Cav2.2 (N-type) Human Calcium Ion Channel [3H] Gabapentin Binding Antagonist Radioligand LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Voltage-gated calcium channels mediate calcium influx in response to membrane depolarization and regulate intracellular processes such as contraction, secretion, neurotransmission, and gene expression. They are members of a gene superfamily of transmembrane ion channel proteins that includes voltage-gated potassium and sodium channels. The pharmacology of the different families of calcium channels is quite distinct. L-Type calcium channel blockers are used in the therapy of cardiovascular disease. N-type (Cav2.2) calcium channels are targets for drugs to relieve chronic and neuropathic pain and for nervous system disorders.
Family:
Ion Channel
Class:
Class C
Protein Name:
Cav2.2 (N-type)
Uniprot Number:
Q00975
Gene Name:
CACNA1B
Gene ID:
774
Gene Aliases:
Cav2.2|CACNN
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant calcium channel Cav2.2/β3/α2δ-1 receptors expressed in CHO cells are used in modified HEPES/KOH buffer pH 7.4. A 3 mgõ aliquot of membrane is incubated with 5 nM [³H]Gabapentin for 120 minutes at 25°C. Non-specific binding is estimated in the presence of 10 μM Gabapentin. Membranes are filtered and washed, the filters are then counted to determine [³H]Gabapentin specifically bound. Compounds are screened at 10 μM.
Ligand:
[³H] Gabapentin
Ligand Kd (nM):
20
Ligand Concentration:
5 nM
Non Specific:
10 µM Gabapentin
Incubation:
120 min at 25°C
Control Inhibitor:
Gabapentin
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:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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