R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.
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.
Si
Yu-Gui
YG
Alcohol Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
Gardner
Matthew P
MP
Tarazi
Frank I
FI
Baldessarini
Ross J
RJ
Neumeyer
John L
JL
D000818:Animals; D001060:Aporphines / Q000737:chemistry / Q000378:metabolism*; D008024:Ligands; D011485:Protein Binding; D051381:Rats; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*
D001060:Aporphines; D008024:Ligands; D044282:Receptor, Serotonin, 5-HT1A; C081279:aporphine