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The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.
Holmes, Ian P; Blunt, Richard J; Lorthioir, Olivier E; Blowers, Stephen M; Gribble, Andy; Payne, Andrew H; Stansfield, Ian G; Wood, Martyn; Woollard, Patrick M; Reavill, Charlie; Howes, Claire M; Micheli, Fabrizio; Di Fabio, Romano; Donati, Daniele; Terreni, Silvia; Hamprecht, Dieter; Arista, Luca; Worby, Angela; Watson, Steve P.
Bioorg Med Chem Lett ; 20(6): 2013-6, 2010 Mar 15.
Article in English | MEDLINE | ID: mdl-20153647

ABSTRACT

The identification of a highly selective D(2) partial agonist, D(3) antagonist tool molecule which demonstrates high levels of brain exposure and selectivity against an extensive range of dopamine, serotonin, adrenergic, histamine, and muscarinic receptors is described.


Subject(s)
Brain/drug effects , Dopamine Agonists/pharmacology , Dopamine Antagonists/pharmacology , Receptors, Dopamine D2/agonists , Receptors, Dopamine D3/antagonists & inhibitors , Animals , Brain/metabolism
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