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Die Verstärkung des narkotischen Effekts und die Abbauhemmung von Hexobarbital durch Malonsäurederivate

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Summary

The potentiating effect of three malonic acid and one succinic acid derivatives on the duration of the anesthetic action of hexobarbital has been studied on rats and mice. It has been found that these substances inhibite the catabolism of hexobarbital in liver homogenates.

Some of the compounds studied were more potent in potentiating the hexobarbital anesthesia after oral administration.

The butyl-ethyl derivative prolonged the anesthesia on female rats twelve fould and on male rats only three fould. This difference were abolished by castration of the animals. In vitro, however, castration did not have any considerable influence on the hexobarbital-oxydation blocking activity of the compounds.

Pretreatment of rats with phenobarbital produce 1. a significant reduction of the anesthetic effect of hexobarbital, due to its more rapid metabolic oxydation, and 2. a nearly complete loss of activity of the butyl-ethylmalonic acid ester to potentiate the hexobarbital effect. On the increased hexobarbital oxydation in liver homogenates from phenobarbital pretreated rats, the phenyl-ethyl- and the butyl-ethyl malonic acid derivatives do not have any blocking activity.

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Authors and Affiliations

  1. Aus dem pharmakologischen Laboratorium der Società Italiana Prodotti Schering, Milano

    M. Kramer & E. Arrigoni-Martelli

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  1. M. Kramer
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  2. E. Arrigoni-Martelli
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Herrn Professor Dr. W. S. Loewe, Salt Lake City, zum 75. Geburtstag gewidmet.

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Kramer, M., Arrigoni-Martelli, E. Die Verstärkung des narkotischen Effekts und die Abbauhemmung von Hexobarbital durch Malonsäurederivate. Naunyn - Schmiedebergs Arch 237, 264–275 (1959). https://doi.org/10.1007/BF00244734

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  • DOI: https://doi.org/10.1007/BF00244734

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