title: R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.
abstract: Several N-substituted-11-hydroxy-10-hydroxymethyl- and 11-hydroxy-10-methylaporphines were synthesized and their binding affinities at dopamine D(1) and D(2) receptors and serotonin 5-HT(1A) and 5-HT(2A) receptors in rat forebrain tissue were evaluated. Tested compounds displayed moderate to high affinity to 5-HT(1A) receptors but low affinity to D(1) and D(2) receptors. The most potent novel 5-HT(1A) agent was R-(-)-N-methyl-10-hydroxymethyl-11-hydroxyaporphine.
authors.affiliation: Alcohol Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
authors.forename: Yu-Gui
authors.initials: YG
authors.lastname: Si
authors.forename: Matthew P
authors.initials: MP
authors.lastname: Gardner
authors.forename: Frank I
authors.initials: FI
authors.lastname: Tarazi
authors.forename: Ross J
authors.initials: RJ
authors.lastname: Baldessarini
authors.forename: John L
authors.initials: JL
authors.lastname: Neumeyer
mesh_terms: D000818:Animals; D001060:Aporphines / Q000737:chemistry / Q000378:metabolism*; D008024:Ligands; D011485:Protein Binding; D051381:Rats; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*
chemical_list: D001060:Aporphines; D008024:Ligands; D044282:Receptor, Serotonin, 5-HT1A; C081279:aporphine