title: N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.
abstract: A series of N-(1-benzylpyrrolidin-3-yl)arylbenzamides 8 has been prepared, and their structure-activity relationships studied. Potent ligands selective for human D(4) (hD(4)) over hD(2) and alpha(1) have been identified. One example was determined to be an antagonist in a cAMP assay, with an IC(50) of 1500 nM.
authors.affiliation: NPS Pharmaceuticals Inc., 6850 Goreway Dr., Mississauga, Ontario L4V 1V7, Canada. iegle@npsp.com
authors.forename: Ian
authors.initials: I
authors.lastname: Egle
authors.forename: Nancy
authors.initials: N
authors.lastname: Barriault
authors.forename: Michel
authors.initials: M
authors.lastname: Bordeleau
authors.forename: Jillian
authors.initials: J
authors.lastname: Drage
authors.forename: Laurence
authors.initials: L
authors.lastname: Dube
authors.forename: Jack
authors.initials: J
authors.lastname: Peragine
authors.forename: Lucy
authors.initials: L
authors.lastname: Mazzocco
authors.forename: Jalaj
authors.initials: J
authors.lastname: Arora
authors.forename: Keith
authors.initials: K
authors.lastname: Jarvie
authors.forename: Ashok
authors.initials: A
authors.lastname: Tehim
mesh_terms: D001549:Benzamides / Q000138:chemical synthesis* / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D006801:Humans; D050638:Receptors, Dopamine D4; D013329:Structure-Activity Relationship
chemical_list: D001549:Benzamides; C493599:DRD4 protein, human; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D050638:Receptors, Dopamine D4