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

✍ Scribed by Stefan Menzler; Jack A Bikker; Nirmala Suman-Chauhan; David C Horwell

• Book ID: 104364981
• Publisher: Elsevier Science
• Year: 2000
• Tongue: English
• Weight: 238 KB
• Volume: 10
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(99)00699-x

✦ Synopsis

AbstractÐOmega-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 IC 50 values of 2.7 and 3.3 mM at the human N-type voltage sensitive calcium channel.