Neurochemical Research

, Volume 38, Issue 4, pp 842–846

Rat Brain-Uptake Index for Phenylethylamine and Various Monomethylated Derivatives

  • Aron D. Mosnaim
  • Owen H. Callaghan
  • Thomas Hudzik
  • Marion E. Wolf
Original Paper

DOI: 10.1007/s11064-013-0988-1

Cite this article as:
Mosnaim, A.D., Callaghan, O.H., Hudzik, T. et al. Neurochem Res (2013) 38: 842. doi:10.1007/s11064-013-0988-1

Abstract

Phenylethylamine and its monomethylated derivatives p-methylphenylethylamine, α-methylphenylethylamine, phenylethylamine itself, N-methylphenylethylamine, o-methylphenylethylamine, and β-methylphenylethylamine, readily cross the blood-brain barrier showing a brain-uptake index (%) ± SD (water considered 100 %), of 108 ± 11, 98 ± 14, 83 ± 6, 78 ± 11, 62 ± 7 and 56 ± 6, respectively (injection of tritiated water and 100 μg standard amine, which was measured by gas-liquid chromatography). Similar brain-uptake index values (determined by double isotope counting) were obtained for phenylethylamine and α-methylphenylethylamine (amphetamine) after the injection of tritiated water and C14-labeled amine (either 3 μg or when added 100 μg standard compound), suggesting that they entered the brain via passive diffusion. Accordingly, both amines distributed rather evenly in the various rat brain areas examined: uptake index (%) ± SD (double isotope counting; non-, and diluted labeled amine) for phenylethylamine (89 ± 8 and 78 ± 7, 83 ± 9 and 86 ± 9, 96 ± 6 and 84 ± 7) and for α-methylphenylethylamine (88 ± 11 and 87 ± 9, 93 ± 14 and 87 ± 11, 97 ± 12 and 87 ± 9) for the cerebellum, frontal cortex, and striatum, respectively. These results will aid a greater understanding of the pharmacological and behavioral effects observed after the administration of phenylethylamine and methylphenylethylamine derivatives.

Keywords

Brain-uptake index Blood-brain barrier Phenylethylamine Monomethylated phenylethylamine derivatives Amphetamine 

Abbreviations

PEA

Phenylethylamine

p-MePEA

Para-methylphenylethylamine

α-MePEA

α-Methylphenylethylamine

AMPH

Amphetamine

N-MePEA

N-Methylphenylethylamine

o-MePEA

o-Methylphenylethylamine

β-MePEA

β-Methylphenylethylamine

BBB

Blood-brain barrier

BUI

Brain-uptake index

GLC

Gas-liquid chromatography

DIC

Double isotope counting

Copyright information

© Springer Science+Business Media New York 2013

Authors and Affiliations

  • Aron D. Mosnaim
    • 1
  • Owen H. Callaghan
    • 2
  • Thomas Hudzik
    • 3
  • Marion E. Wolf
    • 4
  1. 1.Neuroimmunopharmacology Laboratory, Department of Cellular and Molecular PharmacologyThe Chicago Medical School at Rosalind Franklin University of Medicine and ScienceN. ChicagoUSA
  2. 2.Department of Biochemistry and Molecular BiologyThe Chicago Medical School at Rosalind Franklin University of Medicine and ScienceN. ChicagoUSA
  3. 3.AbbvieN. ChicagoUSA
  4. 4.International Neuropsychiatry ConsultantsHighland ParkUSA

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