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Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.

Abstract：

:Building on the previously and successfully applied hypothesis that stereochemical complication in the proximity of the critical cationic head of a cholinergic agonist would result in subtype selective compounds, we synthesized a series of chiral derivatives of furmethide and 5-methylfurmethide, with the aim of obtaining compounds that are useful for treating diseases derived from cholinergic receptor dysfunctions and/or useful for further characterizing subtypes of cholinergic receptors. Unlike their parent compounds, the new molecules lack nicotinic activity, being pure muscarinic ligands. While binding studies on the five cloned human muscarinic receptors showed no subtype selectivity, functional assays revealed that some of the molecules of the series are potent M 2 selective partial agonists with interesting pharmacological profiles.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Scapecchi S,Nesi M,Matucci R,Bellucci C,Buccioni M,Dei S,Guandalini L,Manetti D,Martini E,Marucci G,Romanelli MN,Teodori E,Cirilli R

doi

10.1021/jm800145d

subject

Has Abstract

pub_date

2008-07-10 00:00:00

pages

3905-12

issue

13

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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