| Tclin | D(3) dopamine receptor |
This gene encodes the D3 subtype of the five (D1-D5) dopamine receptors. The activity of the D3 subtype receptor is mediated by G proteins which inhibit adenylyl cyclase. This receptor is localized to the limbic areas of the brain, which are associated with cognitive, emotional, and endocrine functions. Genetic variation in this gene may be associated with susceptibility to hereditary essential tremor 1. Alternative splicing of this gene results in transcript variants encoding different isoforms, although some variants may be subject to nonsense-mediated decay (NMD). [provided by RefSeq, Jul 2008]
Comments
Property Summary
| NCBI Gene PubMed Count | 335 |
| Grant Count | 128 |
| R01 Count | 55 |
| Funding | $21,673,035.94 |
| PubMed Score | 303.42 |
| PubTator Score | 382.09 |
ropinirole
pKi 7.43
prochlorperazine
pKi 8.61
amisulpride
pKi 8.49
risperidone
pKi 7.00
clozapine
pKi 7.00
olanzapine
pKi 7.00
spiperone
pIC50 7.01
flunarizine
pIC50 7.01
bromocriptine
pKi 7.06
dopamine
pKi 7.14
promazine
pKi 7.16
metoclopramide
pKi 7.17
verapamil
pKi 7.20
oxatomide
pKi 7.20
amitriptyline
pKi 7.21
nortriptyline
pKi 7.22
methysergide
pKi 7.23
sulpiride
pKi 7.24
methylergometrine
pKi 7.24
cisapride
pKi 7.31
CHEMBL418321
pKi 7.00
CHEMBL2037521
pKi 7.00
CHEMBL3780140
pKi 7.00
CHEMBL1774544
pKi 7.00
CHEMBL3799157
pKi 7.00
CHEMBL240773
pKi 7.00
CHEMBL2367896
pKi 7.00
CHEMBL325060
pKi 7.00
CHEMBL231070
pKi 7.00
CHEMBL326454
pKi 7.00
CHEMBL1631532
pKi 7.00
CHEMBL168908
pKi 7.00
CHEMBL1803055
pKi 7.00
CHEMBL595489
pKi 7.00
CHEMBL1173288
pKi 7.00
CHEMBL113238
pKi 7.00
CHEMBL1928127
pKi 7.00
CHEMBL127807
pKi 7.00
CHEMBL1632210
pKi 7.00
CHEMBL557110
pKi 7.00
| AID | Type | Active / Inconclusive / Inactive | Description |
|---|---|---|---|
| 1788 | other |
0 / 0 / 0 | Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity |
| 1921 | other |
2 / 0 / 0 | Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: Ancillary Activity |
| 434953 | screening |
0 / 0 / 0 | Late-stage radioligand binding dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Ki |
| 434974 | screening |
0 / 0 / 0 | Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen |
| 504381 | other |
0 / 0 / 0 | Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Set 2 |
| 504410 | confirmatory |
0 / 0 / 0 | Late-stage radioligand binding dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Ki Set 2 |
| 624355 | other |
0 / 0 / 0 | Late stage results from the probe development efforts to identify dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and nuclear factor NF-kappa-B (NF-kB): Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs |
| 624406 | other |
0 / 0 / 0 | Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs |
| 652048 | screening |
2394 / 0 / 409679 | qHTS of D3 Dopamine Receptor Agonist: qHTS |
| 652049 | summary |
0 / 0 / 0 | qHTS of D3 Dopamine Receptor Potentiators: Summary |
| More... |
| PMID | Text |
|---|---|
| 27077655 | Ammonia induced autophagy by MTOR is mediated by DRD3. |
| 26857559 | The combination of MTHFR, DRD3 and MDR1 polymorphisms associated with a slow ATV metabolizer phenotype |
| 26787837 | Drd3 palmitoylation acts as a molecular switch for Drd3-biased signaling via a GIPC1-dependent route, which is likely to affect the mode of action of antipsychotic drugs. |
| 26627941 | The DRD3 (rs6280) polymorphism influences younger Parkinson disease age of onset in the US Caucasian population. |
| 26561806 | A significant positive correlation was found between the DRD3 mRNA level and the score of the excited factor in patients with schizophrenia/schizophreniform disorder. |
| 26376054 | Combined genetic polymorphisms related to dopamine neurotransmission, COMT Val158Met and DRD3 Ser9Gly, might influence executive function in schizophrenia. |
| 26164205 | data utilizing a dopamine agonist tracer demonstrate, for the first time, an inverse association between social status and D2/3R availability. |
| 26116441 | used site-directed mutagenesis to identify key residues involved in D3 receptor signaling function |
| 25931118 | results provide insights into the potential contribution of molecules of cholesterol to the overall organization and potential stability of the D3 receptor and possibly other GPCR quaternary structures |
| 25927430 | We did not find evidence of association between the other four SNPs (rs167771 and rs324029 in DRD3, rs8076005 and rs2066713 in SCL6A4) and Type 2 Diabetes Mellitus. |
| More... |
MASLSQLSSHLNYTCGAENSTGASQARPHAYYALSYCALILAIVFGNGLVCMAVLKERALQTTTNYLVVS 1 - 70 LAVADLLVATLVMPWVVYLEVTGGVWNFSRICCDVFVTLDVMMCTASILNLCAISIDRYTAVVMPVHYQH 71 - 140 GTGQSSCRRVALMITAVWVLAFAVSCPLLFGFNTTGDPTVCSISNPDFVIYSSVVSFYLPFGVTVLVYAR 141 - 210 IYVVLKQRRRKRILTRQNSQCNSVRPGFPQQTLSPDPAHLELKRYYSICQDTALGGPGFQERGGELKREE 211 - 280 KTRNSLSPTIAPKLSLEVRKLSNGRLSTSLKLGPLQPRGVPLREKKATQMVAIVLGAFIVCWLPFFLTHV 281 - 350 LNTHCQTCHVSPELYSATTWLGYVNSALNPVIYTTFNIEFRKAFLKILSC 351 - 400 //
| PMID | Year | Title |
|---|---|---|
| 27077655 | 2016 | Ammonia Induces Autophagy through Dopamine Receptor D3 and MTOR. |
| 26857559 | 2016 | A pharmacogenetic pilot study reveals MTHFR, DRD3, and MDR1 polymorphisms as biomarker candidates for slow atorvastatin metabolizers. |
| 26787837 | 2016 | A GIPC1-Palmitate Switch Modulates Dopamine Drd3 Receptor Trafficking and Signaling. |
| 26627941 | 2016 | Association of Parkinson disease age of onset with DRD2, DRD3 and GRIN2B polymorphisms. |
| 26561806 | 2015 | The mRNA Expression Status of Dopamine Receptor D2, Dopamine Receptor D3 and DARPP-32 in T Lymphocytes of Patients with Early Psychosis. |
| 26460884 | 2015 | G protein-coupled receptors directly bind filamin A with high affinity and promote filamin phosphorylation. |
| 26376054 | Epistasis between COMT Val158Met and DRD3 Ser9Gly polymorphisms and cognitive function in schizophrenia: genetic influence on dopamine transmission. | |
| 26164205 | 2015 | A preliminary study of dopamine D2/3 receptor availability and social status in healthy and cocaine dependent humans imaged with [(11)C](+)PHNO. |
| 26116441 | 2015 | Identification of key residues involved in the activation and signaling properties of dopamine D3 receptor. |
| 25931118 | 2015 | Analysis of Human Dopamine D3 Receptor Quaternary Structure. |
| More... |
