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Literature DB >> 15163212

Development of a new type of allosteric modulator of muscarinic receptors: hybrids of the antagonist AF-DX 384 and the hexamethonio derivative W84.

Marion Mohr¹, Eberhard Heller, Ameneh Ataie, Klaus Mohr, Ulrike Holzgrabe.

Abstract

Various fragments of the hexamethonio-type allosteric agent W84 were linked to the secondary amino group of the muscarinic M(2) acetylcholine receptor-preferring antagonist AF-DX 384 to increase the area of attachment with the allosteric site. Addition of only the phthalimido moiety of W84 gave an allosteric enhancer of NMS binding. Thus, a new lead structure for the development of allosteric enhancers of NMS binding has been discovered.

Entities: Chemical Disease

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Year: 2004 PMID： 15163212 DOI： 10.1021/jm031095t

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

5 in total

1. Allosteric site in M2 acetylcholine receptors: evidence for a major conformational change upon binding of an orthosteric agonist instead of an antagonist.

Authors: Maren Grossmüller; Johannes Antony; Christian Tränkle; Ulrike Holzgrabe; Klaus Mohr
Journal: Naunyn Schmiedebergs Arch Pharmacol Date: 2005-12-16 Impact factor: 3.000

5. Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M₂R Affinity and Selectivity.

Authors: Xueke She; Andrea Pegoli; Judith Mayr; Harald Hübner; Günther Bernhardt; Peter Gmeiner; Max Keller
Journal: ACS Omega Date: 2017-10-16

5 in total

Development of a new type of allosteric modulator of muscarinic receptors: hybrids of the antagonist AF-DX 384 and the hexamethonio derivative W84.

1. Allosteric site in M2 acetylcholine receptors: evidence for a major conformational change upon binding of an orthosteric agonist instead of an antagonist.

Review 2. Rational design of dualsteric GPCR ligands: quests and promise.

3. Allosteric modulators and selective agonists of muscarinic receptors.

4. Crystal structure of 5,11-di-hydro-pyrido[2,3-b][1,4]benzodiazepin-6-one.

5. Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M₂R Affinity and Selectivity.

Development of a new type of allosteric modulator of muscarinic receptors: hybrids of the antagonist AF-DX 384 and the hexamethonio derivative W84.

1. Allosteric site in M2 acetylcholine receptors: evidence for a major conformational change upon binding of an orthosteric agonist instead of an antagonist.

Review 2. Rational design of dualsteric GPCR ligands: quests and promise.

3. Allosteric modulators and selective agonists of muscarinic receptors.

4. Crystal structure of 5,11-di-hydro-pyrido[2,3-b][1,4]benzodiazepin-6-one.

5. Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M2R Affinity and Selectivity.

5. Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M₂R Affinity and Selectivity.