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+].
PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.
Family:
GPCR
Sub Family:
Serotonin
Class:
Class A
Protein Name:
5-HT2A
Uniprot Number:
P35363
Protein Aliases:
5-HT-2A|Serotonin receptor 2A
Gene Name:
HTR2A
Gene ID:
15558
Gene Aliases:
HTR2
Accession Number:
NM_172812
Organism:
Mouse
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
PAM
Testing Information
Control Activator:
serotonin
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 10 concentrations are selected
Test Sample Requirements:
40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)
Minimum Order Quantity:
20
Turnaround Time
Standard:
15 Business Days
Clinical Relevance
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:
USA - Fremont, CA