The identification of a selective dopamine D sub(2) partial agonist, D sub(3) antagonist displaying high levels of brain exposure

The identification of a highly selective D sub(2) partial agonist, D sub(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. AB:

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (6), p.2013-2016
Hauptverfasser: 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
Format: Artikel
Sprache:eng
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Zusammenfassung:The identification of a highly selective D sub(2) partial agonist, D sub(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. AB:
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.01.090