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+].
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:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[125I](±)DOI
Ligand Kd (nM):
0.3
Ligand Concentration:
0.1 nM
Non Specific:
1 µM (±)DOI
Incubation:
60 min at RT
Control Inhibitor:
DOI
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
10 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:
France - Celle L'Evescault
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