Subasinghe, Nalin L. published the artcileA novel series of pyrazolylpiperidine N-type calcium channel blockers, HPLC of Formula: 871332-95-5, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(12), 4080-4083, database is CAplus and MEDLINE.
Selective 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-mol. 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.
Bioorganic & Medicinal Chemistry Letters published new progress about 871332-95-5. 871332-95-5 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (4-Chloro-3-cyanophenyl)boronic acid, and the molecular formula is C5H11NO2S, HPLC of Formula: 871332-95-5.
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