Microbial Conversion of EM574 and EM523, Gastrointestinal Motor Stimulating Agents.
نویسندگان
چکیده
منابع مشابه
Microbial conversion of EM574 and EM523, gastrointestinal motor stimulating agents.
EM574 exerts gastrointestinal motor stimulating (GMS) activity even after being converted to its metabolites P1 and P2 in dogs. These metabolites were isolated from dog liver using a series of chromatographic procedures. Their structures were determined to be the 15- and 14-hydroxyl derivatives of EM574, respectively, by spectral analysis. Large scale preparation by microbial transformation was...
متن کاملBioactive metabolites of EM574 and EM523, erythromycin derivatives having strong gastrointestinal motor stimulating activity.
Two motilides, EM574 (N-demethyl-N-isopropyl-8,9-anhydroerythromycin A 6,9-hemiacetal) and EM523 (N-demethyl-N-ethyl-8,9-anhydroerythromycin A 6,9-hemiacetal) have strong gastrointestinal motor stimulating (GMS) activity. When administered orally to dogs, these agents showed strong GMS activity, but their plasma levels were very low and the metabolites which have been determined so far using th...
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The motor-stimulating action of de(N-methyl)-N-isopropyl-8,9-anhydroerythromycin A 6,9-hemiacetal (EM574) on the upper gastrointestinal tract was studied in fasted conscious dogs using chronically implanted force transducers and compared with those of porcine motilin and cisapride. EM574 induced gastric phase III-like migrating contractions and increased the plasma motilin levels slightly. The ...
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ژورنال
عنوان ژورنال: The Journal of Antibiotics
سال: 1996
ISSN: 0021-8820,1881-1469
DOI: 10.7164/antibiotics.49.802