5-HT2A Human Serotonin GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Serotonin 5-HT receptors belong to the superfamily of G protein-coupled seven transmembrane proteins with the exception of the 5-HT3 subtype, which belongs to the ligand gated cation superfamily of receptors. 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. Serotonin 5-HT2 receptors are widely distributed in the central nervous system and peripheral tissues. The 5-HT2 receptor class couples preferentially to Gq/G11 to increase hydrolysis of inositol phosphates and elevate cytosolic [Ca2+].
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
5-HT2A Human Serotonin GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
355250-0
Protein
5-HT2A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT2A Human Serotonin GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
355250-1
Protein
5-HT2A
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Serotonin
Class:
Class A
Protein Name:
5-HT2A
Uniprot Number:
P28223
Protein Aliases:
5-HT-2A|Serotonin receptor 2A
Gene Name:
HTR2A
Gene ID:
3356
Gene Aliases:
HTR2
Accession Number:
NM_000621
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 recombinant serotonin 5-HT2A receptor stably expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (5 x 10^5 /ml) in stimulation buffer of IP1 Tb kit for 30 minutes at 37°C. Test compound-induced increase of fluorescence by 50 percent or more (≥50%) relative to the 10 μM serotonin response indicates possible serotonin 5-HT2A receptor agonist activity. Test compound-induced inhibition of 0.3 μM serotonin-induced fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
30 min at 37°C
Control Inhibitor:
Ketanserin
Control Activator:
Serotonin (5-HT)
Criteria For Significance:
≥ 50% increase in IP-one relative to Serotonin response, ≥ 50% Inhibition of Serotonin-induced 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
Adverse / Beneficial Action:
Serotonin 5-HT2A receptor agonism may be hallucinogenic, facilitate vasoconstriction and gastrointestinal transit. Receptor antagonism may prevent peripheral vascular thrombosis, reduce psychosis and extrapyramidal side effects of antipsychotic agents.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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5-HT2A Human Serotonin GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
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