beta1 Human Adrenoceptor GPCR Cell Based Agonist & Antagonist cAMP LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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 tissues and within the central nervous system.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
beta1 Human Adrenoceptor GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
302230-0
Protein
beta1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
beta1 Human Adrenoceptor GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
302230-1
Protein
beta1
Organism
Human
Assay Sub Type
Cell Based
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:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human adrenergic β1 receptors expressed in CHO-K1(Rex16) cells are used. Test compound and/or vehicle is incubated with the cells (5 x 10⁵ cell/ml) in modified HBSS pH 7.4 buffer at 37°C for 15 minutes. The reaction is evaluated for cAMP levels by TR-FRET. Test compound-induced cAMP increase by 50 percent or more (≥50%) relative to the 10 μM Isoproterenol control response indicates possible adrenergic β1 receptor agonist activity. Test compound-induced inhibition of the 0.03 μM Isoproterenol-induced cAMP response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
15 min at 37°C
Control Inhibitor:
Atenolol
Control Activator:
Isoproterenol
Criteria For Significance:
≥50% Increase in cAMP relative to Isoproterenol response, ≥50% Inhibition of Isoproterenol-induced cAMP increase
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cardiovascular
Adverse / Beneficial Action:
Adrenergic b1 receptor agonism may increase heart rate and force of contraction. Adrenergic b1 receptor antagonism may facilitate bronchospasm and impair exercise stress cardiovascular performance.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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