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Arzneimittelforschung 2007; 57(12): 757-761
DOI: 10.1055/s-0031-1296676
Cardiac Drugs · Cardiac Stimulants · Coronary Drugs
Editio Cantor Verlag Aulendorf (Germany)

Synthesis and Biological Activity of Thienodiltiazem in Isolated Heart Muscle Preparations of Guinea Pigs

Norbert Handler
1   Department of Pharmaceutical and Medicinal Chemistry, University of Vienna, Vienna, Austria
,
Thomas Erker
1   Department of Pharmaceutical and Medicinal Chemistry, University of Vienna, Vienna, Austria
,
Rosa Lemmens-Gruber
2   Department of Pharmacology and Toxicology, University of Vienna, Vienna, Austria
,
Christian R. Studenik
2   Department of Pharmacology and Toxicology, University of Vienna, Vienna, Austria
› Author Affiliations
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Publication History

Publication Date:
21 December 2011 (online)

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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 chro-notropic 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.

Key words

Antihypertensives - Calcium channel antagonists - Diltiazem - Thienodiltiazem, calcium antagonistic activity, papillary muscles, right atria