Abstract
The intensive SAR study of 3,4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC(50)=41+/-1 nM) against T-type calcium channel and its potency is nearly comparable to that of Kurtoxin. As a small organic molecule, this compound showed the highest blocking activity reported to date.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Calcium Channel Blockers / chemistry*
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Calcium Channel Blockers / pharmacology*
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Calcium Channels, T-Type / drug effects*
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Cell Line
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Humans
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Quinazolines / chemistry*
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Quinazolines / pharmacology*
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Structure-Activity Relationship
Substances
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Calcium Channel Blockers
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Calcium Channels, T-Type
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Quinazolines