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ω-Conotoxin GVIA Mimetics That Bind and Inhibit Neuronal Ca(v)2.2 Ion Channels

ω-Conotoxin GVIA Mimetics That Bind and Inhibit Neuronal Ca(v)2.2 Ion Channels

Charlotte Elisabet Tranberg, Aijun Yang, Irina Vetter, Jeffrey R McArthur, Jonathan B Baell, Richard J Lewis, Kellie L Tuck, Peter J Duggan

Mar Drugs. 2012 Oct;10(10):2349-68.

PMID: 23170089

Abstract:

The neuronal voltage-gated N-type calcium channel (Ca(v)2.2) is a validated target for the treatment of neuropathic pain. A small library of anthranilamide-derived ω-Conotoxin GVIA mimetics bearing the diphenylmethylpiperazine moiety were prepared and tested using three experimental measures of calcium channel blockade. These consisted of a ¹²⁵I-ω-conotoxin GVIA displacement assay, a fluorescence-based calcium response assay with SH-SY5Y neuroblastoma cells, and a whole-cell patch clamp electrophysiology assay with HEK293 cells stably expressing human Ca(v)2.2 channels. A subset of compounds were active in all three assays. This is the first time that compounds designed to be mimics of ω-conotoxin GVIA and found to be active in the ¹²⁵I-ω-conotoxin GVIA displacement assay have also been shown to block functional ion channels in a dose-dependent manner.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP106375284-A	ω-Conotoxin GVIA		106375-28-4	Price

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