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). pKA=7.08, p(αKA)=6.75, pEC50,diss=6.77.
Product Details
| 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 |
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| Formula: | C34H48Br2N4O4 |
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| MW: | 736.6 |
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| CAS: | 402475-33-6 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in DMSO, water or aqueous buffer. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | +4°C |
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| Handling: | Avoid freeze/thaw cycles. |
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| Regulatory Status: | RUO - Research Use Only |
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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
General Literature References
G protein-coupled receptor allosterism and complexing: A. Christopoulos and T. Kenakin; Pharmacol. Rev.
54, 323 (2002),
Abstract;
