A1 Human Adenosine GPCR GTPgammaS Antagonist LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Adenosine receptors 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. Adenosine receptors may also be called P1 receptors, which are distinguished from transmitter-gated ion channels (P2X receptors) and G protein-coupled receptors (P2Y).
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:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Incubation:
15 min at 30°C
Control Inhibitor:
8-Cyclopentyl-1,3-dipropylxanthine
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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