title: Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.
abstract: Hybrid molecules built up by covalent coupling of aminopropanol derivatives (especially pindolol) with antidepressant drugs like fluoxetine, paroxetine or milnacipran were found to be potent and silent 5-HT1A antagonists (KB < 1 nM for 7c and 9a).
authors.affiliation: Medicinal Chemistry, Centre de Recherche Pierre Fabre, Castres, France. michel.perez@pierre-fabre.com
authors.forename: M
authors.initials: M
authors.lastname: Perez
authors.forename: P J
authors.initials: PJ
authors.lastname: Pauwels
authors.forename: I
authors.initials: I
authors.lastname: Pallard-Sigogneau
authors.forename: C
authors.initials: C
authors.lastname: Fourrier
authors.forename: P
authors.initials: P
authors.lastname: Chopin
authors.forename: C
authors.initials: C
authors.lastname: Palmier
authors.forename: V
authors.initials: V
authors.lastname: Colovray
authors.forename: S
authors.initials: S
authors.lastname: Halazy
mesh_terms: D000818:Animals; D015195:Drug Design; D051379:Mice; D010394:Penbutolol / Q000494:pharmacology*; D010869:Pindolol / Q000494:pharmacology*; D011433:Propranolol / Q000494:pharmacology*; D011985:Receptors, Serotonin / Q000187:drug effects*; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D017367:Selective Serotonin Reuptake Inhibitors / Q000494:pharmacology*; D013237:Stereoisomerism
chemical_list: D010394:Penbutolol; D010869:Pindolol; D011433:Propranolol; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists; D017367:Selective Serotonin Reuptake Inhibitors