N-type Calcium Channel Blockers: Novel Therapeutics for the Treatment of Pain

Title: N-type Calcium Channel Blockers: Novel Therapeutics for the Treatment of Pain

Volume: 2 Issue: 5

Author(s): C. I. Schroeder, C. J. Doering, G. W. Zamponi and R. J. Lewis

Affiliation:

Keywords: Voltage-gated calcium channel, ωconotoxin, neuropathic pain, small molecule mimetics

Abstract: Highly selective Cav2.2 voltage-gated calcium channel (VGCC) inhibitors have emerged as a new class of therapeutics for the treatment of chronic and neuropathic pain. Cone snail venoms provided the first drug in class with FDA approval granted in 2005 to Prialt (ω-conotoxin MVIIA, Elan) for the treatment of neuropathic pain. Since this pioneering work, major efforts underway to develop alternative small molecule inhibitors of Cav2.2 calcium channel have met with varied success. This review focuses on the properties of the Cav2.2 calcium channel in different pain states, the action of ω-conotoxins GVIA, MVIIA and CVID, describing their structure-activity relationships and potential as leads for the design of improved Cav2.2 calcium channel therapeutics, and finally the development of small molecules for the treatment of chronic pain.

Cite this article as:

Schroeder I. C., Doering J. C., Zamponi W. G. and Lewis J. R., N-type Calcium Channel Blockers: Novel Therapeutics for the Treatment of Pain, Medicinal Chemistry 2006; 2 (5) . https://dx.doi.org/10.2174/157340606778250216