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:

beta1

Uniprot Number:

P08588

Protein Aliases:

Beta-1 adrenoceptor

Gene Name:

ADRB1

Gene ID:

153

Accession Number:

NM_000684

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H](-)CGP 12177

Ligand Kd (nM):

0.39

Ligand Concentration:

0.3 nM

Non Specific:

50 µM Alprenolol

Incubation:

60 min at RT

Control Inhibitor:

Atenolol

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

2249

Name

Atenolol

Measurement

278nM - IC50

PubChem ID

2685

Name

CGP-20712A

Measurement

6.8nM - IC50

PubChem ID

4946

Name

Propranolol

Measurement

9.9nM - IC50

PubChem ID

Name

ICI 118551

Measurement

300nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

Selective 1-adrenoceptor antagonism may be useful in the treatment of hypertension and stable angina; may also cause bradycardia.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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