Abstract
The new compound thienodiltiazem was synthesized and investigated regarding structure-activity relations and calcium antagonistic properties. Isometric contraction force was measured in guinea-pig papillary muscles and chronotropic activity was studied in right atria of guinea pigs. Compared to the parent drug diltiazem (CAS 42399-41-7) the thieno derivative had a more potent negative chronotropic effect on spontaneously beating right atria and a more potent inotropic effect on papillary muscles. The negative inotropic action was reversed by increasing the extracellular calcium concentration.
MeSH terms
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Animals
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Calcium Channel Blockers / chemical synthesis*
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Calcium Channel Blockers / pharmacokinetics
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Calcium Channel Blockers / pharmacology*
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Calcium Chloride / antagonists & inhibitors
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Calcium Chloride / pharmacology
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Electric Stimulation
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Female
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Guinea Pigs
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Heart / drug effects*
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Heart Atria / drug effects
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In Vitro Techniques
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Indicators and Reagents
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Isometric Contraction / drug effects
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Magnetic Resonance Spectroscopy
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Male
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Myocytes, Cardiac / drug effects*
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Papillary Muscles / drug effects
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Thiazepines / chemical synthesis*
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Thiazepines / pharmacokinetics
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Thiazepines / pharmacology*
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Thiophenes / chemical synthesis*
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Thiophenes / pharmacokinetics
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Thiophenes / pharmacology*
Substances
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4-(2-dimethylaminoethyl)-4,5,6,7-tetrahydro-7-(4-methoxyphenyl)-5-oxothieno(2,3-b)(1,4)thiazepin-6-yl acetate
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Calcium Channel Blockers
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Indicators and Reagents
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Thiazepines
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Thiophenes
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Calcium Chloride