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. .
Family:
GPCR
Sub Family:
Adrenoceptor
Class:
Class A
Protein Name:
alpha2A
Uniprot Number:
P08913
Protein Aliases:
alpha-2AAR subtype C10| alpha-2A-adrenergic receptor
Gene Name:
ADRA2A
Gene ID:
150
Gene Aliases:
ADRA2R|ADRAR
Accession Number:
NM_000681
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]RX 821002
Ligand Kd (nM):
0.8
Ligand Concentration:
1 nM
Non Specific:
100 µM (-)epinephrine
Incubation:
60 min at RT
Control Inhibitor:
yohimbine
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:
Cardiovascular
Adverse / Beneficial Action:
Adrenergic a2A receptor agonist may cause bradycardia and hypotension, inhibit insulin secretion resulting in hyperglycemia; antagonist may cause hypertension and exacerbate heart failure
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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