Human Cav2.2/β3/α2δ1 Calcium Channel Membranes

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  • Displacement of [3H]-gabapentin binding by unlabeled gapapentin and by L-leucine. Membranes from cells expressing human Cav2.2 calcium channels were incubated with 5 μM [3H]-gabapentin and the indicated concentration of either unlabeled gabapentin or of L-leucine. After filtration over GF/B filters, the filters were washed and counted. In this assay, gabapentin yielded an IC50 of 94 nM, and L-leucine had an IC50 of 84 nM.

Human Cav2.2/β3/α2δ1 Calcium Channel Membranes

  • Cat.#:
  • CT3159
  • Lot #:
  • 1401

Availability: In stock

Price: $397.00
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Quick Overview

Human Cav2.2/β3/α2δ1 Calcium Channel membrane preparation derived from stable, replicating cell line.

Background

The human CACNA1B gene encodes the pore-forming subunit of voltage-gated N-type Ca2+ channels. Co-expression with the β3 and α2δ1 auxiliary subunits recapitulates function in heterologous expression (CHO cells). Cav2.2 channels, widely distributed in neurons, are therapeutic targets in neuropathic and inflammatory pain. Gabapentin (Neurontin) has been shown to bind to the α2δ subunit of the calcium channel (Gee et al., 1996)
General Info
Synonyms N-type calcium channel
Product Description Human Cav2.2/β3/α2δ1 Calcium Channel membrane preparation derived from stable, replicating cell line.
Target Type Ion Channel
Product Type membrane
Sub-Type Cav2.2/β3/α2δ1
Class Voltage-gated calcium channel
Therapeutic Area pain & inflammation
Related Services Membrane Preparation
Gene Name CACNA1B/CACNB3/CACNA2D1
Validated Assay/Platform binding
References Catterall WA et al. 2005. International Union of Pharmacology. XLVIII. Nomenclature and structure-function relationships of voltage-gated calcium channels. Pharmacol Rev. 57:411-25
Gee, N.S. et al. 1996 The Novel anticonvulsant drug, gabapentin (Ne
Membrane Info
Host cell CHO-K1
Recommended Assay Conditions Refer to product specification sheet for details
Storage and Packaging
Packaging 0.4 mL of membranes at a protein concentration of 2.5 mg/mL
Storage Recommendation -80°C; Avoid repeated freeze-thawing of this product.
Quantity 400 µL/vial
Media
Specification Sheet  Download PDF Document