sigma2 Human Binding Agonist Radioligand LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Sigma receptor-mediated transduction mechanisms have not as yet been fully elucidated, but require neither G-protein activation nor phosphorylation. Sigma receptors, located primarily in the central nervous system but also in endocrine and immune systems, have been implicated in psychosis, depression, cognition, neuroprotection, and locomotion in the central nervous system and regulation of cell proliferation. Sigma 2 receptor agonism may induce cytotoxicty in various cells through increases in intracellular Ca2+ and promote apoptosis in drug-resistant cancer cells. Receptor antagonism may be antipsychotic.
Family:
Transmembrane (Other)
Sub Family:
Sigma
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human Sigma s2 receptors expressed in Jurkat cells are used in modified potassium phosphate buffer pH 7.6. A 188 µg‡ aliquot is incubated 25 nM [³H] DTG for 60 minutes at 25℃. Non-specific binding is estimated in the presence of 10 μM haloperidol. Membranes are filtered and washed, the filters are then counted to determine [³H] DTG specifically bound. Compounds are screened at 10 µM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.
Ligand:
[³H] DTG
Ligand Kd (nM):
80
Ligand Concentration:
0.025 µM
Non Specific:
10 µM Haloperidol
Incubation:
60 min at 25°C
Control Inhibitor:
Haloperidol
Criteria For Significance:
≥ 50 of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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