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

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at RT

Control Activator:

isoproterenol

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 finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

2083

Name

Salbutamol

Measurement

54.8nM - EC50

PubChem ID

3779

Name

Isoproterenol

Measurement

1nM - EC50

PubChem ID

5152

Name

salmeterol

Measurement

1.78nM - EC50

PubChem ID

5311064

Name

denopamine

Measurement

- EC50

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

RELATED SOLUTIONS

Item: 20
Item: 1977
Item: G008
Item: P347
Item: P426
Item: P427
Item: P460-EU
Item: P452-EU