Literature DB >> 21930376

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

Evan P Lebois1, Gregory J Digby, Douglas J Sheffler, Bruce J Melancon, James C Tarr, Hyekyung P Cho, Nicole R Miller, Ryan Morrison, Thomas M Bridges, Zixiu Xiang, J Scott Daniels, Michael R Wood, P Jeffrey Conn, Craig W Lindsley.   

Abstract

Herein we report the discovery and SAR of a novel series of M(1) agonists based on the MLPCN probe, ML071. From this, VU0364572 emerged as a potent, orally bioavailable and CNS penetrant M(1) agonist with high selectivity, clean ancillary pharmacology and enantiospecific activity.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21930376      PMCID： PMC3190051          DOI： 10.1016/j.bmcl.2011.08.084

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


  35 in total

Review 1.  Towards a muscarinic hypothesis of schizophrenia.

Authors:  T J Raedler; F P Bymaster; R Tandon; D Copolov; B Dean
Journal:  Mol Psychiatry       Date:  2006-12-05       Impact factor: 15.992

Review 2.  Allosteric modulation of kinases and GPCRs: design principles and structural diversity.

Authors:  Jana A Lewis; Evan P Lebois; Craig W Lindsley
Journal:  Curr Opin Chem Biol       Date:  2008-04-18       Impact factor: 8.822

Review 3.  G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms.

Authors:  Thomas M Bridges; Craig W Lindsley
Journal:  ACS Chem Biol       Date:  2008-07-25       Impact factor: 5.100

4.  Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists.

Authors:  Julia N Heinrich; John A Butera; Tikva Carrick; Angela Kramer; Dianne Kowal; Tim Lock; Karen L Marquis; Mark H Pausch; Mike Popiolek; Shaiu-Ching Sun; Eugene Tseng; Albert J Uveges; Scott C Mayer
Journal:  Eur J Pharmacol       Date:  2009-01-11       Impact factor: 4.432

5.  M1 receptors play a central role in modulating AD-like pathology in transgenic mice.

Authors:  Antonella Caccamo; Salvatore Oddo; Lauren M Billings; Kim N Green; Hilda Martinez-Coria; Abraham Fisher; Frank M LaFerla
Journal:  Neuron       Date:  2006-03-02       Impact factor: 17.173

6.  A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning.

Authors:  Jana K Shirey; Ashley E Brady; Paulianda J Jones; Albert A Davis; Thomas M Bridges; J Phillip Kennedy; Satyawan B Jadhav; Usha N Menon; Zixiu Xiang; Mona L Watson; Edward P Christian; James J Doherty; Michael C Quirk; Dean H Snyder; James J Lah; Allan I Levey; Michelle M Nicolle; Craig W Lindsley; P Jeffrey Conn
Journal:  J Neurosci       Date:  2009-11-11       Impact factor: 6.167

7.  AC-260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model.

Authors:  Stefania Risso Bradley; Jelveh Lameh; Linda Ohrmund; Thomas Son; Abhishek Bajpai; Derek Nguyen; Mikael Friberg; Ethan S Burstein; Tracy A Spalding; Thomas R Ott; Hans H Schiffer; Ali Tabatabaei; Krista McFarland; Robert E Davis; Douglas W Bonhaus
Journal:  Neuropharmacology       Date:  2009-10-14       Impact factor: 5.250

8.  Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.

Authors:  Lei Ma; Matthew A Seager; Matthew Seager; Marion Wittmann; Marlene Jacobson; Denise Bickel; Maryann Burno; Keith Jones; Valerie Kuzmick Graufelds; Guangping Xu; Michelle Pearson; Alexander McCampbell; Renee Gaspar; Paul Shughrue; Andrew Danziger; Christopher Regan; Rose Flick; Danette Pascarella; Susan Garson; Scott Doran; Constantine Kreatsoulas; Lone Veng; Craig W Lindsley; William Shipe; Scott Kuduk; Cyrille Sur; Gene Kinney; Guy R Seabrook; William J Ray
Journal:  Proc Natl Acad Sci U S A       Date:  2009-08-26       Impact factor: 11.205

9.  Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia.

Authors:  Anantha Shekhar; William Z Potter; Jeffrey Lightfoot; John Lienemann; Sanjay Dubé; Craig Mallinckrodt; Frank P Bymaster; David L McKinzie; Christian C Felder
Journal:  Am J Psychiatry       Date:  2008-07-01       Impact factor: 18.112

Review 10.  Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Carrie K Jones; Craig W Lindsley
Journal:  Trends Pharmacol Sci       Date:  2009-02-07       Impact factor: 14.819
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  12 in total

1.  Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models.

Authors:  Gregory J Digby; Meredith J Noetzel; Michael Bubser; Thomas J Utley; Adam G Walker; Nellie E Byun; Evan P Lebois; Zixiu Xiang; Douglas J Sheffler; Hyekyung P Cho; Albert A Davis; Natali E Nemirovsky; Sarah E Mennenga; Bryan W Camp; Heather A Bimonte-Nelson; Jacob Bode; Kimberly Italiano; Ryan Morrison; J Scott Daniels; Colleen M Niswender; M Foster Olive; Craig W Lindsley; Carrie K Jones; P Jeffrey Conn
Journal:  J Neurosci       Date:  2012-06-20       Impact factor: 6.167

Review 2.  Emerging approaches for treatment of schizophrenia: modulation of cholinergic signaling.

Authors:  Daniel J Foster; Carrie K Jones; P Jeffrey Conn
Journal:  Discov Med       Date:  2012-12       Impact factor: 2.970

Review 3.  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 4.  Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease.

Authors:  Bruce J Melancon; James C Tarr; Joseph D Panarese; Michael R Wood; Craig W Lindsley
Journal:  Drug Discov Today       Date:  2013-09-17       Impact factor: 7.851

5.  Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.

Authors:  Jerri M Rook; Masahito Abe; Hyekyung P Cho; Kellie D Nance; Vincent B Luscombe; Jeffrey J Adams; Jonathan W Dickerson; Daniel H Remke; Pedro M Garcia-Barrantes; Darren W Engers; Julie L Engers; Sichen Chang; Jarrett J Foster; Anna L Blobaum; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2017-01-10       Impact factor: 4.418

6.  Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Authors:  Bruce J Melancon; Rocco D Gogliotti; James C Tarr; Sam A Saleh; Brian A Chauder; Evan P Lebois; Hyekyung P Cho; Thomas J Utley; Douglas J Sheffler; Thomas M Bridges; Ryan D Morrison; J Scott Daniels; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley; Michael R Wood
Journal:  Bioorg Med Chem Lett       Date:  2012-03-29       Impact factor: 2.823

7.  Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model.

Authors:  Evan P Lebois; Jason P Schroeder; Thomas J Esparza; Thomas M Bridges; Craig W Lindsley; P Jeffrey Conn; David L Brody; J Scott Daniels; Allan I Levey
Journal:  ACS Chem Neurosci       Date:  2017-03-07       Impact factor: 4.418

8.  Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.

Authors:  Gregory J Digby; Thomas J Utley; Atin Lamsal; Christian Sevel; Douglas J Sheffler; Evan P Lebois; Thomas M Bridges; Michael R Wood; Colleen M Niswender; Craig W Lindsley; P Jeffrey Conn
Journal:  ACS Chem Neurosci       Date:  2012-09-09       Impact factor: 4.418

9.  Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.

Authors:  Douglas J Sheffler; Christian Sevel; Uyen Le; Kimberly M Lovell; James C Tarr; Sheridan J S Carrington; Hyekyung P Cho; Gregory J Digby; Colleen M Niswender; P Jeffrey Conn; Corey R Hopkins; Michael R Wood; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2012-11-09       Impact factor: 2.823

10.  Hippocampal place cell dysfunction and the effects of muscarinic M1 receptor agonism in a rat model of Alzheimer's disease.

Authors:  Claire R Galloway; Kaushik Ravipati; Suyashi Singh; Evan P Lebois; Robert M Cohen; Allan I Levey; Joseph R Manns
Journal:  Hippocampus       Date:  2018-07-03       Impact factor: 3.899
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