Summary
Adiphenine was administered in3H-labelled form in doses of 15 u.mole/kg intravenously to male Wistar rats. Plasma and brain levels of the unchanged drug were measured.
The elimination of the3H -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.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Lehmann G. and Knoeffel P.K. (1942): The spasmolytic and local anesthetic action of some derivatives of fluorene-carboxylic acid and related compounds. J. Pharmac. exp. Ther.,74, 274–283.
Mornex R., Jordan D. and Cretin A. (1973): Libération de TSH par l’antéhypophyse de rat sous l’influence de diethyl amino 2 ethyle. C R. Acad. Sci.,276, 2289–2292.
Jordan D., Ponsin G., Mornex R., Fevre M., Poncet C. and Rostagnat A. (1977): Comparison of adiphenine and TRH effects on T SH release by rat pituitary in vitro. Eur. J. Pharmacol,41, 53–58.
Fevre M., Jordan D., Tourniaire J. and Mornex R. (1979): Comparison of pharmacological effect of adiphenine and physiological stimulation by luteinizing hormone releasing hormone or luteinizing hormone release by rat anterior pituitaries in vitro. Can. J. Physiol. Pharmacol.,57, 1388–1392.
Michelot J., Madelmont J.C., Jordan D., Mornex R. and Meyniel G. (1981): Metabolism of adiphenine. I. Absorption, distribution and excretion in rats and mice. Xenobiotica,11, 123–130.
Michelot J., Madelmont J.C., Rousset B., Labarre P., Mornex R. and Meyniel G. (1982): Metabolism of adiphenine. II. Identification of major excretion metabolites in rats. Xenobiotica,12, 457–462.
Kung H.F. and Blau M. (1980): Regional intracellular pH shift: a proposed new mechanism for radiopharmaceutical uptake in brain an dother tissues. J. Nucl. Med.,21, 147–152.
Michelot J., Moreau M.F., Madelmont J.C., Labarre P. and Meyniel G. (1983): Determination of adiphenine, diphenylacetic acid and diethyl-aminoethanol by highperformance liquid chromatography. J. of Chromatography,257, 395–399.
Kung H.F., Tramposch K.M. and Blau M. (1983): A new brain perfusion imaging agent: [1-123] HIPDM: N, N, N’-Trimethyl-N’-[2-Hydroxy-3-methyl-5-iodobenzyl] 1,3-Propanediamine. J. Nucl. Med.,24, 66–72.
Oldendorf W.H. (1981) Clearance of radiol abeled substances by brain after arterial injection using a diffusible internal standard. In: Research Methods in neurochemistry, vol. 5, chap. 4, p. 91-112, edited by Neville Marks, and Richard Rodnight (Plenum Publishing Corporation, 1981).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Michelot, J., Moreau, M.F., Veyre, A. et al. Adiphenine plasma levels and blood-brain barrier crossing in the rat. European Journal of Drug Metabolism and Pharmacokinetics 10, 273–278 (1985). https://doi.org/10.1007/BF03189754
Received:
Issue Date:
DOI: https://doi.org/10.1007/BF03189754