Synthesis and biological activity of the metabolites of syn-3-ethyl-7-methyl-3,7-diazabicyclo[3.3.1]non-9-yl 4-chlorobenzoate hydrochloride.
Five metabolites of syn-3-ethyl-7-methyl-3,7-diazabicyclo[3.3.1]non-9-yl 4-chlorobenzoate hydrochloride (YUTAC) (1) were prepared and examined for Na+ current blocking activity in guinea pig ventricular myocytes. These metabolites showed lower inhibitory activities than the parent compound or were inactive.
Tokushima Research Center, Pharmacokinetics Research Lab., Japan.
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Yamawaki
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Bukovac
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Sunami
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001643:Bridged Bicyclo Compounds / Q000378:metabolism*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002722:Chlorobenzenes; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006352:Heart Ventricles / Q000166:cytology / Q000187:drug effects; D009206:Myocardium / Q000378:metabolism; D015222:Sodium Channels / Q000187:drug effects / Q000502:physiology
D000889:Anti-Arrhythmia Agents; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002722:Chlorobenzenes; D015222:Sodium Channels; C045644:bisaramil