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
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六亚甲基-双-[二甲基-(3-邻苯二甲酰亚氨基丙基)氨基]二溴化物结构式
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常用名 | 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 |
|---|---|---|---|---|
| CAS号 | 21093-51-6 | 分子量 | 708.52400 | |
| 密度 | N/A | 沸点 | N/A | |
| 分子式 | C32H44Br2N4O4 | 熔点 | N/A | |
| MSDS | 中文版 美版 | 闪点 | N/A | |
| 符号 |
GHS07 |
信号词 | Warning |
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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-methylscopolamine in homogenized cardiac tissue. In order to check for a f... |
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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 diminish the effects of (endogenous) agonists or antagonis... |
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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 in aqueous buffered medium. The synthesis of the stable deri... |
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Interaction of Mg2+ with the allosteric site of muscarinic M2 receptors.
Naunyn Schmiedebergs Arch. Pharmacol. 357(4) , 363-70, (1998) Mg2+-ions have been suspected to attenuate the inhibitory effect of allosteric modulators on the dissociation of orthosteric ligands from muscarinic M2 receptors. It was aimed to gain more insight into the molecular events underlying the effect of Mg2+. The i... |
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Allosteric modulators and selective agonists of muscarinic receptors.
J. Mol. Neurosci. 30(1-2) , 165-8, (2006) Allosteric modulators of ligand-receptor interactions are found for a variety of receptors (Christopoulos, 2002). Allosteric agents attach to a binding site being topographically distinct from the site for conventional (orthosteric) agonists or antagonists. I... |
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Testing the specificity of allosteric modulators of muscarinic receptors in phylogenetically closely related histamine H1-receptors.
Naunyn Schmiedebergs Arch. Pharmacol. 361(2) , 107-12, (2000) Gallamine, alcuronium and W84 (hexane-1,6-bis[dimethyl-3'-phthalimidopropyl-ammonium bromide]) are prototype allosteric modulators of the G-protein coupled muscarinic acetylcholine receptor family, especially of the M2-subtype. In order to probe the specifici... |
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Identification of a [3H]Ligand for the common allosteric site of muscarinic acetylcholine M2 receptors.
Mol. Pharmacol. 54 , 139-145, (1998) Muscarinic acetylcholine receptors bind allosteric modulators at a site apart from the orthosteric site used by conventional ligands. We tested in cardiac tissue whether modulator binding to ligand-occupied muscarinic M2 receptors is a preferential event that... |
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Use of a spreadsheet to quantitate the equilibrium binding of an allosteric modulator.
Eur. J. Pharmacol. 355(1) , 103-11, (1998) Using the program Microsoft EXCEL, a spreadsheet was developed for constrained, simultaneous analysis of multiple datasets obtained from equilibrium binding experiments, according to an allosteric model of interaction. This approach was used to quantitate the... |
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Allosteric stabilization of 3H-N-methylscopolamine binding in guinea-pig myocardium by an antidote against organophosphate intoxication.
Pharmacol. Toxicol. 63(3) , 163-8, (1988) W84 (hexamethylene-bis-[dimethyl-(3-phthalimidopropyl)-ammonium bromide]) protects overadditively against an organophosphate-intoxication when applied in combination with atropine. Further experimental evidence led to the hypothesis that W84 exerted an allost... |
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Allosteric interactions with muscarinic acetylcholine receptors: complex role of the conserved tryptophan M2422Trp in a critical cluster of amino acids for baseline affinity, subtype selectivity, and cooperativity.
Mol. Pharmacol. 70(1) , 181-93, (2006) In general, the M2 subtype of muscarinic acetylcholine receptors has the highest sensitivity for allosteric modulators and the M5 subtype the lowest. The M2/M5 selectivity of some structurally diverse allosteric agents is known to be completely explained by M... |