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  • Title: A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold.
    Author: Diouf O, Gadeau S, Chellé F, Gelbcke M, Talaga P, Christophe B, Gillard M, Massingham R, Guyaux M.
    Journal: Bioorg Med Chem Lett; 2002 Sep 16; 12(18):2535-9. PubMed ID: 12182854.
    Abstract:
    A series of 4-amino-piperidine containing molecules have been synthesized and structure-affinity relationship toward the M3-muscarinic receptor has been investigated. Chemical modulations provided molecules with K(i) for the human M3-R up to 1 nM with variable selectivity (3- to 40-fold) over the human M2-R. Compounds 2 (pA(2)=8.3, 8.6) demonstrates in vitro on guinea pig bladder and ileal strips potent anticholinergic properties and tissue selectivity.
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