Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371956 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
Abstract
The identification of a highly selective D2 partial agonist, D3 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.
Graphical abstractThe identification of a hitherto unprecedented pharmacology in a compound (3) displaying highly selective DA D2 partial agonism and DA D3 antagonism, but devoid of activity at other aminergic receptors is described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,