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Volumn 78, Issue 4, 2010, Pages 648-657

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

Author keywords

[No Author keywords available]

Indexed keywords

1 [1' (2 METHYLBENZYL) 1,4' BIPIPERIDIN 4 YL] 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; 4 N BUTYL 1 [4 (2 METHYLPHENYL) 4 OXO 1 BUTYL]PIPERIDINE HYDROGEN CHLORIDE; AC 42; ACETYLCHOLINE; CLOZAPINE; MUSCARINIC M1 RECEPTOR; MUSCARINIC M1 RECEPTOR AGONIST; NORCLOZAPINE; UNCLASSIFIED DRUG; XANOMELINE; 1-(1'-(2-METHYLBENZYL)-1,4'-BIPIPERIDIN-4-YL)-1H-BENZO(D)IMIDAZOL-2-(3H)-ONE; 4-N-BUTYL-1-(4-(2-METHYLPHENYL)-4-OXO-1-BUTYL)-PIPERIDINE HYDROGEN CHLORIDE; BENZIMIDAZOLE DERIVATIVE; PIPERIDINE DERIVATIVE;

EID: 77957233070     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.110.065771     Document Type: Article
Times cited : (25)

References (35)
  • 1
    • 77957055780 scopus 로고
    • Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors
    • Ballesteros JA and Weinstein H (1995) Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors. Methods Neurosci 25:366-428.
    • (1995) Methods Neurosci , vol.25 , pp. 366-428
    • Ballesteros, J.A.1    Weinstein, H.2
  • 2
    • 0035957549 scopus 로고    scopus 로고
    • Multiple allosteric sites on muscarinic receptors
    • DOI 10.1016/S0024-3205(01)01047-5, PII S0024320501010475
    • Birdsall NJ, Lazareno S, Popham A, and Saldanha J (2001) Multiple allosteric sites on muscarinic receptors. Life Sci 68:2517-2524. (Pubitemid 32455690)
    • (2001) Life Sciences , vol.68 , Issue.22-23 , pp. 2517-2524
    • Birdsall, N.J.M.1    Lazareno, S.2    Popham, A.3    Saldanha, J.4
  • 3
    • 19944401545 scopus 로고    scopus 로고
    • Allosterism at muscarinic receptors: Ligands and mechanisms
    • Birdsall NJ and Lazareno S (2005) Allosterism at muscarinic receptors: ligands and mechanisms. Mini Rev Med Chem 5:523-543.
    • (2005) Mini Rev Med Chem , vol.5 , pp. 523-543
    • Birdsall, N.J.1    Lazareno, S.2
  • 5
    • 0037375485 scopus 로고    scopus 로고
    • Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system
    • Bymaster FP, McKinzie DL, Felder CC, and Wess J (2003) Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system. Neurochem Res 28:437-442.
    • (2003) Neurochem Res , vol.28 , pp. 437-442
    • Bymaster, F.P.1    McKinzie, D.L.2    Felder, C.C.3    Wess, J.4
  • 6
    • 64549132538 scopus 로고    scopus 로고
    • M1 agonists as a potential disease-modifying therapy for Alzheimer's disease
    • Caccamo A, Fisher A, and LaFerla FM (2009) M1 agonists as a potential disease-modifying therapy for Alzheimer's disease. Curr Alzheimer Res 6:112-117.
    • (2009) Curr Alzheimer Res , vol.6 , pp. 112-117
    • Caccamo, A.1    Fisher, A.2    LaFerla, F.M.3
  • 7
    • 77951985712 scopus 로고    scopus 로고
    • Allosteric ligands for G protein-coupled receptors: A novel strategy with attractive therapeutic opportunities
    • De Amici M, Dallanoce C, Holzgrabe U, Tränkle C, and Mohr K (2010) Allosteric ligands for G protein-coupled receptors: a novel strategy with attractive therapeutic opportunities. Med Res Rev 30:463-549.
    • (2010) Med Res Rev , vol.30 , pp. 463-549
    • De Amici, M.1    Dallanoce, C.2    Holzgrabe, U.3    Tränkle, C.4    Mohr, K.5
  • 8
    • 0038024615 scopus 로고    scopus 로고
    • The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints
    • Fredriksson R, Lagerström MC, Lundin LG, and Schiöth HB (2003) The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol 63:1256-1272.
    • (2003) Mol Pharmacol , vol.63 , pp. 1256-1272
    • Fredriksson, R.1    Lagerström, M.C.2    Lundin, L.G.3    Schiöth, H.B.4
  • 9
    • 5544242529 scopus 로고    scopus 로고
    • MMFF VI. MMFF94s option for energy minimization studies
    • Halgren TA (1999) MMFF VI. MMFF94s option for energy minimization studies. J Comput Chem 20:720-729.
    • (1999) J Comput Chem , vol.20 , pp. 720-729
    • Halgren, T.A.1
  • 10
    • 0041411237 scopus 로고    scopus 로고
    • Scanning mutagenesis studies of the M1 muscarinic acetylcholine receptor
    • Hulme EC, Lu ZL, and Bee MS (2003) Scanning mutagenesis studies of the M1 muscarinic acetylcholine receptor. Receptors Channels 9:215-228.
    • (2003) Receptors Channels , vol.9 , pp. 215-228
    • Hulme, E.C.1    Lu, Z.L.2    Bee, M.S.3
  • 12
    • 55249118679 scopus 로고    scopus 로고
    • 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, et al. (2008) Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci 28:10422-10433.
    • (2008) J Neurosci , vol.28 , pp. 10422-10433
    • Jones, C.K.1    Brady, A.E.2    Davis, A.A.3    Xiang, Z.4    Bubser, M.5    Tantawy, M.N.6    Kane, A.S.7    Bridges, T.M.8    Kennedy, J.P.9    Bradley, S.R.10
  • 13
    • 33747181100 scopus 로고    scopus 로고
    • Allosteric agonists of TM7 receptors: Expanding the pharmacological toolbox
    • Langmead CJ and Christopoulos A (2006) Allosteric agonists of TM7 receptors: expanding the pharmacological toolbox. Trends Pharmacol Sci 27:475-481.
    • (2006) Trends Pharmacol Sci , vol.27 , pp. 475-481
    • Langmead, C.J.1    Christopoulos, A.2
  • 14
    • 30044435787 scopus 로고    scopus 로고
    • Probing the molecular mechanism of interaction between 4-nbutyl- 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, and Herdon HJ (2006) Probing the molecular mechanism of interaction between 4-nbutyl- 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. Mol Pharmacol 69:236-246.
    • (2006) Mol Pharmacol , vol.69 , pp. 236-246
    • Langmead, C.J.1    Fry, V.A.2    Forbes, I.T.3    Branch, C.L.4    Christopoulos, A.5    Wood, M.D.6    Herdon, H.J.7
  • 15
    • 38349193123 scopus 로고    scopus 로고
    • Muscarinic acetylcholine receptors as CNS drug targets
    • Langmead CJ, Watson J, and Reavill C (2008) Muscarinic acetylcholine receptors as CNS drug targets. Pharmacol Ther 117:232-243.
    • (2008) Pharmacol Ther , vol.117 , pp. 232-243
    • Langmead, C.J.1    Watson, J.2    Reavill, C.3
  • 16
    • 0031978756 scopus 로고    scopus 로고
    • Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: Radioligand binding studies
    • Lazareno S, Gharagozloo P, Kuonen D, Popham A, and Birdsall NJ (1998) Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies. Mol Pharmacol 53: 573-589.
    • (1998) Mol Pharmacol , vol.53 , pp. 573-589
    • Lazareno, S.1    Gharagozloo, P.2    Kuonen, D.3    Popham, A.4    Birdsall, N.J.5
  • 17
    • 59449090754 scopus 로고    scopus 로고
    • Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors
    • Lebon G, Langmead CJ, Tehan BG, and Hulme EC (2009) Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors. Mol Pharmacol 75:331-341.
    • (2009) Mol Pharmacol , vol.75 , pp. 331-341
    • Lebon, G.1    Langmead, C.J.2    Tehan, B.G.3    Hulme, E.C.4
  • 18
    • 0033548654 scopus 로고    scopus 로고
    • The functional topography of transmembrane 3 of the M1 muscarinic acetylcholine receptor, revealed by scanning mutagenesis
    • Lu ZL and Hulme EC (1999) The functional topography of transmembrane 3 of the M1 muscarinic acetylcholine receptor, revealed by scanning mutagenesis. J Biol Chem 274:7309-7315.
    • (1999) J Biol Chem , vol.274 , pp. 7309-7315
    • Lu, Z.L.1    Hulme, E.C.2
  • 19
    • 0035823524 scopus 로고    scopus 로고
    • Transmembrane domains 4 and 7 of the M1 muscarinic acetylcholine receptor are critical for ligand binding and the receptor activation switch
    • Lu ZL, Saldanha JW, and Hulme EC (2001) Transmembrane domains 4 and 7 of the M1 muscarinic acetylcholine receptor are critical for ligand binding and the receptor activation switch. J Biol Chem 276:34098-34104.
    • (2001) J Biol Chem , vol.276 , pp. 34098-34104
    • Lu, Z.L.1    Saldanha, J.W.2    Hulme, E.C.3
  • 22
    • 43749109187 scopus 로고    scopus 로고
    • Crystal structure of squid rhodopsin
    • Murakami M and Kouyama T (2008) Crystal structure of squid rhodopsin. Nature 453:363-367.
    • (2008) Nature , vol.453 , pp. 363-367
    • Murakami, M.1    Kouyama, T.2
  • 24
    • 0028815463 scopus 로고
    • Probing of the location of the allosteric site on the m1 muscarinic receptors by site-directed mutagenesis
    • Matsui H, Lazareno S, and Birdsall NJ (1995) Probing of the location of the allosteric site on the m1 muscarinic receptors by site-directed mutagenesis. Mol Pharmacol 47:88-98.
    • (1995) Mol Pharmacol , vol.47 , pp. 88-98
    • Matsui, H.1    Lazareno, S.2    Birdsall, N.J.3
  • 25
    • 0028989245 scopus 로고
    • The functional role of the binding site aspartate in muscarinic acetylcholine receptors, probed by site-directed mutagenesis
    • Page KM, Curtis CA, Jones PG, and Hulme EC (1995) The functional role of the binding site aspartate in muscarinic acetylcholine receptors, probed by site-directed mutagenesis. Eur J Pharmacol 289:429-437.
    • (1995) Eur J Pharmacol , vol.289 , pp. 429-437
    • Page, K.M.1    Curtis, C.A.2    Jones, P.G.3    Hulme, E.C.4
  • 27
    • 33748643600 scopus 로고    scopus 로고
    • The predicted 3D structures of the human M1 muscarinic acetylcholine receptor with agonist or antagonist bound
    • Peng JY, Vaidehi N, Hall SE, and Goddard WA 3rd (2006) The predicted 3D structures of the human M1 muscarinic acetylcholine receptor with agonist or antagonist bound. Chem Med Chem 1:878-890.
    • (2006) Chem Med Chem , vol.1 , pp. 878-890
    • Peng, J.Y.1    Vaidehi, N.2    Hall, S.E.3    Goddard III, W.A.4
  • 29
    • 33745088619 scopus 로고    scopus 로고
    • Use of an induced fit receptor structure in virtual screening
    • Sherman W, Beard HS, and Farid R (2006) Use of an induced fit receptor structure in virtual screening. Chem Biol Drug Des 67:83-84.
    • (2006) Chem Biol Drug des , vol.67 , pp. 83-84
    • Sherman, W.1    Beard, H.S.2    Farid, R.3
  • 31
    • 33751072945 scopus 로고    scopus 로고
    • 1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: Evidence for three distinct modes of receptor activation
    • DOI 10.1124/mol.106.024901
    • Spalding TA, Ma JN, Ott TR, Friberg M, Bajpai A, Bradley SR, Davis RE, Brann MR, and Burstein ES (2006) 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. Mol Pharmacol 70:1974-1983. (Pubitemid 44771913)
    • (2006) Molecular Pharmacology , vol.70 , Issue.6 , pp. 1974-1983
    • Spalding, T.A.1    Ma, J.-N.2    Ott, T.R.3    Friberg, M.4    Bajpai, A.5    Bradley, S.R.6    Davis, R.E.7    Brann, M.R.8    Burstein, E.S.9
  • 33
    • 0038237079 scopus 로고    scopus 로고
    • Allosteric site on muscarinic acetylcholine receptors: Identification of two amino acids in the muscarinic M2 receptor that account entirely for the M2/M5 subtype selectivities of some structurally diverse allosteric ligands in N-methylscopolamine-occupied receptors
    • Voigtländer U, Jöhren K, Mohr M, Raasch A, Tränkle C, Buller S, Ellis J, Höltje HD, and Mohr K (2003) Allosteric site on muscarinic acetylcholine receptors: identification of two amino acids in the muscarinic M2 receptor that account entirely for the M2/M5 subtype selectivities of some structurally diverse allosteric ligands in N-methylscopolamine-occupied receptors. Mol Pharmacol 64:21-31.
    • (2003) Mol Pharmacol , vol.64 , pp. 21-31
    • Voigtländer, U.1    Jöhren, K.2    Mohr, M.3    Raasch, A.4    Tränkle, C.5    Buller, S.6    Ellis, J.7    Höltje, H.D.8    Mohr, K.9
  • 34
    • 0032756999 scopus 로고    scopus 로고
    • Alanine-scanning mutagenesis of transmembrane domain 6 of the M1 muscarinic acetylcholine receptor suggests that Tyr381 plays a key role in receptor function
    • Ward SD, Curtis CA, and Hulme EC (1999) Alanine-scanning mutagenesis of transmembrane domain 6 of the M1 muscarinic acetylcholine receptor suggests that Tyr381 plays a key role in receptor function. Mol Pharmacol 56:1031-1041.
    • (1999) Mol Pharmacol , vol.56 , pp. 1031-1041
    • Ward, S.D.1    Curtis, C.A.2    Hulme, E.C.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.