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

  • Bioorg Med Chem Lett. 2010 Mar 15;20(6):2013-6. doi: 10.1016/j.bmcl.2010.01.090.
Ian P Holmes  1 ,  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
Affiliations
  • 1. GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.
PMID: 20153647 DOI: 10.1016/j.bmcl.2010.01.090
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.

Products