Introduction of DRD3
DRD3 is a member of the dopamine receptor family, which is classified into two groups: the D1-like receptor class containing DRD1 and DRD5 and the D2-like receptor class containing DRD3, DRD3, and DRD4. DRD3 has the highest affinity for dopamine. DRD3 is a G-protein coupled receptor that inhibits adenylyl cyclase activity. Its signaling pathway is primarily mediated by interaction with and activation of heterotrimeric GTP-binding proteins (G proteins). GPCRs control pro-survival signaling pathways (e.g. ERK and Akt) that are broadly important in human cancer.
|Basic Information of DRD3|
|Protein Name||D(3) dopamine receptor|
|Aliases||D3DR, ETM1, FET1|
|Organism||Homo sapiens (Human)|
Function of DRD3 Membrane Protein
DRD3 is located in the brain areas that control motor function, and DRD3 antagonism has been shown to exacerbate locomotor activity in the brain. In addition, antipsychotics with comparatively low DRD3 affinity, such as clozapine, are reported to cause significantly rarer movement disorders. The DRD3 gene has been suggested as a susceptibility factor for TD, and the Ser9Gly SNP of this gene has been investigated extensively, resulting in many positive findings. Dopamine functions as regulation of movement, cognition, and emotion through activation of dopamine G protein-coupled receptors in the brain. The crystal structure of the human dopamine D3 receptor in complex with the small molecule D2R/D3R-specific antagonist eticlopride reveals important features of the ligand binding pocket and extracellular loops. DRD3 is overexpressed by several types of human cancer and its inhibition is associated with anti-cancer activity.
Fig.1 Structure of DRD3 membrane protein.
Application of DRD3 Membrane Protein in Literature
This article reports that the antagonist-partial agonist properties of cariprazine at D(3) and D(2) receptors, with very high and preferential affinity to D(3) receptors, making it a candidate antipsychotic with a unique pharmacological profile among known antipsychotics.
This article reveals that the difference between the highly homologous D2R and D3R for an extracellular extension of the eticlopride binding site consisting of a second binding pocket for the aryl amide of R-22.
This article underlines the differences in dopamine D(3) properties of new generation antipsychotics which may need to be considered in understanding their diverse therapeutic actions.
This article shows a series of new aporphine analogues (aporlogues) displayed well to high affinity at the D(3) receptor, low or no affinity at the D(1) and D(2) receptors and may be useful in the treatment of several brain disorders.
This article identifies that D(3) receptors are involved in the action of sarizotan, which is in contrast to the more general involvement of 5-HT(1A) receptors in the anti-dyskinetic effects of sarizotan.
DRD3 Preparation Options
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