The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 6, 2010, Pages 2013-2016

  Holmes, Ian P ^a   Blunt, Richard J ^a   Lorthioir, Olivier E ^a   Blowers, Stephen M ^a   Gribble, Andy ^a   Payne, Andrew H ^a   Stansfield, Ian G ^a   Wood, Martyn ^a   Woollard, Patrick M ^a   Reavill, Charlie ^a   Howes, Claire M ^a   Micheli, Fabrizio ^b   Fabio, Romano Di ^b   Donati, Daniele ^b   Terreni, Silvia ^b   Hamprecht, Dieter ^b   Arista, Luca ^b   Worby, Angela ^c   Watson, Steve P ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b Medicines Research Centre   (Italy)

^c Molecular Discovery Research   (United Kingdom)

Author keywords

Aripiprazole; DA D2; DA D3; Dopamine antagonist; Dopamine partial agonist

Indexed keywords

ADRENERGIC RECEPTOR; ARIPIPRAZOLE; DOPAMINE 2 RECEPTOR STIMULATING AGENT; DOPAMINE 3 RECEPTOR BLOCKING AGENT; DOPAMINE RECEPTOR; HISTAMINE RECEPTOR; IMIDAZOLE DERIVATIVE; IMIDAZOLIDINONE; MUSCARINIC RECEPTOR; PIPERIDINE DERIVATIVE; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; SEROTONIN RECEPTOR; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BRAIN; CONTROLLED STUDY; DRUG EXPOSURE; DRUG IDENTIFICATION; DRUG SELECTIVITY; LIVER MICROSOME; NONHUMAN; RAT; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION;

ANIMALS; BRAIN; DOPAMINE AGONISTS; DOPAMINE ANTAGONISTS; RECEPTORS, DOPAMINE D2; RECEPTORS, DOPAMINE D3;

EID: 77549083431     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.01.090     Document Type: Article

References (10)

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