title: The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function.
abstract: The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Thomas
authors.initials: T
authors.lastname: Jensen
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Lisbeth
authors.initials: L
authors.lastname: Elster
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Søren Møller
authors.initials: SM
authors.lastname: Nielsen
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Suresh Babu
authors.initials: SB
authors.lastname: Poda
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Frosty
authors.initials: F
authors.lastname: Loechel
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Christiane
authors.initials: C
authors.lastname: Volbracht
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Ib Vestergaard
authors.initials: IV
authors.lastname: Klewe
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Laurent
authors.initials: L
authors.lastname: David
authors.affiliation: Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
authors.forename: Stephen P
authors.initials: SP
authors.lastname: Watson
mesh_terms: D000818:Animals; D054314:Drug Inverse Agonism; D051379:Mice; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors* / Q000502:physiology*; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology
chemical_list: C494613:GPR3 protein, mouse; D011743:Pyrimidines; D043562:Receptors, G-Protein-Coupled; D014230:Triazoles; C030986:pyrimidine
keywords: AF64394; G protein coupled receptor; GPR12; GPR3; GPR6; Inverse agonist; Orphan receptor