D1 Human Dopamine GPCR Cell Based Agonist & Antagonist cAMP LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Activation of dopamine D₁ and D₅ receptors leads to stimulation of membrane associated adenylyl cyclase, the enzyme responsible for conversion of ATP to the important intracellular messenger cAMP. In contrast, activation of dopamine D₂ receptors leads to inhibition of adenylyl cyclase.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
D1 Human Dopamine GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
310000-0
Protein
D1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
D1 Human Dopamine GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
310000-1
Protein
D1
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Dopamine
Class:
Class A
Protein Name:
D1
Uniprot Number:
P21728
Protein Aliases:
Dopamine D1 receptor
Gene Name:
DRD1
Gene ID:
1812
Accession Number:
NM_000794
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant dopamine D₁ receptor stably expressed in CHO cells are used. Test compound and/or vehicle is incubated with the cells in incubation buffer at 37°C for 15 minutes. The reaction is evaluated for cAMP levels by TR-FRET. Test compound-induced cAMP increase by 50 percent or more (≥50%) relative to 1 µM dopamine response indicates possible dopamine D1 receptor agonist activity. Test compound inhibition of 0.02 µM dopamine-induced response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
15 min at 37°C
Control Inhibitor:
(+)-Butaclamol
Control Activator:
Dopamine
Criteria For Significance:
≥ 50% Increase in cAMP relative to dopamine response, ≥ 50% Inhibition of dopamine-induced cAMP increase
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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