SOME OBSERVATIONS ON ANTIHISTAMINE ACTIVITY IN GUINEA-PIG OF ALIPHATIC 2,4-DIKETONES - NEW CLASS OF PHYSIOLOGICAL TISSUE COMPONENTS

  • 1 January 1977
    • journal article
    • letter
    • Vol. 17  (2) , 357-360
Abstract
Eight saturated aliphatic 2,4-diketones, ranging in chain length from C7-C21 were examined for their potency in counteracting the effects of histamine anaphylaxis in guinea pigs. A 0.2% suspension of the mixed C15, C17, C19 and C21 diketones was more effective than a 1% phenylephrine solution when these were administered as aerosols. Of the individual diketones, 2,4-nonadecanedione was the most potent in vivo. ED50 data for the antihistamine activity of the C7, C9, and C13 homologues in the in vitro guinea pig ileum bioassay indicated that, on a weight basis, the activity increased with increasing MW. The antiallergic activity of tissue and of urine extracts was attributed to the presence of 2,4-diketones. [Possible therapeutic applications are suggested, such as the treatment of asthma.].

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