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Zalicus AŞ Message Board

  • scistats scistats Sep 15, 2013 12:21 AM Flag

    Z160 - Margaret S Lee, Poster

    Z160, a potent, selective, state-dependent,
    small molecule N-type calcium channel blocker. Z160 blocked native and recombinant N-type
    channel currents in an irreversible, dose-dependent manner with sub-micromolar potency and
    25- to 100-fold selectivity over P/Q- and L-type calcium channels. Z160 mediated a
    hyperpolarizing shift in steady-state inactivation, consistent with a mechanism involving
    inactivated state blockade. Z160 also demonstrated use-dependent block of N-type channels,
    with significantly greater potency at stimulation frequencies similar to the action potential
    firing rate typical of neurons processing pain signals. After oral administration in the Chung
    and CCI rodent models of neuropathic pain, Z160 demonstrated dose-dependent reduction of
    thermal hyperalgesia and tactile allodynia at levels comparable to morphine...

    Sentiment: Strong Buy