W-84 dibromide  (Synonyms: HDMPPA)

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].

muscarinic acetylcholine receptors^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

708.52

C₃₂H₄₄Br₂N₄O₄

21093-51-6

Solid

White to off-white

C[N+](C)(CCCN(C(C1=C2C=CC=C1)=O)C2=O)CCCCCC[N+](C)(CCCN(C(C3=C4C=CC=C3)=O)C4=O)C.[Br-].[Br-]

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]