alpha2C Human Adrenoceptor GPCR GTPgammaS Agonist & Antagonist 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 tissue and within the central nervous system. Adrenergic a2C receptor may cause peripheral vasoconstriction; antagonism may act peripherally to increase the skeletal muscle blood flow.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
alpha2C Human Adrenoceptor GPCR GTPgammaS Agonist LeadHunter Assay - TW
Item
302190-0
Protein
alpha2C
Organism
Human
Assay Sub Type
GTPgammaS
Family
GPCR
Name
alpha2C Human Adrenoceptor GPCR GTPgammaS Antagonist LeadHunter Assay - TW
Item
302190-1
Protein
alpha2C
Organism
Human
Assay Sub Type
GTPgammaS
Family:
GPCR
Sub Family:
Adrenoceptor
Class:
Class A
Protein Name:
alpha2C
Uniprot Number:
P18825
Protein Aliases:
Alpha-2C adrenoreceptor|Alpha-2C adrenoceptor|Alpha-2CAR
Gene Name:
ADRA2C
Gene ID:
152
Gene Aliases:
ADRA2L2|ADRA2RL2
Accession Number:
NM_000683
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 adrenergic α2C receptors expressed in CHO-K1 cells are used. Test compound is preincubated with 0.023 mg/ml‡ membranes and 1 µM GDP for 20 minutes at 25°C in modified HEPES buffer pH 7.4, then SPA beads are added for another 60 minutes at 30°C. The reaction is initiated by 0.3 nM [35S]GTPγS for an additional 30 minute incubation period. Test compound-induced increase of [35S]GTPγS binding by 50 percent or more (≥50%) relative to 100 µM UK 14,304 response indicates possible adrenergic α2C receptor agonist activity. Test compound-induced inhibition of 1 µM UK 14,304-induced increase of [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:
30 min at 30°C
Control Inhibitor:
Yohimbine
Control Activator:
Brimonidine
Criteria For Significance:
≥ 50% Inhibition of UK-14304-induced bound [35S]GTPgammaS, ≥50% Increase in bound [35S]GTPgammaS relative to UK-14304 response
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:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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alpha2C Human Adrenoceptor GPCR GTPgammaS Agonist LeadHunter Assay - TW
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