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

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

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

The identification of a hitherto unprecedented pharmacology in a compound (3) displaying highly selective DA D2 partial agonism and DA D3 antagonism, but devoid of activity at other aminergic receptors is described.

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关键词

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

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