D5 Human Dopamine GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Dopamine receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Various members of the dopamine receptor family are generally classified as either ‘D1-like’ or ‘D2-like’. D1-like receptors comprise the D1 and D5 receptors, which activate adenylate cyclases via coupling to GS protein.
Family:
GPCR
Sub Family:
Dopamine
Class:
Class A
Protein Name:
D5
Uniprot Number:
P21918
Gene Name:
DRD5
Gene ID:
1816
Gene Aliases:
DRD1B
Accession Number:
NM_000798
Organism:
Human
Construct Details:
Full Length, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
This assay measures binding of [³H]SCH-23390 to human dopamine D5 receptors. CHO cells stably transfected with a plasmid encoding the human dopamine D5 receptor are used to prepare membranes in modified Tris-HCl pH 7.4 buffer using standard techniques. A 40 μg‡ aliquot of membrane is incubated with 2.0 nM [³H]SCH-23390 for 120 minutes at 37℃. Non-specific binding is estimated in the presence of 10 µM cis-flupentixol. Membranes are filtered and washed 3 times and the filters are counted to determine [³H]SCH-23390 specifically bound. Compounds are screened at 10 µM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.
Ligand:
[³H] SCH-23390
Ligand Kd (nM):
0.73
Ligand Concentration:
2 nM
Non Specific:
10 µM Flupentixol
Incubation:
120 min at 37°C
Control Inhibitor:
R(+)-SCH-23390
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Adverse / Beneficial Action:
D5 receptor agonism may be of therapeutic benefit in the treatment of Parkinsons disease as well as induce dyskinesia, extreme arousal, locomotor activation, vasodilatation and hypotension.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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