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Development of a New Type of Allosteric Modulator of Muscarinic Receptors: Hybrids of the Antagonist AF-DX 384 and the Hexamethonio Derivative W84

2004; American Chemical Society; Volume: 47; Issue: 12 Linguagem: Inglês

10.1021/jm031095t

1520-4804

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

Neuropeptides and Animal Physiology

Various fragments of the hexamethonio-type allosteric agent W84 were linked to the secondary amino group of the muscarinic M2 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.