Determination of adiphenine, diphenylacetic acid and diethylaminoethanol by high-performance liquid chromatography

Veyre

et al. 1986

Biopharm & Drug Disp

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This study describes the behaviour of a dual labelled drug, adiphenine, in the rat brain. Macroautoradiographies show images of the brain at different times after injection. Some of the tissue metabolites are identified at the brain level and the passage of the blood brain barrier is compared with tritiated water. The obtained data give very interesting indications on the blood brain distribution and on the metabolism at the brain level. Different techniques of high pressure liquid chromatography, macro- and histoautoradiographies allowed us to visualize how the drug is fixed on cerebral structures, giving indications on its mechanism of action. This fat soluble compound freely crosses the normal blood brain barrier and if labelled with the appropriate emittor could be very useful in nuclear medicine to obtain imaging of the brain.

“…Chromatographic properties of compounds were expressed as retention times (Rt). 8 The mobile phase consisted of a non-linear gradient from two mobile phases:…”

Section: High Pressure Liquid Chromatography (Hplc)mentioning

confidence: 99%

Brain uptake of labelled adiphenine in rats

Veyre

et al. 1986

Biopharm & Drug Disp

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Synthèse et distribution tissulaire chez le rat du Phénylacétate de Diéthylamino‐2 éthyle marqué par ¹⁴C

Labelled Comp Radiopharmac

Labarre

et al. 1987

Adiphenine plasma levels and blood-brain barrier crossing in the rat

European Journal of Drug Metabolism and Pharmacokinetics

Veyre

et al. 1985

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Adiphenine was administered in 3H-labelled form in doses of 15 mumole/kg intravenously to male Wistar rats. Plasma and brain levels of the unchanged drug were measured. The elimination of the 3H-labelled compound from the plasma was monophasic with a half-life of 13 minutes. The unchanged drug was detectable in the plasma for 30 minutes after the injection. The time course of brain levels of unchanged drug paralleled that found in the plasma with a half-life of 9 to 12 minutes. In all experiments, brain and plasma levels of unchanged adiphenine correlate highly.