Novel,potent, selective,and brain penetrant phosphodiesterase 10A inhibitors |
| |
| Authors: | Hervé Geneste Karla Drescher Clarissa Jakob Loïc Laplanche Michael Ochse Maricel Torrent |
| |
| Affiliation: | 1. AbbVie Deutschland GmbH & Co. KG, Neuroscience Research, D-67008 Ludwigshafen, Germany;2. AbbVie, Structural Biology, IL 60064-6101, USA;3. AbbVie Deutschland GmbH & Co. KG, DMPK, D-67008 Ludwigshafen, Germany |
| |
| Abstract: | ![]()
Herein we report the discovery of a novel series of phosphodiesterase 10A inhibitors. Optimization of a HTS hit (17) resulted in potent, selective, and brain penetrant 23 and 26; both exhibited much lower clearance in vivo and decreased volume of distribution (rat PK) and have thus the potential to inhibit the PDE10A target in vivo at a lower efficacious dose than the reference compound WEB-3. |
| |
| Keywords: | Phosphodiesterase PDE10A WEB-3 |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
