Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M 4 muscarinic acetylcholine receptor

British Journal of Pharmacology

Volumn 162, Issue 7, 2011, Pages 1659-1670

  Suratman, S ^a   Leach, K ^a   Sexton, P M ^a   Felder, C C ^b   Loiacono, R E ^a   Christopoulos, A ^a  

^a MONASH UNIVERSITY   (Australia)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

allosteric interaction; antipsychotic; drug discovery; locomotor activity; muscarinic receptors; positive allosteric modulator; positive co operativity; probe dependence; radioligand binding; species variability

Indexed keywords

3 AMINO 5 CHLORO 6 METHOXY 4 METHYL THIENO(2,3 B)PYRIDINE 2 CARBOXYLIC ACID CYCLOPROPYLAMIDE; ACETYLCHOLINE; GLYCOGEN SYNTHASE KINASE 3ALPHA; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); LY 2033298; MITOGEN ACTIVATED PROTEIN KINASE 1; MUSCARINIC AGENT; MUSCARINIC M4 RECEPTOR; OXOTREMORINE; UNCLASSIFIED DRUG; XANOMELINE;

ALLOSTERISM; ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BEHAVIOR DISORDER; BINDING AFFINITY; COMBINATION CHEMOTHERAPY; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENTIATION; DRUG RECEPTOR BINDING; ENZYME PHOSPHORYLATION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LOCOMOTION; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; SPECIES DIFFERENCE; VALIDATION PROCESS;

ACETYLCHOLINE; ALLOSTERIC REGULATION; ALLOSTERIC SITE; ANIMALS; CELL LINE; CHO CELLS; CRICETINAE; CRICETULUS; GLYCOGEN SYNTHASE KINASE 3; HUMANS; LIGANDS; MICE; MITOGEN-ACTIVATED PROTEIN KINASE 1; MITOGEN-ACTIVATED PROTEIN KINASE 3; MOLECULAR PROBE TECHNIQUES; NICOTINIC ACIDS; OXOTREMORINE; PROTEIN BINDING; PYRIDINES; RECEPTOR, MUSCARINIC M4; SPECIES SPECIFICITY; THIADIAZOLES; THIOPHENES;

EID: 79952396557     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2010.01184.x     Document Type: Article

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