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Dimethyl-W84 (dibromide) Sale

目录号 : GC43468

A selective M2 receptor allosteric modulator

Dimethyl-W84 (dibromide) Chemical Structure

Cas No.:402475-33-6

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5mg
¥1,970.00
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产品描述

Dimethyl-W84 is a selective allosteric modulator of the M2 muscarinic acetylcholine receptor. It hinders the dissociation of the orthosteric antagonist N-methylscopolamine from the M2 receptor with an EC50 value of 3 nM.

Chemical Properties

Cas No. 402475-33-6 SDF
Canonical SMILES CC1=CC=C(C(N(CCC[N+](C)(C)CCCCCC[N+](C)(C)CCCN2C(C(C=C(C)C=C3)=C3C2=O)=O)C4=O)=O)C4=C1.[Br-].[Br-]
分子式 C34H48N4O4•2Br 分子量 736.6
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 1.3576 mL 6.7879 mL 13.5759 mL
5 mM 0.2715 mL 1.3576 mL 2.7152 mL
10 mM 0.1358 mL 0.6788 mL 1.3576 mL
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Research Update

Interactions of orthosteric and allosteric ligands with [3H]Dimethyl-W84 at the common allosteric site of muscarinic M2 receptors

Mol Pharmacol 2003 Jul;64(1):180-90.PMID:12815174DOI:10.1124/mol.64.1.180

An optimized assay for the binding of [3H]Dimethyl-W84 to its allosteric site on M2 muscarinic receptors has been used to directly measure the affinities of allosteric ligands. Their potencies agree with those deduced indirectly by their modulation of the equilibrium binding and kinetics of [3H]N-methylscopolamine ([3H]NMS) binding to the orthosteric site. The affinities and cooperativities of orthosteric antagonists with [3H]Dimethyl-W84 have also been quantitated. These affinities agree with those measured directly in a competition assay using [3H]NMS. All these data are compatible with the predictions of the allosteric ternary complex model. The association and dissociation kinetics of [3H]Dimethyl-W84 are rapid but the estimate of its association rate constant is nevertheless comparable with that found for the orthosteric radioligand, [3H]NMS. This is unexpected, given that the allosteric site to which [3H]Dimethyl-W84 binds is thought to be located on the external face of the receptor and above the [3H]NMS binding site that is buried within the transmembrane helices. The atypical allosteric ligands tacrine and 4,4'-bis-[(2,6-dichloro-benzyloxy-imino)-methyl]-1,1'-propane-1,3-diyl-bis-pyridinium dibromide (Duo3) inhibit [3H]Dimethyl-W84 binding with the same potencies and comparably steep slope factors as found for inhibition of [3H]NMS binding. Tacrine and Duo3 decrease [3H]Dimethyl-W84 affinity, not the number of binding sites. It is suggested that these atypical ligands either bind to the two known spatially separated allosteric sites on muscarinic receptors with positive cooperativity or their binding to the common allosteric site modulates receptor-receptor interactions such that homotropic positive cooperativity within a dimer or higher oligomer is generated.