Y1 Human Neuropeptide Y GPCR GTPgammaS Agonist LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Neuropeptide Y 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. Neuropeptide Y Y1 receptors are found in multiple tissues including brain, heart, kidney and gastrointestinal tract. Neuropeptide Y Y1 receptor agonism may be antidepressant and cause vasoconstriction as well as inhibit gut motility, gastric emptying, acid secretion and pancreatic exocrine secretion. Neuropeptide Y Y1 receptor agonism may cause vasoconstriction and anxiolysis. Receptor antagonism has been reported to be anxiogenic as well as inhibit ischemic brain injury.
Family:
GPCR
Sub Family:
Neuropeptide Y
Class:
Class A
Protein Name:
NPY1-R
Uniprot Number:
P25929
Gene Name:
NPY1R
Gene ID:
4886
Gene Aliases:
neuropeptide Y receptor Y1
Accession Number:
NM_000909
Organism:
Human
Construct Details:
Full Length, Recombinant
Assay Information
Assay Type:
Functional
Assay Sub Type:
GTPgammaS
Functional Mode:
Agonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant neuropeptide Y Y1 receptors expressed CHO-K1 Gαqi5 cells are used. Test compound is preincubated with membranes and 1 μM GDP at RT for 20 minutes at RT 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 15 minute incubation period. Test compound-induced increase of [35S]GTPγS binding by 50 percent or more (≥50%) relative to 3 μM neuropeptide Y (human, rat) response indicates possible neuropeptide Y Y1 receptor agonist activity. Test compound-induced inhibition of 0.3 μM neuropeptide Y (human, rat)-induced increase of [35S]GTPγS binding response by 50 percent or more (≥50%) indicates possible receptor antagonist activity.
Incubation:
15 min at 30°C
Control Activator:
Neuropeptide Y (human, rat)
Criteria For Significance:
≥ 50% Increase in bound [35S]GTPgammaS relative to Neuropeptide Y (human, rat) 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
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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