Substituted phenoxyalkylpiperazines as dopamine D3 receptor ligands.
A novel series of potential antipsychotic agents were prepared by combination of condensed heterocycles containing bridgehead nitrogen with (2-methoxyphenyl)piperazine using phenoxyalkyl spacer of variable length. The affinity of the compounds was determined at rat cloned D3 and rat D2, 5-HT1A receptors by an vitro receptor binding assay. The D3 selectivity of the compounds was calculated from the Ki values.
Laszlovszky
I
I
Laboratory of Molecular Pharmacology, Gedeon Richter Ltd., Budapest, Hungary. i.laszlovszky@richter.hu
Acs
T
T
Kiss
B
B
Domány
G
G
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D015259:Dopamine Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism; D007700:Kinetics; D008024:Ligands; D017072:Neostriatum / Q000187:drug effects / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000187:drug effects*; D050637:Receptors, Dopamine D3; D011985:Receptors, Serotonin / Q000187:drug effects; D044263:Receptors, Serotonin, 5-HT1; D018490:Serotonin Agents / Q000138:chemical synthesis / Q000494:pharmacology
D015259:Dopamine Agents; C493595:Drd3 protein, rat; D008024:Ligands; D010879:Piperazines; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D018490:Serotonin Agents