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Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: Optimization of in vitro activity |
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| Authors: | Jens-Uwe Peters Holger Kühne Henrietta Dehmlow Uwe Grether Aurelia Conte Dominik Hainzl Cornelia Hertel Nicole A. Kratochwil Michael Otteneder Robert Narquizian Constantinos G. Panousis Fabienne Ricklin Stephan Röver |
| Affiliation: | 1. Pharma Research, F. Hoffmann-La Roche Ltd, 4070 Basel, Switzerland;2. Pharma Research, F. Hoffmann-La Roche Ltd, Nutley, NJ 07110, USA |
| Abstract: | Pyrido pyrimidinones are selective agonists of the human high affinity niacin receptor GPR109A (HM74A). They show no activity on the highly homologous low affinity receptor GPR109B (HM74). Starting from a high throughput screening hit the in vitro activity of the pyrido pyrimidinones was significantly improved providing lead compounds suitable for further optimization. |
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