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

• Whole body autoradiography of 14C-methyl-selegiline was studied in rats.
• Blood, CSF and tissue distribution of selegiline was measured by HPLC.
• Data verified both BBB and blood–testis barrier's penetration of the compound.
• Binding of selegiline to the MAO enzyme both in brain and testis is suggested.

Tissue distribution of selegiline including N-methyl-14C-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-14C-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.

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