title: Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.
abstract: The synthesis and the structure activity of a new series of pyrrolo[1,2-a]pyrazine is reported. These molecules are potent and selective non-competitive mGluR5 antagonists and may shed new light on the pattern of substitution tolerated by this receptor.
authors.affiliation: GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming 4, 37135 Verona, Italy. fm20244@gsk.com
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Micheli
authors.forename: Barbara
authors.initials: B
authors.lastname: Bertani
authors.forename: Andrea
authors.initials: A
authors.lastname: Bozzoli
authors.forename: Luca
authors.initials: L
authors.lastname: Crippa
authors.forename: Paolo
authors.initials: P
authors.lastname: Cavanni
authors.forename: Romano
authors.initials: R
authors.lastname: Di Fabio
authors.forename: Daniele
authors.initials: D
authors.lastname: Donati
authors.forename: Paola
authors.initials: P
authors.lastname: Marzorati
authors.forename: Giancarlo
authors.initials: G
authors.lastname: Merlo
authors.forename: Alfredo
authors.initials: A
authors.lastname: Paio
authors.forename: Lorenzo
authors.initials: L
authors.lastname: Perugini
authors.forename: Paola
authors.initials: P
authors.lastname: Zarantonello
mesh_terms: D050483:Dopamine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors; D005453:Fluorescence; D006801:Humans; D015394:Molecular Structure; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors; D011719:Pyrazines / Q000138:chemical synthesis / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology*; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D050483:Dopamine Plasma Membrane Transport Proteins; C578935:GRM5 protein, human; D050484:Norepinephrine Plasma Membrane Transport Proteins; D011719:Pyrazines; D011758:Pyrroles; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate