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A novel, orally active N-type calcium channel blocker inhibitory actions in vitro



A novel, orally active N-type calcium channel blocker inhibitory actions in vitro



Society for Neuroscience Abstracts 26(1-2): Abstract No -351 4



Voltage gated N-type calcium channel is composed from several subunit, and alpha1B subunit is an ion-permeable domain in the channel. Immunostaining with polyclonal antibody for alpha1B subunit showed an evenly distributed staining pattern throughout all laminae of the dorsal horn, with a higher density seen on the soma of alpha-motor neurons in the spinal cord (L3-S1), and all DRG cell types of normal rats1). In neuropathic pain model induced by nerve-ligation of L5 and L6 spinal nerves, showing tactile allodynia, a significant increase in alpha1B immunoreactivity was detected in lamina II of the dorsal horn and on the cell bodies of DRG cells depending the occurrence of allodynia1). From these observations they suggested the usefulness of N-type calcium channel blockers on pain. We have been screening non-peptidic compounds to block N-type calcium channel and found a novel compound. The novel compound has been demonstrated to block selectively N-type calcium channel in IMR-32 cells to L-type calcium channel in AtT-20 cells at the concentration of upto muM using the calcium indicator method. The compound has been cleared to decrease in barium current in IMR-32 cells using the patch clamp technique. Therefore our novel compound blocking N-type calcium channel might be useful for neuropathic pain treatment. Reference: 1. D. Cizkova et. al., in Abst of 9th World Congress on Pain, 134, 1999.

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