Dopamine D3 and D4 receptor antagonists in the treatment of schizophrenia.
The findings that dopamine D3 and D4 receptors are highly expressed in limbic and cortical areas (D4 more than D3), and the fact that the atypical drug clozapine has preferential affinity for the D4 receptors have suggested an involvement of these receptors in schizophrenia. Subsequently, many pharmaceutical companies have pursued the approach of developing selective dopamine D3 or D4 antagonists as potential antipsychotics. This review will discuss the current status of selective dopamine D3 and D4 receptor antagonists for the treatment of schizophrenia.
Jardemark
Kent
K
Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden. kent.jardemark@fyfa.ki.se
Wadenberg
Marie-Louise
ML
Grillner
Pernilla
P
Svensson
Torgny H
TH
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D018492:Dopamine Antagonists / Q000737:chemistry / Q000627:therapeutic use*; D065127:Dopamine D2 Receptor Antagonists; D006801:Humans; D017448:Receptors, Dopamine D2 / Q000096:biosynthesis; D050637:Receptors, Dopamine D3; D050638:Receptors, Dopamine D4; D012559:Schizophrenia / Q000188:drug therapy* / Q000378:metabolism
C493593:DRD3 protein, human; C493599:DRD4 protein, human; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D050638:Receptors, Dopamine D4