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177 related items for PubMed ID: 29544056

  • 1. Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles.
    Dallagnol JCC, Khajehali E, van der Westhuizen ET, Jörg M, Valant C, Gonçalves AG, Capuano B, Christopoulos A, Scammells PJ.
    J Med Chem; 2018 Apr 12; 61(7):2875-2894. PubMed ID: 29544056
    [Abstract] [Full Text] [Related]

  • 2. 4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.
    Mistry SN, Jörg M, Lim H, Vinh NB, Sexton PM, Capuano B, Christopoulos A, Lane JR, Scammells PJ.
    J Med Chem; 2016 Jan 14; 59(1):388-409. PubMed ID: 26624844
    [Abstract] [Full Text] [Related]

  • 3. Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor.
    Khajehali E, Valant C, Jörg M, Tobin AB, Conn PJ, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A.
    Biochem Pharmacol; 2018 Aug 14; 154():243-254. PubMed ID: 29777683
    [Abstract] [Full Text] [Related]

  • 4. Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.
    Rook JM, Abe M, Cho HP, Nance KD, Luscombe VB, Adams JJ, Dickerson JW, Remke DH, Garcia-Barrantes PM, Engers DW, Engers JL, Chang S, Foster JJ, Blobaum AL, Niswender CM, Jones CK, Conn PJ, Lindsley CW.
    ACS Chem Neurosci; 2017 Apr 19; 8(4):866-883. PubMed ID: 28001356
    [Abstract] [Full Text] [Related]

  • 5. Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M1 Muscarinic Acetylcholine Receptors.
    van der Westhuizen ET, Spathis A, Khajehali E, Jörg M, Mistry SN, Capuano B, Tobin AB, Sexton PM, Scammells PJ, Valant C, Christopoulos A.
    Mol Pharmacol; 2018 Jul 19; 94(1):770-783. PubMed ID: 29691279
    [Abstract] [Full Text] [Related]

  • 6. The pharmacologic characterization of allosteric molecules: Gq protein activation.
    Bdioui S, Verdi J, Pierre N, Trinquet E, Roux T, Kenakin T.
    J Recept Signal Transduct Res; 2019 Apr 19; 39(2):106-113. PubMed ID: 31322035
    [Abstract] [Full Text] [Related]

  • 7. Inositol Phosphate Accumulation in Vivo Provides a Measure of Muscarinic M1 Receptor Activation.
    Popiolek M, Nguyen DP, Reinhart V, Edgerton JR, Harms J, Lotarski SM, Steyn SJ, Davoren JE, Grimwood S.
    Biochemistry; 2016 Dec 27; 55(51):7073-7085. PubMed ID: 27958713
    [Abstract] [Full Text] [Related]

  • 8. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity.
    Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ.
    Mol Pharmacol; 2009 Mar 27; 75(3):577-88. PubMed ID: 19047481
    [Abstract] [Full Text] [Related]

  • 9. Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes.
    Bradley SJ, Molloy C, Bundgaard C, Mogg AJ, Thompson KJ, Dwomoh L, Sanger HE, Crabtree MD, Brooke SM, Sexton PM, Felder CC, Christopoulos A, Broad LM, Tobin AB, Langmead CJ.
    Mol Pharmacol; 2018 Jun 27; 93(6):645-656. PubMed ID: 29695609
    [Abstract] [Full Text] [Related]

  • 10. Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.
    Berizzi AE, Gentry PR, Rueda P, Den Hoedt S, Sexton PM, Langmead CJ, Christopoulos A.
    Mol Pharmacol; 2016 Oct 27; 90(4):427-36. PubMed ID: 27461343
    [Abstract] [Full Text] [Related]

  • 11. 6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity.
    Jörg M, van der Westhuizen ET, Khajehali E, Burger WAC, White JM, Choy KHC, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A, Scammells PJ.
    ACS Chem Neurosci; 2019 Mar 20; 10(3):1099-1114. PubMed ID: 30547573
    [Abstract] [Full Text] [Related]

  • 12. Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.
    Chen X, Klöckner J, Holze J, Zimmermann C, Seemann WK, Schrage R, Bock A, Mohr K, Tränkle C, Holzgrabe U, Decker M.
    J Med Chem; 2015 Jan 22; 58(2):560-76. PubMed ID: 25478907
    [Abstract] [Full Text] [Related]

  • 13. Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.
    Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.
    J Med Chem; 2013 Jun 27; 56(12):5151-72. PubMed ID: 23718562
    [Abstract] [Full Text] [Related]

  • 14. Characterization of a Novel M1 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator Radioligand, [3H]PT-1284.
    Smith DL, Davoren JE, Edgerton JR, Lazzaro JT, Lee CW, Neal S, Zhang L, Grimwood S.
    Mol Pharmacol; 2016 Sep 27; 90(3):177-87. PubMed ID: 27382013
    [Abstract] [Full Text] [Related]

  • 15. Allosteric modulators of M1 muscarinic receptors enhance acetylcholine efficacy and decrease locomotor activity and turning behaviors in zebrafish.
    Widman CJ, Ventresca S, Dietrich J, Elmslie G, Smith H, Kaup G, Wesley A, Doenecke M, Williams FE, Schiefer IT, Ellis J, Messer WS.
    Sci Rep; 2024 Jun 28; 14(1):14901. PubMed ID: 38942828
    [Abstract] [Full Text] [Related]

  • 16. Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators.
    Berizzi AE, Bender AM, Lindsley CW, Conn PJ, Sexton PM, Langmead CJ, Christopoulos A.
    ACS Chem Neurosci; 2018 Jul 18; 9(7):1818-1828. PubMed ID: 29683647
    [Abstract] [Full Text] [Related]

  • 17. Pharmacological characterization of LY593093, an M1 muscarinic acetylcholine receptor-selective partial orthosteric agonist.
    Watt ML, Schober DA, Hitchcock S, Liu B, Chesterfield AK, McKinzie D, Felder CC.
    J Pharmacol Exp Ther; 2011 Aug 18; 338(2):622-32. PubMed ID: 21558436
    [Abstract] [Full Text] [Related]

  • 18. Towards a high-affinity allosteric enhancer at muscarinic M1 receptors.
    Lazareno S, Popham A, Birdsall NJ.
    J Mol Neurosci; 2002 Aug 18; 19(1-2):123-7. PubMed ID: 12212769
    [Abstract] [Full Text] [Related]

  • 19. PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems.
    Moran SP, Cho HP, Maksymetz J, Remke DH, Hanson RM, Niswender CM, Lindsley CW, Rook JM, Conn PJ.
    ACS Chem Neurosci; 2018 Sep 19; 9(9):2218-2224. PubMed ID: 29683646
    [Abstract] [Full Text] [Related]

  • 20. Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors.
    May LT, Avlani VA, Langmead CJ, Herdon HJ, Wood MD, Sexton PM, Christopoulos A.
    Mol Pharmacol; 2007 Aug 19; 72(2):463-76. PubMed ID: 17525129
    [Abstract] [Full Text] [Related]

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