The dopamine receptor type 3 (D3R) has been focused as an important drug target for diagnosis and/or treatment of CNS disorders because its abnormality relates to various neuropsychiatric disorders such as schizophrenia, Parkinson’s disease, and drug addiction. However, the development of D3R ligands with high affinity and selectivity to the receptor is not satisfactory because of high sequence homology (78%) of D2R and D3R. Moreover, serotonin 5-HT1A receptors widely distributed in the brain can disturb the specific binding of D3R ligands. In this study, we developed a series of substituted N-phenylpiperazine analogs with thiophenyl or thazolyl benzamide to get a potent D3R selective ligand. We will describe the synthesis, evaluation, and structural-activity relationship of these compounds having a high affinity and high selectivity for D3R versus D2R, but a low affinity for 5-HT1A receptors.

Development of substituted N-phenylpiperazine analogs for dopamine D3 receptor specific ligands with low affinities to D2 and 5-HT1A receptors

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.