Biological Information
Background Information:
Five subtypes of dopamine receptors, D1, D2, D3, D4 and D5, were identified on the basis of pharmacological or biochemical criteria. The D2-like receptors include the two isoforms of the D2 receptor, differing in the length of their predicted third cytoplasmic loop, dubbed D2 short (D2S) and D2 long (D2L). The dopamine D2S receptor couples to PTX-sensitive G proteins (Gi/o) to initiate multiple signaling pathways. In cells of neuroendocrine origin, the D2S couples to "inhibitory" pathways, including inhibition of adenylyl cyclase, activation of potassium channels to hyperpolarize the cell membrane, and inhibition of L-type calcium channels, which in concert mediate inhibition of hormone secretion and gene transcription, and inhibition of cell proliferation. D2 dopamine receptors have been implicated in the pathophysiology of schizophrenia and Parkinson’s disease.
Family:
GPCR
Sub Family:
Dopamine
Class:
Class A
Protein Name:
D2
Uniprot Number:
P14416
Gene Name:
DRD2
Gene ID:
1813
Accession Number:
NM_000795
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]methyl-spiperone
Ligand Kd (nM):
0.1
Ligand Concentration:
0.3 nM
Non Specific:
10 µM Butaclamol
Incubation:
60 min at RT
Control Inhibitor:
Butaclamol
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Adverse / Beneficial Action:
Dopamine D2L antagonist may be useful in the treatment of psychosis without development of tardive dyskinesia.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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