,N'-bis-(3-phthalimidopropyl)-N,N'-hexane- 1,6- diyl-bis-ammonium dibromide) is a potent stabilizer of antagonist binding to muscarinic receptors; however, W84 hydrolyses i...

更多文献