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J Pharm Biomed Anal. 2015;111:147-52. doi: 10.1016/j.jpba.2015.03.022. Epub 2015 Mar 30.

Distribution of N-methyl-(14)C-labeled selegiline in the rat.

Author information

1
Department of Pharmacodynamics, Semmelweis University, Budapest, Hungary. Electronic address: drtekes@gmail.com.
2
Department of Pharmacology and Pharmacotherapy, Semmelweis University, Budapest, Hungary; National Research Institute for Radiobiology and Radiohygenie, Budapest, Hungary.
3
Laboratory of Synthesis, Institute of Isotopes, Co., Ltd. Budapest, Hungary.
4
Department of Pharmacodynamics, Semmelweis University, Budapest, Hungary.
5
Radiopharmacy Laboratories, Ltd., Budaörs, Hungary.
6
Department of Nuclear Medicine, University of Debrecen, Debrecen, Hungary.
7
National Research Institute for Radiobiology and Radiohygenie, Budapest, Hungary.
8
Department of Pharmacology and Pharmacotherapy, Semmelweis University, Budapest, Hungary. Electronic address: drkalasz@gmail.com.

Abstract

Tissue distribution of selegiline including N-methyl-(14)C-selegiline was studied with three different techniques. Whole body autoradiography of labeled selegiline in rats completed the former results obtained in mice. Counting radioactivity by liquid scintillation method in various body compartments gave an in-depth numerical estimation of distribution, while RP-HPLC determination of selegiline determined the fate of intact, non-metabolized parent compound. Whole body autoradiography following 15 and 60 min of intraperitoneal application of N-methyl-(14)C-selegiline verified definite and time-dependent blood-brain penetration of selegiline. Quantitative determination of tissue concentrations by liquid scintillation and RP-HPLC methods following 5, 15, 60 and 180 min of intraperitoneal administration of selegiline unanimously verified both blood-brain and blood-testis penetration of the compound through the barrier.

KEYWORDS:

HPLC; Radiolabeled ligand; Rat; Selegiline; Whole body autoradiography

PMID:
25886391
DOI:
10.1016/j.jpba.2015.03.022
[Indexed for MEDLINE]

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