The regional localization of a new potent centrally acting antihypertensive agent R 28935 and its less active threo isomer R 29814 in the cat brain

A.J.M. Loonen, W. Soudijn, H.H. Van Rooy, I. Van Wijngaarden

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    Abstract

    Systemic administration of the centrally acting antihypertensive agent R 28935 to cats resulted in a long lasting decrease of mean arterial pressure (±30%) whereas the same dose of the threo-isomer R 29814 was ineffective. The antihypertensive activity was due to the unaltered drug. In spite of an identical log P, pKa, dose and a comparable plasma level, the concentration of R 28935 in all the brain areas tested was about twice that of the threo-isomer, suggesting a stereoselective uptake and/or binding of R 28935.
    Original languageEnglish
    Pages (from-to)281-285
    Number of pages5
    JournalEuropean Journal of Pharmacology
    Volume45
    Issue number3
    DOIs
    Publication statusPublished - 22-Apr-1977

    Keywords

    • 1 [1 [2 (1,4 benzodioxan 2 yl) 2 hydroxyethyl] 4 piperidyl] 2 benzimidazolinone
    • radioisotope
    • tritium
    • unclassified drug
    • blood pressure
    • brain
    • cat
    • drug absorption
    • drug binding
    • drug distribution
    • drug isomer
    • erythro 1 {1 [2 (2,3 dihydro 1,4 benzodioxin 2 yl) 2 hydroxyethyl] 4 piperidinyl} 1,3 dihydro 2h benzimidazol 2 one h 3
    • pharmacokinetics
    • plasma
    • stereochemistry
    • theoretical study
    • threo 1 {1 [2 (2,3 dihydro 1,4 benzodioxin 2 yl) 2 hydroxyethyl] 4 piperidinyl} 1,3 dihydro 2h benzimidazol 2 one h 3

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