A1 Human Adenosine GPCR GTPgammaS Agonist & Antagonist LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Adenosine receptors are members of the G-protein coupled receptor (GPCR) superfamily, and are typically thought to mediate stimulation or inhibition of adenylyl cyclase activity. Four subtypes of receptor have been identified, designated A1, A2A, A2B and A3. A1 receptors, distributed widely in CNS and peripheral tissues, inhibit adenylyl cyclase and voltage-dependent calcium channels, and activate potassium channels through a pertussis-toxin-sensitive G-protein, probably of the Gi/Go class.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
A1 Human Adenosine GPCR GTPgammaS Agonist LeadHunter Assay - TW
Item
301400-0
Protein
A1
Organism
Human
Assay Sub Type
GTPgammaS
Family
GPCR
Name
A1 Human Adenosine GPCR GTPgammaS Antagonist LeadHunter Assay - TW
Item
301400-1
Protein
A1
Organism
Human
Assay Sub Type
GTPgammaS
Family:
GPCR
Sub Family:
Adenosine
Class:
Class A
Protein Name:
A1
Uniprot Number:
P30542
Gene Name:
ADORA1
Gene ID:
134
Gene Aliases:
RDC7
Accession Number:
NM_000674
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
GTPgammaS
Functional Mode:
Agonist & Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant adenosine A1 receptors expressed in CHO-K1 cells are used. Test compound and/or vehicle is preincubated with the 36 µg/ml‡ receptors and 10 μM GDP in modified HEPES buffer pH 7.4 for 20 minutes at 25°C, SPA beads are then added for another 60 minutes at 30°C. The reaction is initiated by 0.3 nM [35S]GTPγS for an additional 15 minute incubation period. Test compound-induced increase of [35S]GTPγS binding by 50 percent or more (≥50%) relative to 3 μM CPA response indicates possible adenosine A1 receptor agonist activity. Inhibition of 0.1 μM CPA-induced [35S]GTPγS binding response by 50 percent or more (≥50%) indicates receptor antagonist activity. Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.
Incubation:
15 min at 30°C
Control Inhibitor:
8-Cyclopentyl-1,3-dipropylxanthine
Control Activator:
CPA
Criteria For Significance:
≥ 50% increase in bound [35S]GTPgammaS relative to CPA response, ≥ 50% inhibition of CPA-induced bound [35S]GTPgammaS
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:
Adenosine A1 receptor agonism, through inhibition of adenyl cyclase, may cause bradycardia, analgesia and anxiolytic activity; antagonism may cause hyperalgesia and anxiety.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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A1 Human Adenosine GPCR GTPgammaS Agonist LeadHunter Assay - TW
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