Abstract
A novel class of tetrahydroindolone-derived carbamates has been discovered whose members are potent Kv1.5 blockers. The in vitro data show that compounds 6 and 29 are quite potent. They are also very selective over hERG (>450-fold) and L-type calcium channels (>450-fold).
MeSH terms
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Calcium Channels, L-Type / pharmacology
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Carbamates / chemistry*
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Carbamates / pharmacology*
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels / pharmacology
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Humans
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Indoles / chemistry*
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Indoles / pharmacology*
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Kv1.5 Potassium Channel / antagonists & inhibitors*
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Potassium Channel Blockers / chemical synthesis*
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Potassium Channel Blockers / pharmacology*
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Structure-Activity Relationship
Substances
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Calcium Channels, L-Type
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Carbamates
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels
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Indoles
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KCNH2 protein, human
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Kv1.5 Potassium Channel
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Potassium Channel Blockers