Abstract
The synthesis of (2RS)-1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol ((RS)-9) and its enantiomers has been described and tested for electrocardiographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for alpha(1)-, alpha(2)- and beta(1)-adrenoceptors' binding affinities. All compounds significantly decrease systolic and diastolic blood pressure, and possess antiarrhythmic activity and affinity to alpha(1)-, alpha(2)- and beta(1)-adrenoceptors. The results suggest that the antiarrhythmic and hypotensive effects of these compounds are related to their adrenolytic but not spasmolytic properties.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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2-Propanol
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Adrenergic Antagonists / chemical synthesis*
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Adrenergic Antagonists / pharmacology
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Animals
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Anti-Arrhythmia Agents / chemical synthesis
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Arrhythmias, Cardiac / drug therapy
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Electrocardiography
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Hypotension / drug therapy
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Parasympatholytics / chemical synthesis
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Propanolamines / chemical synthesis*
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Propanolamines / pharmacology
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Propanols / chemical synthesis*
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Propanols / pharmacology
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Rabbits
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Rats
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Receptors, Adrenergic / metabolism*
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Receptors, Adrenergic, alpha-1 / metabolism
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Receptors, Adrenergic, beta-1 / metabolism
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Spasm / drug therapy
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Stereoisomerism
Substances
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1-(1H-indol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)propan-2-ol
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Adrenergic Antagonists
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Anti-Arrhythmia Agents
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Indoles
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Parasympatholytics
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Propanolamines
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Propanols
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Receptors, Adrenergic
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Receptors, Adrenergic, alpha-1
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Receptors, Adrenergic, beta-1
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2-Propanol