Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1921719 | Parkinsonism & Related Disorders | 2008 | 6 Pages |
Abstract
The effects of aripiprazole, S33592, bifeprunox, N-desmethylclozapine and preclamol acting as partial agonists on recombinant D2L and D3 receptors expressed both separately and concomitantly in COS-7 cells are evaluated here. Aripiprazole, S33592, bifeprunox, N-desmethylclozapine and preclamol behave as partial agonists on D2L receptors coupled with adenylyl cyclase, but they behave as antagonists on co-expression of D3 with D2L receptors. These data raise the intriguing hypothesis that antipsychotic actions of “partial agonists” such as aripiprazole may not reflect inefficient stimulation of D2 and/or D3 receptors but, by analogy with other antipsychotics, may instead represent a blockade of D2/D3 heterodimers (and/or D3 receptors) that are “weakly” coupled to transduction mechanisms postsynaptically of the dopaminergic pathway.
Related Topics
Life Sciences
Biochemistry, Genetics and Molecular Biology
Ageing
Authors
Roberto Maggio, Francesca Novi, Mario Rossi, Giovanni U. Corsini, Mark J. Millan,