title: Dopamine D3 receptor agonists as pharmacological tools.
abstract: Dysregulation of the dopaminergic innervation in the central nervous system plays a key role in different neurological disorders like Parkinson´s disease, restless legs syndrome, schizophrenia etc. Although dopamine D3 receptors have been recognized as an important target in these diseases, their full pharmacological properties need further investigations. With focus on dopamine D3 receptor full agonists, this review has divided the ergoline and non-ergoline ligands in dissimilar chemical subclasses describing their pharmacodynamic properties on different related receptors, on species differences and their functional properties on different signaling mechanism. This is combined with a short description of structure-activity relationships for each class. Therefore, this overview should support the rational choice for the optimal compound selection based on affinity, selectivity and efficacy data in biochemical and pharmacological studies.
authors.affiliation: Heinrich-Heine-University, Universitaetsstr. 1, 40225 Duesseldorf, Germany.
authors.forename: S
authors.initials: S
authors.lastname: Kassel
authors.affiliation: Heinrich-Heine-University, Universitaetsstr. 1, 40225 Duesseldorf, Germany.
authors.forename: J S
authors.initials: JS
authors.lastname: Schwed
authors.affiliation: Heinrich-Heine-University, Universitaetsstr. 1, 40225 Duesseldorf, Germany. Electronic address: stark@hhu.de.
authors.forename: H
authors.initials: H
authors.lastname: Stark
mesh_terms: D000818:Animals; D018491:Dopamine Agonists / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D050637:Receptors, Dopamine D3 / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D018491:Dopamine Agonists; D050637:Receptors, Dopamine D3
keywords: Affinity; Dopamine D(3) receptor; Efficacy; GPCR; Pharmacophore; Selectivity