Christopoulos A

General

Full name : Christopoulos Arthur

First name : Arthur

Mail : Monash Institute of Pharmaceutical Sciences, Monash University, Drug Discovery Biology and Dept. of Pharmacology 399 Royal Parade, Parkville, Victoria, 3052

Zip Code :

City :

Country : Australia

Email : arthur.christopoulos@monash.edu

Phone :

Fax :

Website : \/\/www.monash.edu.au\/pharm\/research\/researchers\/profile.html?sid=9159&pid=4119

Directory :

References (82)

Title : From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease - Brown_2021_Cell_184_5886
Author(s) : Brown AJH , Bradley SJ , Marshall FH , Brown GA , Bennett KA , Brown J , Cansfield JE , Cross DM , de Graaf C , Hudson BD , Dwomoh L , Dias JM , Errey JC , Hurrell E , Liptrot J , Mattedi G , Molloy C , Nathan PJ , Okrasa K , Osborne G , Patel JC , Pickworth M , Robertson N , Shahabi S , Bundgaard C , Phillips K , Broad LM , Goonawardena AV , Morairty SR , Browning M , Perini F , Dawson GR , Deakin JFW , Smith RT , Sexton PM , Warneck J , Vinson M , Tasker T , Tehan BG , Teobald B , Christopoulos A , Langmead CJ , Jazayeri A , Cooke RM , Rucktooa P , Congreve MS , Weir M , Tobin AB
Ref : Cell , 184 :5886 , 2021
Abstract :
PubMedSearch : Brown_2021_Cell_184_5886
PubMedID: 34822784

Title : Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs - Bradley_2020_Nat.Chem.Biol_16_240
Author(s) : Bradley SJ , Molloy C , Valuskova P , Dwomoh L , Scarpa M , Rossi M , Finlayson L , Svensson KA , Chernet E , Barth VN , Gherbi K , Sykes DA , Wilson CA , Mistry R , Sexton PM , Christopoulos A , Mogg AJ , Rosethorne EM , Sakata S , John Challiss RA , Broad LM , Tobin AB
Ref : Nat Chemical Biology , 16 :240 , 2020
Abstract :
PubMedSearch : Bradley_2020_Nat.Chem.Biol_16_240
PubMedID: 32080630

Title : THE CONCISE GUIDE TO PHARMACOLOGY 2017\/18: Overview - Alexander_2017_Br.J.Pharmacol_174 Suppl 1_S1
Author(s) : Alexander SP , Kelly E , Marrion NV , Peters JA , Faccenda E , Harding SD , Pawson AJ , Sharman JL , Southan C , Buneman OP , Cidlowski JA , Christopoulos A , Davenport AP , Fabbro D , Spedding M , Striessnig J , Davies JA
Ref : British Journal of Pharmacology , 174 Suppl 1 :S1 , 2017
Abstract :
PubMedSearch : Alexander_2017_Br.J.Pharmacol_174 Suppl 1_S1
PubMedID: 29055037

Title : M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss - Bradley_2017_J.Clin.Invest_127_487
Author(s) : Bradley SJ , Bourgognon JM , Sanger HE , Verity N , Mogg AJ , White DJ , Butcher AJ , Moreno JA , Molloy C , Macedo-Hatch T , Edwards JM , Wess J , Pawlak R , Read DJ , Sexton PM , Broad LM , Steinert JR , Mallucci GR , Christopoulos A , Felder CC , Tobin AB
Ref : J Clinical Investigation , 127 :487 , 2017
Abstract :
PubMedSearch : Bradley_2017_J.Clin.Invest_127_487
PubMedID: 27991860

Title : Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation - Changeux_2016_Cell_166_1084
Author(s) : Changeux JP , Christopoulos A
Ref : Cell , 166 :1084 , 2016
Abstract :
PubMedSearch : Changeux_2016_Cell_166_1084
PubMedID: 27565340

Title : Muscarinic acetylcholine receptors: novel opportunities for drug development - Kruse_2014_Nat.Rev.Drug.Discov_13_549
Author(s) : Kruse AC , Kobilka BK , Gautam D , Sexton PM , Christopoulos A , Wess J
Ref : Nat Rev Drug Discov , 13 :549 , 2014
Abstract :
PubMedSearch : Kruse_2014_Nat.Rev.Drug.Discov_13_549
PubMedID: 24903776

Title : Molecular determinants of allosteric modulation at the m1 muscarinic acetylcholine receptor - Abdul-Ridha_2014_J.Biol.Chem_289_6067
Author(s) : Abdul-Ridha A , Lopez L , Keov P , Thal DM , Mistry SN , Sexton PM , Lane JR , Canals M , Christopoulos A
Ref : Journal of Biological Chemistry , 289 :6067 , 2014
Abstract :
PubMedSearch : Abdul-Ridha_2014_J.Biol.Chem_289_6067
PubMedID: 24443568

Title : Development of a photoactivatable allosteric ligand for the m1 muscarinic acetylcholine receptor - Davie_2014_ACS.Chem.Neurosci_5_902
Author(s) : Davie BJ , Sexton PM , Capuano B , Christopoulos A , Scammells PJ
Ref : ACS Chem Neurosci , 5 :902 , 2014
Abstract :
PubMedSearch : Davie_2014_ACS.Chem.Neurosci_5_902
PubMedID: 25188871

Title : Activation and allosteric modulation of a muscarinic acetylcholine receptor - Kruse_2013_Nature_504_101
Author(s) : Kruse AC , Ring AM , Manglik A , Hu J , Hu K , Eitel K , Hubner H , Pardon E , Valant C , Sexton PM , Christopoulos A , Felder CC , Gmeiner P , Steyaert J , Weis WI , Garcia KC , Wess J , Kobilka BK
Ref : Nature , 504 :101 , 2013
Abstract :
PubMedSearch : Kruse_2013_Nature_504_101
PubMedID: 24256733

Title : Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor - Mistry_2013_J.Med.Chem_56_5151
Author(s) : Mistry SN , Valant C , Sexton PM , Capuano B , Christopoulos A , Scammells PJ
Ref : Journal of Medicinal Chemistry , 56 :5151 , 2013
Abstract :
PubMedSearch : Mistry_2013_J.Med.Chem_56_5151
PubMedID: 23718562

Title : Allosteric modulation of a chemogenetically modified G protein-coupled receptor - Abdul-Ridha_2013_Mol.Pharmacol_83_521
Author(s) : Abdul-Ridha A , Lane JR , Sexton PM , Canals M , Christopoulos A
Ref : Molecular Pharmacology , 83 :521 , 2013
Abstract :
PubMedSearch : Abdul-Ridha_2013_Mol.Pharmacol_83_521
PubMedID: 23197649

Title : Probing structural requirements of positive allosteric modulators of the m4 muscarinic receptor - Huynh_2013_J.Med.Chem_56_8196
Author(s) : Huynh T , Valant C , Crosby IT , Sexton PM , Christopoulos A , Capuano B
Ref : Journal of Medicinal Chemistry , 56 :8196 , 2013
Abstract :
PubMedSearch : Huynh_2013_J.Med.Chem_56_8196
PubMedID: 24074052

Title : Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits - Davie_2013_ACS.Chem.Neurosci_4_1026
Author(s) : Davie BJ , Christopoulos A , Scammells PJ
Ref : ACS Chem Neurosci , 4 :1026 , 2013
Abstract :
PubMedSearch : Davie_2013_ACS.Chem.Neurosci_4_1026
PubMedID: 23659787

Title : Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M(1) muscarinic acetylcholine receptor - Keov_2013_Mol.Pharmacol_84_425
Author(s) : Keov P , Valant C , Devine SM , Lane JR , Scammells PJ , Sexton PM , Christopoulos A
Ref : Molecular Pharmacology , 84 :425 , 2013
Abstract :
PubMedSearch : Keov_2013_Mol.Pharmacol_84_425
PubMedID: 23798605

Title : Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs - Dror_2013_Nature_503_295
Author(s) : Dror RO , Green HF , Valant C , Borhani DW , Valcourt JR , Pan AC , Arlow DH , Canals M , Lane JR , Rahmani R , Baell JB , Sexton PM , Christopoulos A , Shaw DE
Ref : Nature , 503 :295 , 2013
Abstract :
PubMedSearch : Dror_2013_Nature_503_295
PubMedID: 24121438

Title : Structure-function studies of muscarinic acetylcholine receptors - Leach_2012_Handb.Exp.Pharmacol_208_29
Author(s) : Leach K , Simms J , Sexton PM , Christopoulos A
Ref : Handbook of Experimental Pharmacology , :29 , 2012
Abstract :
PubMedSearch : Leach_2012_Handb.Exp.Pharmacol_208_29
PubMedID: 22222693

Title : A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation - Canals_2012_J.Biol.Chem_287_650
Author(s) : Canals M , Lane JR , Wen A , Scammells PJ , Sexton PM , Christopoulos A
Ref : Journal of Biological Chemistry , 287 :650 , 2012
Abstract :
PubMedSearch : Canals_2012_J.Biol.Chem_287_650
PubMedID: 22086918

Title : Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor - Gregory_2012_J.Biol.Chem_287_37066
Author(s) : Gregory KJ , Sexton PM , Tobin AB , Christopoulos A
Ref : Journal of Biological Chemistry , 287 :37066 , 2012
Abstract :
PubMedSearch : Gregory_2012_J.Biol.Chem_287_37066
PubMedID: 22965232

Title : Allosteric modulation of endogenous metabolites as an avenue for drug discovery - Wootten_2012_Mol.Pharmacol_82_281
Author(s) : Wootten D , Savage EE , Valant C , May LT , Sloop KW , Ficorilli J , Showalter AD , Willard FS , Christopoulos A , Sexton PM
Ref : Molecular Pharmacology , 82 :281 , 2012
Abstract :
PubMedSearch : Wootten_2012_Mol.Pharmacol_82_281
PubMedID: 22576254

Title : A simple method for quantifying functional selectivity and agonist bias - Kenakin_2012_ACS.Chem.Neurosci_3_193
Author(s) : Kenakin T , Watson C , Muniz-Medina V , Christopoulos A , Novick S
Ref : ACS Chem Neurosci , 3 :193 , 2012
Abstract :
PubMedSearch : Kenakin_2012_ACS.Chem.Neurosci_3_193
PubMedID: 22860188

Title : Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects - Valant_2012_Mol.Pharmacol_81_41
Author(s) : Valant C , Felder CC , Sexton PM , Christopoulos A
Ref : Molecular Pharmacology , 81 :41 , 2012
Abstract :
PubMedSearch : Valant_2012_Mol.Pharmacol_81_41
PubMedID: 21989256

Title : Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery -
Author(s) : Melancon BJ , Hopkins CR , Wood MR , Emmitte KA , Niswender CM , Christopoulos A , Conn PJ , Lindsley CW
Ref : Journal of Medicinal Chemistry , 55 :1445 , 2012
PubMedID: 22148748

Title : Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor - Suratman_2011_Br.J.Pharmacol_162_1659
Author(s) : Suratman S , Leach K , Sexton P , Felder CC , Loiacono R , Christopoulos A
Ref : British Journal of Pharmacology , 162 :1659 , 2011
Abstract :
PubMedSearch : Suratman_2011_Br.J.Pharmacol_162_1659
PubMedID: 21198541

Title : The role of transmembrane domain 3 in the actions of orthosteric, allosteric, and atypical agonists of the M4 muscarinic acetylcholine receptor - Leach_2011_Mol.Pharmacol_79_855
Author(s) : Leach K , Davey AE , Felder CC , Sexton PM , Christopoulos A
Ref : Molecular Pharmacology , 79 :855 , 2011
Abstract :
PubMedSearch : Leach_2011_Mol.Pharmacol_79_855
PubMedID: 21300722

Title : The effect of social isolation on rat brain expression of genes associated with endocannabinoid signaling - Robinson_2010_Brain.Res_1343_153
Author(s) : Robinson SA , Loiacono RE , Christopoulos A , Sexton PM , Malone DT
Ref : Brain Research , 1343 :153 , 2010
Abstract :
PubMedSearch : Robinson_2010_Brain.Res_1343_153
PubMedID: 20430015

Title : Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms - Nawaratne_2010_J.Biol.Chem_285_19012
Author(s) : Nawaratne V , Leach K , Felder CC , Sexton PM , Christopoulos A
Ref : Journal of Biological Chemistry , 285 :19012 , 2010
Abstract :
PubMedSearch : Nawaratne_2010_J.Biol.Chem_285_19012
PubMedID: 20406819

Title : Detection of novel functional selectivity at M3 muscarinic acetylcholine receptors using a Saccharomyces cerevisiae platform - Stewart_2010_ACS.Chem.Biol_5_365
Author(s) : Stewart GD , Sexton PM , Christopoulos A
Ref : ACS Chemical Biology , 5 :365 , 2010
Abstract :
PubMedSearch : Stewart_2010_ACS.Chem.Biol_5_365
PubMedID: 20155933

Title : Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias - Gregory_2010_J.Biol.Chem_285_7459
Author(s) : Gregory KJ , Hall NE , Tobin AB , Sexton PM , Christopoulos A
Ref : Journal of Biological Chemistry , 285 :7459 , 2010
Abstract :
PubMedSearch : Gregory_2010_J.Biol.Chem_285_7459
PubMedID: 20051519

Title : Prediction of functionally selective allosteric interactions at an M3 muscarinic acetylcholine receptor mutant using Saccharomyces cerevisiae - Stewart_2010_Mol.Pharmacol_78_205
Author(s) : Stewart GD , Sexton PM , Christopoulos A
Ref : Molecular Pharmacology , 78 :205 , 2010
Abstract :
PubMedSearch : Stewart_2010_Mol.Pharmacol_78_205
PubMedID: 20466821

Title : Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor - Avlani_2010_Mol.Pharmacol_78_94
Author(s) : Avlani VA , Langmead CJ , Guida E , Wood MD , Tehan BG , Herdon HJ , Watson JM , Sexton PM , Christopoulos A
Ref : Molecular Pharmacology , 78 :94 , 2010
Abstract :
PubMedSearch : Avlani_2010_Mol.Pharmacol_78_94
PubMedID: 20413650

Title : Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties - Leach_2010_Neuropsychopharmacology_35_855
Author(s) : Leach K , Loiacono RE , Felder CC , McKinzie DL , Mogg A , Shaw DB , Sexton PM , Christopoulos A
Ref : Neuropsychopharmacology , 35 :855 , 2010
Abstract :
PubMedSearch : Leach_2010_Neuropsychopharmacology_35_855
PubMedID: 19940843

Title : Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity - Antony_2009_FASEB.J_23_442
Author(s) : Antony J , Kellershohn K , Mohr-Andra M , Kebig A , Prilla S , Muth M , Heller E , Disingrini T , Dallanoce C , Bertoni S , Schrobang J , Trankle C , Kostenis E , Christopoulos A , Holtje HD , Barocelli E , De Amici M , Holzgrabe U , Mohr K
Ref : FASEB Journal , 23 :442 , 2009
Abstract :
PubMedSearch : Antony_2009_FASEB.J_23_442
PubMedID: 18842964

Title : Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity - Stewart_2009_J.Pharmacol.Exp.Ther_331_277
Author(s) : Stewart GD , Valant C , Dowell SJ , Mijaljica D , Devenish RJ , Scammells PJ , Sexton PM , Christopoulos A
Ref : Journal of Pharmacology & Experimental Therapeutics , 331 :277 , 2009
Abstract :
PubMedSearch : Stewart_2009_J.Pharmacol.Exp.Ther_331_277
PubMedID: 19641164

Title : Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa - Mansfield_2009_J.Pharmacol.Exp.Ther_328_893
Author(s) : Mansfield KJ , Chandran JJ , Vaux KJ , Millard RJ , Christopoulos A , Mitchelson FJ , Burcher E
Ref : Journal of Pharmacology & Experimental Therapeutics , 328 :893 , 2009
Abstract :
PubMedSearch : Mansfield_2009_J.Pharmacol.Exp.Ther_328_893
PubMedID: 19029429

Title : A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric\/allosteric ligand - Valant_2008_J.Biol.Chem_283_29312
Author(s) : Valant C , Gregory KJ , Hall NE , Scammells PJ , Lew MJ , Sexton PM , Christopoulos A
Ref : Journal of Biological Chemistry , 283 :29312 , 2008
Abstract :
PubMedSearch : Valant_2008_J.Biol.Chem_283_29312
PubMedID: 18723515

Title : New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug) - Nawaratne_2008_Mol.Pharmacol_74_1119
Author(s) : Nawaratne V , Leach K , Suratman N , Loiacono RE , Felder CC , Armbruster BN , Roth BL , Sexton PM , Christopoulos A
Ref : Molecular Pharmacology , 74 :1119 , 2008
Abstract :
PubMedSearch : Nawaratne_2008_Mol.Pharmacol_74_1119
PubMedID: 18628403

Title : Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia - Chan_2008_Proc.Natl.Acad.Sci.U.S.A_105_10978
Author(s) : Chan WY , McKinzie DL , Bose S , Mitchell SN , Witkin JM , Thompson RC , Christopoulos A , Lazareno S , Birdsall NJ , Bymaster FP , Felder CC
Ref : Proc Natl Acad Sci U S A , 105 :10978 , 2008
Abstract :
PubMedSearch : Chan_2008_Proc.Natl.Acad.Sci.U.S.A_105_10978
PubMedID: 18678919

Title : The impact of orthosteric radioligand depletion on the quantification of allosteric modulator interactions - Avlani_2008_J.Pharmacol.Exp.Ther_325_927
Author(s) : Avlani VA , McLoughlin DJ , Sexton PM , Christopoulos A
Ref : Journal of Pharmacology & Experimental Therapeutics , 325 :927 , 2008
Abstract :
PubMedSearch : Avlani_2008_J.Pharmacol.Exp.Ther_325_927
PubMedID: 18322151

Title : Involvement of the sigma1 (sigma1) receptor in the anti-amnesic, but not antidepressant-like, effects of the aminotetrahydrofuran derivative ANAVEX1-41 - Espallergues_2007_Br.J.Pharmacol_152_267
Author(s) : Espallergues J , Lapalud P , Christopoulos A , Avlani VA , Sexton PM , Vamvakides A , Maurice T
Ref : British Journal of Pharmacology , 152 :267 , 2007
Abstract :
PubMedSearch : Espallergues_2007_Br.J.Pharmacol_152_267
PubMedID: 17641675

Title : Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands - Avlani_2007_J.Biol.Chem_282_25677
Author(s) : Avlani VA , Gregory KJ , Morton CJ , Parker MW , Sexton PM , Christopoulos A
Ref : Journal of Biological Chemistry , 282 :25677 , 2007
Abstract :
PubMedSearch : Avlani_2007_J.Biol.Chem_282_25677
PubMedID: 17591774

Title : Allosteric modulation of muscarinic acetylcholine receptors - Gregory_2007_Curr.Neuropharmacol_5_157
Author(s) : Gregory KJ , Sexton PM , Christopoulos A
Ref : Curr Neuropharmacol , 5 :157 , 2007
Abstract :
PubMedSearch : Gregory_2007_Curr.Neuropharmacol_5_157
PubMedID: 19305798

Title : Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors - May_2007_Mol.Pharmacol_72_463
Author(s) : May LT , Avlani VA , Langmead CJ , Herdon HJ , Wood MD , Sexton PM , Christopoulos A
Ref : Molecular Pharmacology , 72 :463 , 2007
Abstract :
PubMedSearch : May_2007_Mol.Pharmacol_72_463
PubMedID: 17525129

Title : 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_2006_Mol.Pharmacol_69_236
Author(s) : Langmead CJ , Fry VA , Forbes IT , Branch CL , Christopoulos A , Wood MD , Herdon HJ
Ref : Molecular Pharmacology , 69 :236 , 2006
Abstract :
PubMedSearch : Langmead_2006_Mol.Pharmacol_69_236
PubMedID: 16207821

Title : Interaction studies of multiple binding sites on m4 muscarinic acetylcholine receptors - Lanzafame_2006_Mol.Pharmacol_70_736
Author(s) : Lanzafame AA , Sexton PM , Christopoulos A
Ref : Molecular Pharmacology , 70 :736 , 2006
Abstract :
PubMedSearch : Lanzafame_2006_Mol.Pharmacol_70_736
PubMedID: 16709648

Title : Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators - May_2005_J.Pharmacol.Exp.Ther_312_382
Author(s) : May LT , Lin Y , Sexton PM , Christopoulos A
Ref : Journal of Pharmacology & Experimental Therapeutics , 312 :382 , 2005
Abstract :
PubMedSearch : May_2005_J.Pharmacol.Exp.Ther_312_382
PubMedID: 15333678

Title : Investigation of the interaction of a putative allosteric modulator, N-(2,3-diphenyl-1,2,4-thiadiazole-5-(2H)-ylidene) methanamine hydrobromide (SCH-202676), with M1 muscarinic acetylcholine receptors - Lanzafame_2004_J.Pharmacol.Exp.Ther_308_830
Author(s) : Lanzafame A , Christopoulos A
Ref : Journal of Pharmacology & Experimental Therapeutics , 308 :830 , 2004
Abstract :
PubMedSearch : Lanzafame_2004_J.Pharmacol.Exp.Ther_308_830
PubMedID: 14617684

Title : Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors - Avlani_2004_J.Pharmacol.Exp.Ther_308_1062
Author(s) : Avlani V , May LT , Sexton PM , Christopoulos A
Ref : Journal of Pharmacology & Experimental Therapeutics , 308 :1062 , 2004
Abstract :
PubMedSearch : Avlani_2004_J.Pharmacol.Exp.Ther_308_1062
PubMedID: 14711931

Title : Effects of anandamide on the binding and signaling properties of M1 muscarinic acetylcholine receptors - Lanzafame_2004_Biochem.Pharmacol_68_2207
Author(s) : Lanzafame AA , Guida E , Christopoulos A
Ref : Biochemical Pharmacology , 68 :2207 , 2004
Abstract :
PubMedSearch : Lanzafame_2004_Biochem.Pharmacol_68_2207
PubMedID: 15498511

Title : G-protein-coupled receptor allosterism: the promise and the problem(s) - Christopoulos_2004_Biochem.Soc.Trans_32_873
Author(s) : Christopoulos A , May LT , Avlani VA , Sexton PM
Ref : Biochemical Society Transactions , 32 :873 , 2004
Abstract :
PubMedSearch : Christopoulos_2004_Biochem.Soc.Trans_32_873
PubMedID: 15494038

Title : Cellular signaling mechanisms for muscarinic acetylcholine receptors - Lanzafame_2003_Receptors.Channels_9_241
Author(s) : Lanzafame AA , Christopoulos A , Mitchelson F
Ref : Receptors Channels , 9 :241 , 2003
Abstract :
PubMedSearch : Lanzafame_2003_Receptors.Channels_9_241
PubMedID: 12893537

Title : Interaction of anandamide with the M(1) and M(4) muscarinic acetylcholine receptors - Christopoulos_2001_Brain.Res_915_70
Author(s) : Christopoulos A , Wilson K
Ref : Brain Research , 915 :70 , 2001
Abstract :
PubMedSearch : Christopoulos_2001_Brain.Res_915_70
PubMedID: 11578621

Title : The allosteric interaction of otenzepad (AF-DX 116) at muscarinic M2 receptors in guinea pig atria - Lanzafame_2001_Eur.J.Pharmacol_416_235
Author(s) : Lanzafame A , Christopoulos A , Mitchelson F
Ref : European Journal of Pharmacology , 416 :235 , 2001
Abstract :
PubMedSearch : Lanzafame_2001_Eur.J.Pharmacol_416_235
PubMedID: 11290374

Title : From 'captive' agonism to insurmountable antagonism: demonstrating the power of analytical pharmacology - Christopoulos_2001_Clin.Exp.Pharmacol.Physiol_28_223
Author(s) : Christopoulos A
Ref : Clinical & Experimental Pharmacology & Physiology , 28 :223 , 2001
Abstract :
PubMedSearch : Christopoulos_2001_Clin.Exp.Pharmacol.Physiol_28_223
PubMedID: 11236130

Title : Poster: M1 muscarinic receptor-mediated nitric oxide formation modifies agonist signaling: a paradigm of intracellular feedback regulation. -
Author(s) : Christopoulos A , Lanzafame AA
Ref : Life Sciences , 68 :2616 , 2001
PubMedID:

Title : Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists - Christopoulos_2001_J.Pharmacol.Exp.Ther_298_1260
Author(s) : Christopoulos A , Grant MK , Ayoubzadeh N , Kim ON , Sauerberg P , Jeppesen L , El-Fakahany EE
Ref : Journal of Pharmacology & Experimental Therapeutics , 298 :1260 , 2001
Abstract :
PubMedSearch : Christopoulos_2001_J.Pharmacol.Exp.Ther_298_1260
PubMedID: 11504829

Title : Further evidence for the heterogeneity of functional muscarinic receptors in guinea pig gallbladder - Akici_2000_Eur.J.Pharmacol_388_115
Author(s) : Akici A , Karaalp A , Iskender E , Christopoulos A , El-Fakahany EE , Oktay S
Ref : European Journal of Pharmacology , 388 :115 , 2000
Abstract :
PubMedSearch : Akici_2000_Eur.J.Pharmacol_388_115
PubMedID: 10657554

Title : Transducer abstraction: a novel approach to the detection of partial agonist efficacy in radioligand binding studies - Christopoulos_2000_J.Pharmacol.Toxicol.Methods_43_55
Author(s) : Christopoulos A , Grant MK , El-Fakahany EE
Ref : Journal of Pharmacological & Toxicological Methodsods , 43 :55 , 2000
Abstract :
PubMedSearch : Christopoulos_2000_J.Pharmacol.Toxicol.Methods_43_55
PubMedID: 11091130

Title : Pharmacological analysis of the novel mode of interaction between xanomeline and the M1 muscarinic acetylcholine receptor - Christopoulos_1999_J.Pharmacol.Exp.Ther_289_1220
Author(s) : Christopoulos A , Parsons AM , El-Fakahany EE
Ref : Journal of Pharmacology & Experimental Therapeutics , 289 :1220 , 1999
Abstract :
PubMedSearch : Christopoulos_1999_J.Pharmacol.Exp.Ther_289_1220
PubMedID: 10336509

Title : The assessment of antagonist potency under conditions of transient response kinetics - Christopoulos_1999_Eur.J.Pharmacol_382_217
Author(s) : Christopoulos A , Parsons AM , Lew MJ , El-Fakahany EE
Ref : European Journal of Pharmacology , 382 :217 , 1999
Abstract :
PubMedSearch : Christopoulos_1999_Eur.J.Pharmacol_382_217
PubMedID: 10556673

Title : Characterization of the subtype selectivity of the allosteric modulator heptane-1,7-bis-(dimethyl-3'-phthalimidopropyl) ammonium bromide (C7\/3-phth) at cloned muscarinic acetylcholine receptors - Christopoulos_1999_Biochem.Pharmacol_57_171
Author(s) : Christopoulos A , Sorman JL , Mitchelson F , El-Fakahany EE
Ref : Biochemical Pharmacology , 57 :171 , 1999
Abstract :
PubMedSearch : Christopoulos_1999_Biochem.Pharmacol_57_171
PubMedID: 9890565

Title : Poster: The interaction of otenzepad (AF-DX 116) with allosteric modulators and competitive antagonists at a muscarinic M2 receptor -
Author(s) : Mitchelson F , Lanzafame A , Christopoulos A
Ref : Life Sciences , 64 :559 , 1999
PubMedID:

Title : Poster: Pharmacological determination of the interaction of xanomeline with M1 muscarinic acetylcholine receptors -
Author(s) : Parsons AM , Christopoulos A , El-Fakahany EE
Ref : Life Sciences , 64 :578 , 1999
PubMedID:

Title : Poster: A novel and simple approach to detecting partial agonist efficacy in radioligand binding experiments -
Author(s) : Christopoulos A , Grant MK , El-Fakahany EE
Ref : Life Sciences , 64 :568 , 1999
PubMedID:

Title : Poster: Characterization of the subtype selectivity of the allosteric modulator, C7\/3-phth, at cloned muscarinic acetylcholine receptors -
Author(s) : El-Fakahany EE , Christopoulos A , Sorman JL , Mitchelson F
Ref : Life Sciences , 64 :561 , 1999
PubMedID:

Title : Regulation of acetylcholine binding by ATP at the muscarinic M(1) receptor in intact CHO cells - Grant_1999_Brain.Res_839_94
Author(s) : Grant MK , Christopoulos A , El-Fakahany EE
Ref : Brain Research , 839 :94 , 1999
Abstract :
PubMedSearch : Grant_1999_Brain.Res_839_94
PubMedID: 10482803

Title : Poster: Investigation of the multiple agonist affinity states at the M1 muscarinic acetylcholine receptor in intact and broken cell binding experiments -
Author(s) : Grant MK , Christopoulos A , Sorman JL , El-Fakahany EE
Ref : Life Sciences , 64 :567 , 1999
PubMedID:

Title : Use of a spreadsheet to quantitate the equilibrium binding of an allosteric modulator - Christopoulos_1998_Eur.J.Pharmacol_355_103
Author(s) : Christopoulos A , Mitchelson F
Ref : European Journal of Pharmacology , 355 :103 , 1998
Abstract :
PubMedSearch : Christopoulos_1998_Eur.J.Pharmacol_355_103
PubMedID: 9754944

Title : On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor - Christopoulos_1998_Mol.Pharmacol_53_1120
Author(s) : Christopoulos A , Pierce TL , Sorman JL , El-Fakahany EE
Ref : Molecular Pharmacology , 53 :1120 , 1998
Abstract :
PubMedSearch : Christopoulos_1998_Mol.Pharmacol_53_1120
PubMedID: 9614217

Title : Allosteric interactions at muscarinic cholinoceptors - Christopoulos_1998_Clin.Exp.Pharmacol.Physiol_25_185
Author(s) : Christopoulos A , Lanzafame A , Mitchelson F
Ref : Clinical & Experimental Pharmacology & Physiology , 25 :185 , 1998
Abstract :
PubMedSearch : Christopoulos_1998_Clin.Exp.Pharmacol.Physiol_25_185
PubMedID: 9590567

Title : Application of an allosteric ternary complex model to the technique of pharmacological resultant analysis - Christopoulos_1997_J.Pharm.Pharmacol_49_781
Author(s) : Christopoulos A , Mitchelson F
Ref : J Pharm Pharmacol , 49 :781 , 1997
Abstract :
PubMedSearch : Christopoulos_1997_J.Pharm.Pharmacol_49_781
PubMedID: 9379356

Title : Pharmacological analysis of the mode of interaction of McN-A-343 at atrial muscarinic M2 receptors - Christopoulos_1997_Eur.J.Pharmacol_339_153
Author(s) : Christopoulos A , Mitchelson F
Ref : European Journal of Pharmacology , 339 :153 , 1997
Abstract :
PubMedSearch : Christopoulos_1997_Eur.J.Pharmacol_339_153
PubMedID: 9473129

Title : Poster: A common site of action for two allosteric antagonists -
Author(s) : Christopoulos A , Lanzafame A , Mitchelson F
Ref : Life Sciences , 60 :1173 , 1997
PubMedID:

Title : Three allosteric modulators act at a common site, distinct from that of competitive antagonists, at muscarinic acetylcholine M2 receptors - Lanzafame_1997_J.Pharmacol.Exp.Ther_282_278
Author(s) : Lanzafame A , Christopoulos A , Mitchelson F
Ref : Journal of Pharmacology & Experimental Therapeutics , 282 :278 , 1997
Abstract :
PubMedSearch : Lanzafame_1997_J.Pharmacol.Exp.Ther_282_278
PubMedID: 9223565

Title : Interaction of ebeinone, an alkaloid from Fritillaria imperialis, at two muscarinic acetylcholine receptor subtypes - Gilani_1997_Life.Sci_60_535
Author(s) : Gilani AH , Shaheen F , Christopoulos A , Mitchelson F
Ref : Life Sciences , 60 :535 , 1997
Abstract :
PubMedSearch : Gilani_1997_Life.Sci_60_535
PubMedID: 9042388

Title : Novel persistent activation of muscarinic M1 receptors by xanomeline - Christopoulos_1997_Eur.J.Pharmacol_334_R3
Author(s) : Christopoulos A , El-Fakahany EE
Ref : European Journal of Pharmacology , 334 :R3 , 1997
Abstract :
PubMedSearch : Christopoulos_1997_Eur.J.Pharmacol_334_R3
PubMedID: 9346340

Title : Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an infinite dilution procedure - Christopoulos_1997_Biochem.Pharmacol_53_795
Author(s) : Christopoulos A , Lanzafame A , Ziegler A , Mitchelson F
Ref : Biochemical Pharmacology , 53 :795 , 1997
Abstract :
PubMedSearch : Christopoulos_1997_Biochem.Pharmacol_53_795
PubMedID: 9113100

Title : Interactions of agonists with an allosteric antagonist at muscarinic acetylcholine M2 receptors - Lanzafame_1996_Eur.J.Pharmacol_316_27
Author(s) : Lanzafame A , Christopoulos A , Mitchelson F
Ref : European Journal of Pharmacology , 316 :27 , 1996
Abstract :
PubMedSearch : Lanzafame_1996_Eur.J.Pharmacol_316_27
PubMedID: 8982646

Title : [3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators - Christopoulos_1995_Eur.J.Pharmacol_290_259
Author(s) : Christopoulos A , Mitchelson F
Ref : European Journal of Pharmacology , 290 :259 , 1995
Abstract :
PubMedSearch : Christopoulos_1995_Eur.J.Pharmacol_290_259
PubMedID: 7589221

Title : Poster: Concordance between two methods for estimating heterotropic cooperativity at muscarine receptors -
Author(s) : Mitchelson F , Christopoulos A
Ref : Life Sciences , 56(11-12) :1011 , 1995
PubMedID:

Title : Assessment of the allosteric interactions of the bisquaternary heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at M1 and M2 muscarine receptors - Christopoulos_1994_Mol.Pharmacol_46_105
Author(s) : Christopoulos A , Mitchelson F
Ref : Molecular Pharmacology , 46 :105 , 1994
Abstract :
PubMedSearch : Christopoulos_1994_Mol.Pharmacol_46_105
PubMedID: 8058045

Title : Poster: Variations in the degree of allosteric interaction with muscarine receptor antagonists -
Author(s) : Mitchelson F , Christopoulos A
Ref : Life Sciences , 52(5-6) :574 , 1993
PubMedID:

Title : Binding of the muscarine receptor antagonist heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at cholinoceptor sites - Christopoulos_1993_Eur.J.Pharmacol_246_1
Author(s) : Christopoulos A , Loiacono R , Mitchelson F
Ref : European Journal of Pharmacology , 246 :1 , 1993
Abstract :
PubMedSearch : Christopoulos_1993_Eur.J.Pharmacol_246_1
PubMedID: 8354340