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277 related items for PubMed ID: 20660086

  • 1. The M1 muscarinic receptor allosteric agonists AC-42 and 1-[1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one bind to a unique site distinct from the acetylcholine orthosteric site.
    Jacobson MA, Kreatsoulas C, Pascarella DM, O'Brien JA, Sur C.
    Mol Pharmacol; 2010 Oct; 78(4):648-57. PubMed ID: 20660086
    [Abstract] [Full Text] [Related]

  • 2. Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.
    Keov P, Valant C, Devine SM, Lane JR, Scammells PJ, Sexton PM, Christopoulos A.
    Mol Pharmacol; 2013 Sep; 84(3):425-37. PubMed ID: 23798605
    [Abstract] [Full Text] [Related]

  • 3. Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist.
    Langmead CJ, Fry VA, Forbes IT, Branch CL, Christopoulos A, Wood MD, Herdon HJ.
    Mol Pharmacol; 2006 Jan; 69(1):236-46. PubMed ID: 16207821
    [Abstract] [Full Text] [Related]

  • 4. 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; 72(2):463-76. PubMed ID: 17525129
    [Abstract] [Full Text] [Related]

  • 5. Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation.
    Spalding TA, Ma JN, Ott TR, Friberg M, Bajpai A, Bradley SR, Davis RE, Brann MR, Burstein ES.
    Mol Pharmacol; 2006 Dec; 70(6):1974-83. PubMed ID: 16959945
    [Abstract] [Full Text] [Related]

  • 6. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats.
    Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, Peterson TE, Ansari MS, Baldwin RM, Kessler RM, Deutch AY, Lah JJ, Levey AI, Lindsley CW, Conn PJ.
    J Neurosci; 2008 Oct 08; 28(41):10422-33. PubMed ID: 18842902
    [Abstract] [Full Text] [Related]

  • 7. Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor.
    Avlani VA, Langmead CJ, Guida E, Wood MD, Tehan BG, Herdon HJ, Watson JM, Sexton PM, Christopoulos A.
    Mol Pharmacol; 2010 Jul 08; 78(1):94-104. PubMed ID: 20413650
    [Abstract] [Full Text] [Related]

  • 8. Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.
    Daval SB, Valant C, Bonnet D, Kellenberger E, Hibert M, Galzi JL, Ilien B.
    J Med Chem; 2012 Mar 08; 55(5):2125-43. PubMed ID: 22329602
    [Abstract] [Full Text] [Related]

  • 9. 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 08; 338(2):622-32. PubMed ID: 21558436
    [Abstract] [Full Text] [Related]

  • 10. Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias.
    Gregory KJ, Hall NE, Tobin AB, Sexton PM, Christopoulos A.
    J Biol Chem; 2010 Mar 05; 285(10):7459-74. PubMed ID: 20051519
    [Abstract] [Full Text] [Related]

  • 11. Contrasting effects of allosteric and orthosteric agonists on m1 muscarinic acetylcholine receptor internalization and down-regulation.
    Thomas RL, Langmead CJ, Wood MD, Challiss RA.
    J Pharmacol Exp Ther; 2009 Dec 05; 331(3):1086-95. PubMed ID: 19767446
    [Abstract] [Full Text] [Related]

  • 12. Long-term changes in the muscarinic M1 receptor induced by instantaneous formation of wash-resistant xanomeline-receptor complex.
    De Lorme KC, Grant MK, Noetzel MJ, Polson SB, El-Fakahany EE.
    J Pharmacol Exp Ther; 2007 Dec 05; 323(3):868-76. PubMed ID: 17855477
    [Abstract] [Full Text] [Related]

  • 13. Differential regulation of muscarinic M1 receptors by orthosteric and allosteric ligands.
    Davis CN, Bradley SR, Schiffer HH, Friberg M, Koch K, Tolf BR, Bonhaus DW, Lameh J.
    BMC Pharmacol; 2009 Dec 02; 9():14. PubMed ID: 19951444
    [Abstract] [Full Text] [Related]

  • 14. G protein coupling and signaling pathway activation by m1 muscarinic acetylcholine receptor orthosteric and allosteric agonists.
    Thomas RL, Mistry R, Langmead CJ, Wood MD, Challiss RA.
    J Pharmacol Exp Ther; 2008 Nov 02; 327(2):365-74. PubMed ID: 18664591
    [Abstract] [Full Text] [Related]

  • 15. 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 02; 154():243-254. PubMed ID: 29777683
    [Abstract] [Full Text] [Related]

  • 16. The role of transmembrane domain 3 in the actions of orthosteric, allosteric, and atypical agonists of the M4 muscarinic acetylcholine receptor.
    Leach K, Davey AE, Felder CC, Sexton PM, Christopoulos A.
    Mol Pharmacol; 2011 May 02; 79(5):855-65. PubMed ID: 21300722
    [Abstract] [Full Text] [Related]

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  • 18. Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis.
    Matsui H, Lazareno S, Birdsall NJ.
    Mol Pharmacol; 1995 Jan 02; 47(1):88-98. PubMed ID: 7838137
    [Abstract] [Full Text] [Related]

  • 19. A novel multivalent ligand that bridges the allosteric and orthosteric binding sites of the M2 muscarinic receptor.
    Steinfeld T, Mammen M, Smith JA, Wilson RD, Jasper JR.
    Mol Pharmacol; 2007 Aug 02; 72(2):291-302. PubMed ID: 17478612
    [Abstract] [Full Text] [Related]

  • 20. Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.
    Sheffler DJ, Sevel C, Le U, Lovell KM, Tarr JC, Carrington SJ, Cho HP, Digby GJ, Niswender CM, Conn PJ, Hopkins CR, Wood MR, Lindsley CW.
    Bioorg Med Chem Lett; 2013 Jan 01; 23(1):223-7. PubMed ID: 23200253
    [Abstract] [Full Text] [Related]

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