alpha1D Human Adrenoceptor GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Adrenoreceptors 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. Adrenoreceptors are found in most peripheral tissue and within the central nervous system. Phenylephrine induced a significant increase in activated extracellular signal-regulated kinases 1 and 2 (ERK1/2)；this increase in phosphorylated ERK was blocked by a1D inhibitor (BM5-7378). a1D plays a key role in contractile response as well as in ERK activation.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
alpha1D Human Adrenoceptor GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
302080-0
Protein
alpha1D
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
alpha1D Human Adrenoceptor GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
302080-1
Protein
alpha1D
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Adrenoceptor
Class:
Class A
Protein Name:
alpha1D
Uniprot Number:
P25100
Protein Aliases:
Alpha-1D adrenoreceptor|Alpha-1D adrenoceptor|Alpha-adrenergic receptor 1a
Gene Name:
ADRA1D
Gene ID:
146
Gene Aliases:
ADRA1R|ADRA1A|ADRA1
Accession Number:
NM_000678
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
HEK293
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 α1D receptors expressed in HEK-293 cells are used. Test compound and/or vehicle is incubated with the cells (1 x 10^6 /ml) in stimulation buffer of IP1 Tb kit for 60 minutes at 37°C. Test compound-induced increase of fluorescence by 50 percent or more (≥50%) relative to the 30 μM phenylephrine response indicates possible α1D receptor agonist activity. Test compound-induced inhibition of 3 μM phenylephrine-induced increase of fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity. Compounds are screened at 10, 1, 0.1, 0.01 and 0.001 μM.
Incubation:
1 hr at 37°C
Control Inhibitor:
Bmy-7378
Control Activator:
Phenylephrine
Criteria For Significance:
≥ 50% increase in IP-one relative to Phenylephrine response, ≥ 50% Inhibition of Phenylephrine-induced response
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:
Cardiovascular
Adverse / Beneficial Action:
Adrenergic a1D receptor antagonism may be useful in the treatment of hypertension with minimal associated orthostatic hypotension.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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