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

PubChem ID

4636

Name

Oxymetazoline

Measurement

5.8nM - IC50

PubChem ID

4893

Name

Prazosin

Measurement

4300nM - IC50

PubChem ID

8969

Name

Yohimbine

Measurement

5.5nM - IC50

PubChem ID

108094

Name

2-Methoxyidazoxan

Measurement

1.2nM - IC50

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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