Monitoring the level of 14C-labelled selegiline following oral administration

H. Kalász, K. Tekes, Erzsébet B. Faigl, Zita Pöstényi, Eszter Berekméri, Gellért Karvaly, Ernest Adeghate

Research output: Contribution to journalArticle

Abstract

Background: Selegiline [(-)-deprenyl] is widely used for the treatment of Parkinson’s disease in humans. Objective: Time-dependence of tissue distribution of selegiline following per os administration to rats. Method: Oral administration of radiolabeled selegiline to rats resulted in a pattern of tissue distribution similar to that following intraperitoneal injection. Analyses were done using both reversed-phase HPLC and also by counting radioactivity in various body compartments of rats. Results: As a consequence of oral administration of 30 mg/kg of selegiline, its level in the stomach was extremely high (179.57 µg/g tissue through 54.67 µg/g at 15 min to 120 min), that is one magnitude higher than that in the serum level. High selegiline concentrations were also detected in the lacrimal glands (7.45 µg/g), kidneys (6.87 µg/g), livers (6.01 µg/g) and lungs (3.47 µg/g) after 30 minutes of application, which were higher than after intraperitoneal injections. Conclusion: The relatively high tissue levels remained for 120 min monitoring. Selegiline levels in the brain (1.69 µg/g) and in the testes (1.88 µg/g) were also considerably higher than following intraperitoneal administration during the entire period of observation (15 to 120 min).

Original languageEnglish
Pages (from-to)1-8
Number of pages8
JournalOpen Medicinal Chemistry Journal
Volume11
DOIs
Publication statusPublished - Jan 1 2017

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Selegiline
Oral Administration
Tissue Distribution
Intraperitoneal Injections
Lacrimal Apparatus
Radioactivity
Parkinson Disease
Testis
Stomach
High Pressure Liquid Chromatography
Observation
Kidney
Lung
Liver
Brain
Serum

Keywords

  • (-)-deprenyl
  • Distribution
  • HPLC
  • Oral administration
  • Rats
  • Selegiline

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery

Cite this

Monitoring the level of 14C-labelled selegiline following oral administration. / Kalász, H.; Tekes, K.; Faigl, Erzsébet B.; Pöstényi, Zita; Berekméri, Eszter; Karvaly, Gellért; Adeghate, Ernest.

In: Open Medicinal Chemistry Journal, Vol. 11, 01.01.2017, p. 1-8.

Research output: Contribution to journalArticle

Kalász, H. ; Tekes, K. ; Faigl, Erzsébet B. ; Pöstényi, Zita ; Berekméri, Eszter ; Karvaly, Gellért ; Adeghate, Ernest. / Monitoring the level of 14C-labelled selegiline following oral administration. In: Open Medicinal Chemistry Journal. 2017 ; Vol. 11. pp. 1-8.
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