Cardiotonic action of ring A-modified cardenolides, with special reference to cleavage of the ring.
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- TSURU Hiromichi
- Department of Pharmacology, Nagoya University School of Medicine
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- ISHIKAWA Naohisa
- Department of Pharmacology, Nagoya University School of Medicine
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- SHIGEI Tatsuro
- Department of Pharmacology, Nagoya University School of Medicine
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- ANJYO Takako
- Tokyo Biochemical Research Institute
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- OKADA Masashi
- Tokyo Biochemical Research Institute
Bibliographic Information
- Other Title
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- Cardiotonic action of ring A modified c
- INVOLVEMENT OF HISTAMINE H1- AND H2-RECEPTORS IN INDUCED ASTHMAS IN DOGS
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Abstract
Cardiotonic activities of six newly synthesized ring A-modified cardenolides, four 3, 5-seco-4-nor-cardenolides and two 4-oxa-cardenolides, were studied in isolated frog hearts and guinea pig atria. These compounds were 14-hydroxy-3, 5-seco-4-nor-5-oxo-l4β-card-20(22)-enolid-3-oic acid (IIa), and its methyl ester (IIb); 5β, 14 and 5α, 14-dihydroxy-3, 5-seco-4-nor-14β, -card-20(22)-enolid-3-ols (IIIa and IIIb); 3-dehydro-4-oxa-uzarigenin (IVa) and 3-dehydro-4-oxa-digitoxigenin (1Vb). In the frog heart (Straub's preparation), positive inotropic effects were demonstrated with all compounds except IIa. The pattern of response was the same as that to digitoxigenin (I). The relative potencies obtained on the basis of the concentration of each compound in which a contracture was brought about, the potency of I being taken as standard, were as follows: I (1.0), IIa (-), IIb (0.03-0.1), IIIa (0.01), IIIb (<0.01), IVa (<0.01), and IVb (0.03-0.1). The positive isotropic effect of IIb was also confirmed in guinea pig atria. IIb and IVb potentiated dose-dependently the K-contracture of the frog ventricular muscle just as was seen with I, indicating that the cardiotonic activity of the compounds is the same in nature as that of digitoxigenin. It was clearly demonstrated that the perhydrocyclopentanophenanthrene nucleus is not an indispensable requirement for cardiotonic activity.
Journal
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- The Japanese Journal of Pharmacology
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The Japanese Journal of Pharmacology 27 (6), 799-805, 1977
The Japanese Pharmacological Society
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Keywords
Details 詳細情報について
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- CRID
- 1390282679267230720
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- NII Article ID
- 130000839234
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- NII Book ID
- AA00691188
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- COI
- 1:CAS:528:DyaE1cXpvV2gtw%3D%3D
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- ISSN
- 13473506
- 00215198
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- NDL BIB ID
- 1916959
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- PubMed
- 609150
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed