Literature DB >> 20156687

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.

Thomas M Bridges1, J Phillip Kennedy, Meredith J Noetzel, Micah L Breininger, Patrick R Gentry, P Jeffrey Conn, Craig W Lindsley.   

Abstract

This Letter describes a chemical lead optimization campaign directed at VU0119498, a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) with the goal of developing a selective M(1) PAM. An iterative library synthesis approach delivered a potent (M(1) EC(50)=830 nM) and highly selective M(1) PAM (>30 microM vs M(2)-M(5)). Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20156687      PMCID： PMC2834874          DOI： 10.1016/j.bmcl.2010.01.109

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  23 in total

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4.  Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.

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Journal:  Trends Pharmacol Sci       Date:  2009-02-07       Impact factor: 14.819

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Journal:  Chem Rev       Date:  2016-02-16       Impact factor: 60.622

4.  A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity.

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Review 5.  Cholinergic interneurons in the dorsal and ventral striatum: anatomical and functional considerations in normal and diseased conditions.

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6.  Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.

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7.  Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.

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Review 8.  Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

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Review 9.  Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits.

Authors:  Briana J Davie; Arthur Christopoulos; Peter J Scammells
Journal:  ACS Chem Neurosci       Date:  2013-05-23       Impact factor: 4.418

Review 10.  Drugs for allosteric sites on receptors.

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