title: N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: human dopamine D4 ligands with high affinity for the 5-HT2A receptor.
abstract: A series of N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides 8 has been prepared and found to bind with high affinity to the human D(4) (hD(4)) and 5-HT(2A) receptors. Several compounds displayed selectivity for these receptors versus hD(2) and alpha(1) adrenergic receptors of over 500-fold.
authors.affiliation: NPS Pharmaceuticals, 6850 Goreway Dr., Mississauga, Ont., Canada L4V 1V7.
authors.forename: Jalaj
authors.initials: J
authors.lastname: Arora
authors.forename: Michel
authors.initials: M
authors.lastname: Bordeleau
authors.forename: Laurence
authors.initials: L
authors.lastname: Dube
authors.forename: Keith
authors.initials: K
authors.lastname: Jarvie
authors.forename: Lucy
authors.initials: L
authors.lastname: Mazzocco
authors.forename: Jack
authors.initials: J
authors.lastname: Peragine
authors.forename: Ashok
authors.initials: A
authors.lastname: Tehim
authors.forename: Ian
authors.initials: I
authors.lastname: Egle
mesh_terms: D014150:Antipsychotic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004298:Dopamine / Q000737:chemistry; D006801:Humans; D008024:Ligands; D050638:Receptors, Dopamine D4 / Q000037:antagonists & inhibitors*; D058830:Serotonin 5-HT2 Receptor Antagonists
chemical_list: D014150:Antipsychotic Agents; D001549:Benzamides; D008024:Ligands; D058830:Serotonin 5-HT2 Receptor Antagonists; D050638:Receptors, Dopamine D4; D004298:Dopamine