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

doi:10.1016/j.bmcl.2010.01.090

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. Epub 2010 Jan 25.

Affiliation

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.

MeSH terms

Animals
Brain / drug effects*
Brain / metabolism
Dopamine Agonists / pharmacology*
Dopamine Antagonists / pharmacology*
Receptors, Dopamine D2 / agonists*
Receptors, Dopamine D3 / antagonists & inhibitors*

Substances

Dopamine Agonists
Dopamine Antagonists
Receptors, Dopamine D2
Receptors, Dopamine D3