• Bioorg. Med. Chem. Lett. · Jun 2012

    A novel series of pyrazolylpiperidine N-type calcium channel blockers.

    • Nalin L Subasinghe, Mark J Wall, Michael P Winters, Ning Qin, Mary Lou Lubin, Michael F A Finley, Michael R Brandt, Michael P Neeper, Craig R Schneider, Raymond W Colburn, Christopher M Flores, and Zhihua Sui.
    • Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA. NSUBASIN@its.jnj.com
    • Bioorg. Med. Chem. Lett. 2012 Jun 15; 22 (12): 4080-3.

    AbstractSelective blockers of the N-type calcium channel have proven to be effective in animal models of chronic pain. However, even though intrathecally delivered synthetic ω-conotoxin MVIIA from Conus magnus (ziconotide [Prialt®]) has been approved for the treatment of chronic pain in humans, its mode of delivery and narrow therapeutic window have limited its usefulness. Therefore, the identification of orally active, small-molecule N-type calcium channel blockers would represent a significant advancement in the treatment of chronic pain. A novel series of pyrazole-based N-type calcium channel blockers was identified by structural modification of a high-throughput screening hit and further optimized to improve potency and metabolic stability. In vivo efficacy in rat models of inflammatory and neuropathic pain was demonstrated by a representative compound from this series.Copyright © 2012 Elsevier Ltd. All rights reserved.

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