| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370078 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
Abstract
The seminal human dopamine D3 receptor (hD3R) ligand BP 897 has shown interesting properties during clinical trials. However, its lack of selectivity towards human adrenergic receptor impedes further development. Two approaches were followed to increase hD3R selectivity. The lead optimisation succeeded, we disclose here ligands with subnanomolar potency for D3R, combined with a good selectivity for the closely related human dopamine D2 and human adrenergic alpha-1 receptors.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Marc Capet, Thierry Calmels, Nicolas Levoin, Denis Danvy, Isabelle Berrebi-Bertrand, Holger Stark, Jean-Charles Schwartz, Jeanne-Marie Lecomte,