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The rat brain as a "deep compartment" in the kinetics of a common metabolite of prochlorperazine and perphenazine.

作者信息

Jahns I, Breyer U

出版信息

Drug Metab Dispos. 1976 Nov-Dec;4(6):522-9.

PMID:11973
Abstract

N-[gamma-(2-Chlorophenothiazin-10-yl)propyl]ethylenediamine (Cl-PPED), a common metabolite of prochlorperazine and perphenazine, was orally administered to male rats at a dose of 50 mg/kg, and its concentrations in plasma, liver, lung, kidney, and brain were followed from 6 hr to 40 days after dosage. Small quantities were measured by two-dimensional thin-layer chromatography of a fluorescent derivative and in situ fluorometry of the chromatograms. The kinetic behavior of Cl-PPED in brain differed from that in other tissues in that the concentration maximum was achieved later and the elimination half-life was distinctly longer (8 days vs. 1.2-3 days). Cl-PPED was evenly among the three major brain regions. Subcellular fractionation of liver and brain revealed preferential localization in mitochondria.

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