title: Characterization of RO4583298 as a novel potent, dual antagonist with in vivo activity at tachykinin NK₁ and NK₃ receptors.
authors.affiliation: Discovery Research CNS, F. Hoffmann-La Roche Ltd., Basel, Switzerland. parichehr.malherbe@roche.com
authors.forename: P
authors.initials: P
authors.lastname: Malherbe
authors.forename: F
authors.initials: F
authors.lastname: Knoflach
authors.forename: M C
authors.initials: MC
authors.lastname: Hernandez
authors.forename: T
authors.initials: T
authors.lastname: Hoffmann
authors.forename: P
authors.initials: P
authors.lastname: Schnider
authors.forename: R H
authors.initials: RH
authors.lastname: Porter
authors.forename: J G
authors.initials: JG
authors.lastname: Wettstein
authors.forename: T M
authors.initials: TM
authors.lastname: Ballard
authors.forename: W
authors.initials: W
authors.lastname: Spooren
authors.forename: L
authors.initials: L
authors.lastname: Steward
mesh_terms: D000200:Action Potentials / Q000187:drug effects; D000577:Amides / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D000631:Aminopyridines; D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D044482:Benzeneacetamides; D004305:Dose-Response Relationship, Drug; D005260:Female; D005849:Gerbillinae; D006168:Guinea Pigs; D057809:HEK293 Cells; D006801:Humans; D066298:In Vitro Techniques; D007294:Inositol / Q000378:metabolism; D008024:Ligands; D008252:Macaca fascicularis; D008297:Male; D008636:Mesencephalon / Q000187:drug effects* / Q000502:physiology; D051379:Mice; D064729:Neurokinin-1 Receptor Antagonists; D009474:Neurons / Q000187:drug effects / Q000502:physiology; D010766:Phosphorylation / Q000187:drug effects; D011725:Pyridines / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D018040:Receptors, Neurokinin-1 / Q000819:agonists / Q000235:genetics / Q000378:metabolism; D018042:Receptors, Neurokinin-3 / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D012559:Schizophrenia / Q000188:drug therapy; D013373:Substance P / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors; D013378:Substantia Nigra / Q000187:drug effects / Q000502:physiology
chemical_list: C558113:2-(3,5-bis-trifluoromethylphenyl)-N-(4-(4-fluoro-2-methylphenyl)-6-(3-hydroxy-2-hydroxymethylpyrrolidin-1-yl)pyridin-3-yl)-N-methylisobutyramide; D000577:Amides; D000631:Aminopyridines; D014150:Antipsychotic Agents; D044482:Benzeneacetamides; D008024:Ligands; D064729:Neurokinin-1 Receptor Antagonists; D011725:Pyridines; D018040:Receptors, Neurokinin-1; D018042:Receptors, Neurokinin-3; D013373:Substance P; D007294:Inositol