W-84 dibromide

Modify Date: 2024-01-08 19:21:12

W-84 dibromide Structure
W-84 dibromide structure
Common Name W-84 dibromide
CAS Number 21093-51-6 Molecular Weight 708.52400
Density N/A Boiling Point N/A
Molecular Formula C32H44Br2N4O4 Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of W-84 dibromide


W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine[1][2][3].

 Names

Name 3-(1,3-dioxoisoindol-2-yl)propyl-[6-[3-(1,3-dioxoisoindol-2-yl)propyl-dimethylazaniumyl]hexyl]-dimethylazanium,dibromide
Synonym More Synonyms

 W-84 dibromide Biological Activity

Description W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine[1][2][3].
Related Catalog
Target

muscarinic acetylcholine receptors[1]

In Vitro The stabilizing effect of W-84 (dibromide) on antagonist-receptor complexes may explain the overadditive protective action exerted by the combination of atropine and W-84 (dibromide) against organophosphate intoxication[1]. W-84 (dibromide) not only inhibits radioligand association but also strongly stabilizes antagonist-receptor complexes[2].
References

[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.

 Chemical & Physical Properties

Molecular Formula C32H44Br2N4O4
Molecular Weight 708.52400
Exact Mass 706.17300
PSA 74.76000

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xi
RIDADR NONH for all modes of transport

 Articles19

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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-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...

 Synonyms

Hexamethylene-bis-[dimethyl-(3-phthalimidopropyl)ammonium]dibromide
Hdmppa
W-84 dibromide
W-84
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