title: Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.
abstract: The rational design of a novel series of pyrrolidine derivatives as neurokinin-3 receptor antagonists is reported starting from a selective neurokinin-1 receptor antagonist. Typical representatives in this series showed in vivo efficacy after oral administration in a NK3 mediated functional assay. This series of NK3 antagonists shows promise to deliver a novel antipsychotic.
authors.affiliation: F. Hoffmann-La Roche Ltd, Pharmaceuticals Division, Preclinical Research, CH-4070 Basel, Switzerland. hasane.ratni@roche.com
authors.forename: Hassen
authors.initials: H
authors.lastname: Ratni
authors.forename: Theresa M
authors.initials: TM
authors.lastname: Ballard
authors.forename: Caterina
authors.initials: C
authors.lastname: Bissantz
authors.forename: Torsten
authors.initials: T
authors.lastname: Hoffmann
authors.forename: Philippe
authors.initials: P
authors.lastname: Jablonski
authors.forename: Frederic
authors.initials: F
authors.lastname: Knoflach
authors.forename: Henner
authors.initials: H
authors.lastname: Knust
authors.forename: Parichehr
authors.initials: P
authors.lastname: Malherbe
authors.forename: Matthias
authors.initials: M
authors.lastname: Nettekoven
authors.forename: Angelique
authors.initials: A
authors.lastname: Patiny-Adam
authors.forename: Claus
authors.initials: C
authors.lastname: Riemer
authors.forename: Monique
authors.initials: M
authors.lastname: Schmitt
authors.forename: Will
authors.initials: W
authors.lastname: Spooren
mesh_terms: D000284:Administration, Oral; D015195:Drug Design; D008958:Models, Molecular; D011759:Pyrrolidines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D018042:Receptors, Neurokinin-3 / Q000037:antagonists & inhibitors*
chemical_list: D011759:Pyrrolidines; D018042:Receptors, Neurokinin-3; C032519:pyrrolidine