Biological Information

Background Information:

There are three known subtypes of b-adrenergic receptors, b1, b2, and b3, all of which are thought to couple primarily via Gsa to adenylyl cylase, leading to an increase in cAMP. The receptor subtypes differ primarily in their location: b1-adrenoceptors predominate in the heart, cerebral cortex, and the kidney. The major subtype in the lungs, cerebellum, uterus, skeletal muscle, and blood vessels is the b2-adrenoceptor. The b3-adrenoceptor has been detected in brain, stomach, and gall bladder but are expressed predominantly in white and brown adipose tissue (WAT and BAT, respectively). b2 adrenoceptors are mainly associated with causing relaxation of smooth muscle in a variety of tissues. Adrenergic b2 receptor agonism have been found useful in the treatment of bronchospasm but may facilitate cardiac arrest. Adrenergic b2 receptor antagonism may facilitate bronchospasm and impair exercise stress cardiovascular performance.

Family:

GPCR

Sub Family:

Adrenoceptor

Class:

Class A

Protein Name:

beta2

Uniprot Number:

P07550

Protein Aliases:

Beta-2 adrenoceptor

Gene Name:

ADRB2

Gene ID:

154

Gene Aliases:

ADRBR|BAR|B2AR

Accession Number:

NM_000024

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):

0.15

Ligand Concentration:

0.3 nM

Non Specific:

50 µM Alprenolol

Incubation:

120 min at RT

Control Inhibitor:

ICI 118551

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

2083

Name

Salbutamol

Measurement

3100nM - IC50

PubChem ID

4946

Name

Propranolol

Measurement

1.6nM - IC50

PubChem ID

9888075

Name

SR 59230A

Measurement

30nM - IC50

PubChem ID

Name

ICI 118551

Measurement

0.8nM - IC50

Clinical Relevance

Therapeutic Area:

Pulmonology

Adverse / Beneficial Action:

Adrenergic b2 receptor agonism have been found useful in the treatment of bronchospasm but may facilitate cardiac arrest. Adrenergic b2 receptor antagonism may facilitate bronchospasm and impair exercise stress cardiovascular performance.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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