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. 2011 May 1;21(9):2621-5.
doi: 10.1016/j.bmcl.2011.01.059. Epub 2011 Jan 22.

Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder

Douglas S Johnson  1 , Chung Choi, Lorraine K Fay, David A Favor, Joseph T Repine, Andrew D White, Hyacinth C Akunne, Lawrence Fitzgerald, Kim Nicholls, Bradley J Snyder, Steven Z Whetzel, Liming Zhang, Kevin A Serpa
Affiliations

Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder

Douglas S Johnson et al. Bioorg Med Chem Lett. .

Abstract

The synthesis and structure-activity relationship (SAR) of a novel series of aryl piperazine napthyridinone D(2) partial agonists is described. Our goal was to optimize the affinities for the D(2), 5-HT(2A) and 5-HT(1A) receptors, such that the D(2)/5-HT(2A) ratio was greater than 5 to ensure maximal occupancy of these receptors when the D(2) occupancy reached efficacious levels. This strategy led to identification of PF-00217830 (2) with robust inhibition of sLMA (MED=0.3mg/kg) and DOI-induced head twitches in rats (31% and 78% at 0.3 and 1mg/kg) with no catalepsy observed at the highest dose tested (10 mg/kg).

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