title: Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.
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.
authors: Pharma Research, F. Hoffmann-La Roche Ltd, 4070 Basel, Switzerland.
authors: Jens-Uwe
authors: JU
authors: Peters
authors: Holger
authors: H
authors: Kühne
authors: Henrietta
authors: H
authors: Dehmlow
authors: Uwe
authors: U
authors: Grether
authors: Aurelia
authors: A
authors: Conte
authors: Dominik
authors: D
authors: Hainzl
authors: Cornelia
authors: C
authors: Hertel
authors: Nicole A
authors: NA
authors: Kratochwil
authors: Michael
authors: M
authors: Otteneder
authors: Robert
authors: R
authors: Narquizian
authors: Constantinos G
authors: CG
authors: Panousis
authors: Fabienne
authors: F
authors: Ricklin
authors: Stephan
authors: S
authors: Röver
mesh_terms: D000818:Animals; D008862:Microsomes, Liver / Q000378:metabolism; D009525:Niacin / Q000378:metabolism*; D011744:Pyrimidinones / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism*; D011978:Receptors, Nicotinic / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: C530636:HCAR2 protein, human; C554445:Hcar2 protein, rat; D011744:Pyrimidinones; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D009525:Niacin