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Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA

S Menzler, JA Bikker, N Suman-Chauhan…

文献索引:Menzler, Stefan; Bikker, Jack A.; Suman-Chauhan, Nirmala; Horwell, David C. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 4 p. 345 - 347

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被引用次数: 53

摘要

Omega-conotoxin MVIIA, a highly potent antagonist of the N-type voltage sensitive calcium channel, has shown utility in several models of pain and ischemia. We report a series of three alkylphenyl ether based analogues which mimic three key amino acids of the toxin. Two of the compounds have been found to exhibit IC50 values of 2.7 and 3.3 μM at the human N-type voltage sensitive calcium channel.