Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part one: lead identification

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4799-801. doi: 10.1016/j.bmcl.2009.06.043. Epub 2009 Jun 14.

Authors

Ian P Holmes¹, Fabrizio Micheli, Simon Gaines, Olivier Lorthioir, Steve P Watson, Romano Di Fabio, Gabriella Gentile, Christian Heidbreder, Chiara Savoia, Angela Worby

Affiliation

¹ Cancer Therapeutics, Melbourne, Australia.

PMID: 19560918
DOI: 10.1016/j.bmcl.2009.06.043

Abstract

The synthesis and SAR of a new series of potent and selective dopamine D(3) receptor antagonists is reported.

MeSH terms

Animals
Cats
Ether-A-Go-Go Potassium Channels / metabolism
Humans
Imidazolidines / chemical synthesis
Imidazolidines / chemistry*
Imidazolidines / pharmacology
Ligands
Positron-Emission Tomography*
Receptors, Dopamine D3 / antagonists & inhibitors*
Receptors, Dopamine D3 / metabolism
Structure-Activity Relationship

Substances

Ether-A-Go-Go Potassium Channels
Imidazolidines
KCNH1 protein, human
Ligands
Receptors, Dopamine D3