Tetrahydroisoquinololine derivatives as modulators of dopamine D₃ receptors

Abstract

This patent describes the discovery of a novel series of tetrahydroisoquinolines as ligands for the dopamine D₃ receptor. These compounds have been identified as agonists or partial agonists in functional assays. The greater affinity for dopamine D₃ than for dopamine D₂ receptors can be of benefit in reducing the undesirable extrapyramidal side effects associated with classical neuroleptic agents. The therapeutic applications of dopamine D₃ agonists or partial agonists have great potentialities, the possible indications are: anxiety, depression, memory disorders, sexual dysfunction and drug dependency (addiction).

• agonist
• CNS disorders
• dopamine D3 receptor
• partial agonist
• tetrahydroisoquinoline