W84 dibromide

M2 receptor modulator



ALX-550-399-M005	5 mg	44.00 USD

One of the first potent allosteric modulator of muscarinic receptors, selective for M2-receptors. Retards the dissociation of the antagonist N-methylscopolamine. Affinity for the free receptor is about 10-fold lower than with dimethyl-W84 (Prod. No. ALX-550-400) and about 100-fold lower than with naphmethonium. pK_A=6.19, P(αK_A)=5.73, pEC_50,diss=5.87.

Product Specification

Alternative Name:	N,N’-Bis[3-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)propyl]-N,N,N’,N’-tetramethyl-1,6-hexanediamminium dibromide, Hexamethylene-bis-[dimethyl-(3-phthalimidopropyl)ammonium] dibromide

Formula:	C₃₂H₄₄Br₂N₄O₄

MW:	708.5

Purity:	≥98% (HPLC)

Appearance:	White to off-white solid.

CAS:	21093-51-6

Solubility:	Soluble in DMSO, water or aqueous buffer.

Long Term Storage:	+4°C

Handling:	After reconstitution, prepare aliquots and store at -20°C.

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Product Literature References

Design, Synthesis, and Action of Oxotremorine-Related Hybrid-Type Allosteric Modulators of Muscarinic Acetylcholine Receptors: T. Disingrini, et al.; J. Med. Chem. 49, 366 (2006), Abstract;

Allosteric site in M(2) acetylcholine receptors: evidence for a major conformational change upon binding of an orthosteric agonist instead of an antagonist: M. Grossmuller, et al.; Naunyn Schmiedebergs Arch. Pharmacol. In print (2005), Abstract;

Atypical muscarinic allosteric modulation: cooperativity between modulators and their atypical binding topology in muscarinic M2 and M2/M5 chimeric receptors: C. Trankle, et al.; Mol. Pharmacol. 68, 1597 (2005), Abstract;

Muscarinic allosteric enhancers of ligand binding: pivotal pharmacophoric elements in hexamethonio-type agents: M. Muth, et al.; J. Med. Chem. 48, 2212 (2005), Abstract;

Allosteric site on muscarinic acetylcholine receptors: identification of two amino acids in the muscarinic M2 receptor that account entirely for the M2/M5 subtype selectivities of some structurally diverse allosteric ligands in N-methylscopolamine-occupie: U. Voigtlander, et al.; Mol. Pharmacol. 64, 21 (2003), Abstract; Full Text

Contribution of lateral substituents in symmetrical and non-symmetrical heptane-bisammonio compounds to the allosteric stabilization of N-methylscopolamine binding to muscarinic M2 receptors: M. Staudt, et al.; Arch. Pharm. (Weinheim) 336, 385 (2003), Abstract;

Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors: C. Trankle, et al.; Mol. Pharmacol. 64, 180 (2003), Abstract; Full Text

Systematic development of high affinity bis(ammonio)alkane-type allosteric enhancers of muscarinic ligand binding: M. Muth, et al.; J. Med. Chem. 46, 1031 (2003), Abstract;

Hexamethonium-type allosteric modulators of the muscarinic receptors bearing lateral dibenzazepine moieties: R. Li, et al.; Arch. Pharm. 334, 121 (2001), Abstract;

Structure-activity relationships in a series of bisquaternary bisphthalimidine derivatives modulating the muscarinic M(2)-receptor allosterically: H.M. Botero Cid, et al.; J. Med. Chem. 43, 2155 (2000), Abstract;

M2 receptor binding of the selective antagonist AF-DX 384: possible involvement of the common allosteric site: C. Trankle, et al.; Mol. Pharmacol. 53, 304 (1998), Abstract; Full Text

Search for lead structures to develop new allosteric modulators of muscarinic receptors: C. Trankle, et al.; J. Pharmacol. Exp. Ther. 279, 926 (1996), Abstract;