Bioorg Med Chem Lett. 2010 Mar 15;20(6):2013-6. doi: 10.1016/j.bmcl.2010.01.090. Epub 2010 Jan 25.

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

Holmes IP, Blunt RJ, Lorthioir OE, Blowers SM, Gribble A, Payne AH, Stansfield IG, Wood M, Woollard PM, Reavill C, Howes CM, Micheli F, Di Fabio R, Donati D, Terreni S, Hamprecht D, Arista L, Worby A, Watson SP.

Source

GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.

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.

PMID:: 20153647; [PubMed - indexed for MEDLINE]

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The identification of a selective dopamine D2 partial agonist, D3 antagonist dis...
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 .

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