Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand |
| |
Authors: | Macchia B Cervetto L Demontis G C Domiano P Longoni B Macchia M Minutolo F Orlandini E Ortore G Papi C |
| |
Affiliation: | Dipartimento di Scienze Farmaceutiche, Università di Pisa, Italy. bmacchia@farm.unipi.it |
| |
Abstract: | The synthesis of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine 1, a potent and selective D4 dopaminergic ligand, was performed. The 3-(3,4-dimethylphenyl)- 1-propylpiperidine with the R configuration showed an affinity for the D4 receptors 6-fold higher than the corresponding enantiomer with the S configuration. Furthermore, the (R)-1 enantiomer proved to be highly selective for D4 receptors with respect to D2-D3 receptors, with a Ki ratio higher than 25,000, while the (S)-1 enantiomer was about 100-fold less selective than the (R)-1 one. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|