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.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
beta2 Human Adrenoceptor GPCR Cell Based Agonist cAMP LeadHunter Assay - FR
Item
1976
Protein
beta2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
beta2 Human Adrenoceptor GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
Item
1977
Protein
beta2
Organism
Human
Assay Sub Type
Cell Based
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
Organism:
Human
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist & Antagonist
Detection Method:
HTRF
Testing Information
Incubation:
30 min at RT
Control Activator:
isoproterenol (10 nM)
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
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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