Abstract
Some 4-(3,5-dimethylpyrazol) 5H-pyridazino [4,5-b]indoles (7), 1,2,4-triazolo [4,3-b]pyridazino [4,5-b]indoles (9) and 1,2,4-tetrazolo [4,5-b]pyridazino [4,5-b] indoles (11) substituted in position 1 by amino groups have been synthesized and tested as inotropic agents and inhibitors of platelet aggregation. 6-Imidazolyl-11H-1,2,4-triazolo [4,3-b]pyridazino [4,5-b]indole (9) shows an activity superior to that of amrinone, with a notable selectivity towards phosphodiesterase (PDE) IV and PDEV, vasodilator activity and a good effect on blood platelet aggregation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Aorta, Thoracic / drug effects
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Blood Platelets / drug effects
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Blood Platelets / enzymology
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Cardiotonic Agents / chemical synthesis*
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Cardiotonic Agents / pharmacology
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Dogs
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Female
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Guinea Pigs
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Heart Rate / drug effects
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Humans
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In Vitro Techniques
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Male
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Muscle Contraction / drug effects
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Muscle, Smooth, Vascular / drug effects
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Myocardial Contraction / drug effects
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Phosphodiesterase Inhibitors / chemical synthesis
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Phosphodiesterase Inhibitors / pharmacology
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Platelet Aggregation / drug effects
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Platelet Aggregation Inhibitors / chemical synthesis*
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Platelet Aggregation Inhibitors / pharmacology
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Pyridazines / chemical synthesis*
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Pyridazines / pharmacology
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Rats
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Rats, Wistar
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Thromboxane-A Synthase / antagonists & inhibitors
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Vasodilator Agents / chemical synthesis*
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Vasodilator Agents / pharmacology
Substances
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Cardiotonic Agents
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Indoles
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Phosphodiesterase Inhibitors
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Platelet Aggregation Inhibitors
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Pyridazines
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Vasodilator Agents
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Thromboxane-A Synthase