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.
MeSH terms
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Animals
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Calcium Channel Blockers / chemical synthesis
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Calcium Channel Blockers / chemistry
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Calcium Channel Blockers / pharmacology
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Calcium Channels, L-Type
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Calcium Channels, N-Type
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Drug Evaluation
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Inhibitory Concentration 50
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Models, Molecular
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Mollusk Venoms / chemical synthesis
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Mollusk Venoms / chemistry
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Mollusk Venoms / pharmacology
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Muscle, Smooth / chemistry
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Muscle, Smooth / cytology
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Phenyl Ethers / chemical synthesis
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Phenyl Ethers / chemistry*
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Phenyl Ethers / pharmacology*
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Rats
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Rats, Inbred Strains
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Snails / chemistry
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Structure-Activity Relationship
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omega-Conotoxins / chemical synthesis
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omega-Conotoxins / chemistry*
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omega-Conotoxins / pharmacology*
Substances
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Calcium Channel Blockers
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Calcium Channels, L-Type
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Calcium Channels, N-Type
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Mollusk Venoms
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Phenyl Ethers
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omega-Conotoxins
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ziconotide