Abstract
We report the preliminary in vitro characterization of a series of pyrimidines as a new chemotype that modulates cardiovascular parameters and relaxes ileum smooth muscle according to classical calcium entry blockers. Tested compounds showed an interesting negative inotropic selectivity. In patch-clamp experiments they block L- over T-type calcium currents. Two requisites seem essential for the activity: lipophilic substituents in positions 2 and 5 of the pyrimidine ring and the acetamidic function in position 6.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminopyridines / chemical synthesis
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Aminopyridines / pharmacology*
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Animals
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Calcium Channel Blockers / pharmacology*
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Calcium Channels, L-Type / drug effects
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Guinea Pigs
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Heart Rate / drug effects
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Patch-Clamp Techniques
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Pyrimidines / chemical synthesis
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Pyrimidines / pharmacology*
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Structure-Activity Relationship
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Vasodilator Agents / pharmacology
Substances
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Aminopyridines
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Calcium Channel Blockers
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Calcium Channels, L-Type
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Pyrimidines
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Vasodilator Agents
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pyrimidine-2-thiol