Dimethyl-W84 dibromide

M2 receptor modulator



ALX-550-400-M005	5 mg	86.00 USD

Very 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 higher than with W84 (Prod. No. ALX-550-399). pK_A=7.08, p(αK_A)=6.75, pEC_50,diss=6.77.

Product Specification

Alternative Name:	N,N’-Bis[3-(1,3-dihydro-5-methyl-1,3-dioxo-2H-isoindol-2-yl)propyl]-N,N,N’,N’-tetramethyl-1,6-hexanediamminium dibromide

Formula:	C₃₄H₄₈Br₂N₄O₄

MW:	736.6

Purity:	≥98% (HPLC)

Appearance:	White to off-white solid.

CAS:	402475-33-6

Solubility:	Soluble in DMSO, water or aqueous buffer.

Long Term Storage:	+4°C

Handling:	Avoid freeze/thaw cycles.

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Product Literature References

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;

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

Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators: A. Raasch, et al.; J. Med. Chem. 45, 3809 (2002), Abstract;

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

Using a radioalloster to test predictions of the cooperativity model for gallamine binding to the allosteric site of muscarinic acetylcholine M(2) receptors: C. Trankle, et al.; Mol. Pharmacol. 56, 962 (1999), Abstract; Full Text

Identification of a [3H]Ligand for the common allosteric site of muscarinic acetylcholine M2 receptors: C. Trankle, et al.; Mol. Pharmacol. 54, 139 (1998), Abstract; Full Text