5-HT2A Human Serotonin GPCR GTPgammaS Agonist & Antagonist 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+]. 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.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
5-HT2A Human Serotonin GPCR GTPgammaS Agonist LeadHunter Assay - TW
Item
355180-0
Protein
5-HT2A
Organism
Human
Assay Sub Type
GTPgammaS
Family
GPCR
Name
5-HT2A Human Serotonin GPCR GTPgammaS Antagonist LeadHunter Assay - TW
Item
355180-1
Protein
5-HT2A
Organism
Human
Assay Sub Type
GTPgammaS
Family:
GPCR
Sub Family:
Serotonin
Class:
Class A
Protein Name:
5-HT2A
Gene Aliases:
5-HT2A
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 serotonin 5-HT2A receptor stably expressed in CHO-K1 cells is used. Test compound and/or vehicle is preincubated with the membranes and GDP in modified HEPES pH 7.4 buffer for 20 minutes and SPA beads are then added for another 60 minutes at 30°C. The reaction is initiated by [³⁵S]GTPγS for an additional 15 minutes incubation period. Test compound-induced increase of [³⁵S]GTPγS binding 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 1 µM serotonin-induced increase of [³⁵S]GTPγS binding response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
15 min at 30°C
Control Activator:
Serotonin (5-HT)
Criteria For Significance:
≥ 50% Increase in bound [35S]GTPgammaS relative to serotonin response, ≥ 50% Inhibition of serotonin-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
Adverse / Beneficial Action:
Serotonin 5-HT1A receptor agonists may be useful for the treatment of anxiety and depression.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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