5-HT6 Human Serotonin GPCR Cell Based Agonist & Antagonist cAMP LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Serotonin (5-hydroxytryptamine, 5-HT) is one of the well-known examples of a neurotransmitter that mediates a wide variety of physiological effects, including peripheral and central actions. At least four classes of 5-HT receptors have been distinguished pharmacologically, reflecting the second messenger system to which the receptor is coupled. The subfamily of 5-HT₁ and 5-HT₅ interacts negatively with adenylyl cyclase. The second subfamily of 5-HT₂ is coupled to the activation of the phospholipase C. The third, 5-HT₃, is a ligand-gated ion channel and the last subfamily, including 5-HT₄, 5-HT₆, and 5-HT₇ activates adenylyl cyclase to increase intracellular cAMP.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
5-HT6 Human Serotonin GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
318000-0
Protein
5-HT6
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
5-HT6 Human Serotonin GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
318000-1
Protein
5-HT6
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Serotonin
Class:
Class A
Protein Name:
5-HT6
Uniprot Number:
P50406
Protein Aliases:
5-HT6|Serotonin receptor 6
Gene Name:
HTR6
Gene ID:
3362
Gene Aliases:
5-HT6|5-HT6R
Accession Number:
NM_000871
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
HeLa
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-HT₆ receptor stably expressed in HeLa cells are used. Test compound and/or vehicle is incubated with the cells (1 × 10⁴ cells/well) in HBSS buffer pH 7.4 at 37°C for 20 minutes. The reaction is evaluated for cAMP levels by TR-FRET. Test compound-induced cAMP increase by 50 percent or more (≥50%) relative to 10 µM serotonin response indicates possible serotonin 5-HT₆ receptor agonist activity. Test compound inhibition of 0.3 µM serotonin-induced response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
20 min at 37°C
Control Inhibitor:
Methiothepin
Control Activator:
Serotonin (5-HT)
Criteria For Significance:
≥ 50% Inhibition of serotonin-induced cAMP increase, ≥50% Increase in cAMP relative to serotonin 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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5-HT6 Human Serotonin GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
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