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-HT5A receptors are widely present in the central nervous system but not or minimally in peripheral tissues. The 5-HT5A receptor class couples preferentially to GS to promote cAMP formation. Serotonin 5-HT5A receptor agonism may be hallucinatory and alter circadian rhythms.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
5-HT5A Human Serotonin GPCR Cell Based Agonist Calcium Flux LeadHunter Assay - TW
Item
355400-0
Protein
5-HT5A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT5A Human Serotonin GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - TW
Item
355400-1
Protein
5-HT5A
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Serotonin
Class:
Class A
Protein Name:
5-HT5A
Uniprot Number:
P47898
Protein Aliases:
5-HT-5A|5-HT5A|Serotonin receptor 5A
Gene Name:
HTR5A
Gene ID:
3361
Gene Aliases:
5-HT5A
Accession Number:
NM_024012
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:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant serotonin 5-HT5A 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 incubation buffer of fluo-4 direct calcium kit for 20 minutes at RT. Test compound-induced increase of fluorescence by 50 percent or more (≥50%) relative to the 10 μM 5-CT response indicates possible serotonin 5-HT5A receptor agonist activity. Test compound-induced inhibition of 0.03 μM 5-CT-induced fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
20 min at RT
Control Inhibitor:
Methiothepin
Control Activator:
5-Carboxamidotryptamine
Criteria For Significance:
≥ 50% increase in fluorescence relative to 5-CT response, ≥ 50% inhibition in fluorescence relative to 5-CT-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
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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