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Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA
S Menzler1, J A Bikker, N Suman-Chauhan
1Parke-Davis Neuroscience Research Centre, Cambridge, UK.
Bioorganic & Medicinal Chemistry Letters
|March 14, 2000
Abstract:
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 microM at the human N-type voltage sensitive calcium channel.