Abstract
The present paper reports on the synthesis and preliminary pharmacological properties of N-[beta-hydroxy-gamma-(N-phenylpiperazinepropyl)]-2- pyrrolidinone (MG-1). MG-1 was obtained by aminolysis of 1-(beta, gamma-epoxypropyl)-2-pyrrolidinone and N-phenylpiperazine. Its structure was established by elemental and spectral analyses (IR, UV, MS, 1H, 13C, 2D H-H and 2D C-H NMR). The antiarrhythmic activity of MG-1 was investigated on mice, rats and guinea pigs, using several models of arrhythmia. MG-1 attenuated or prevented the adrenaline- and barium chloride-induced arrhythmia. MG-1 demonstrated potent local anesthetic properties and depressed the depolarization phase of the action potential of cardiac cells. These results indicate that MG-1 possesses antiarrhythmic activity.
MeSH terms
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Animals
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Anti-Arrhythmia Agents / chemical synthesis
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Anti-Arrhythmia Agents / chemistry
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Anti-Arrhythmia Agents / pharmacology*
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Anti-Arrhythmia Agents / therapeutic use
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Arrhythmias, Cardiac / chemically induced
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Arrhythmias, Cardiac / drug therapy
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Electrocardiography / drug effects
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Female
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Guinea Pigs
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Magnetic Resonance Spectroscopy
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Male
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Mice
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Papillary Muscles / drug effects*
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Papillary Muscles / physiology
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Piperazines / chemical synthesis
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Piperazines / chemistry
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Piperazines / metabolism*
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Piperazines / therapeutic use
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Pyrrolidinones / chemical synthesis
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Pyrrolidinones / chemistry
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Pyrrolidinones / metabolism*
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Pyrrolidinones / therapeutic use
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Rats
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Rats, Wistar
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Spectrophotometry, Infrared
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Spectrophotometry, Ultraviolet
Substances
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Anti-Arrhythmia Agents
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Piperazines
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Pyrrolidinones
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N-(beta-hydroxy-gamma-(N-phenylpiperazinepropyl))-2-pyrrolidinone