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Rat Brain-Uptake Index for Phenylethylamine and Various Monomethylated Derivatives

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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.

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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

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Acknowledgments

This research was supported, in part, by The National Migraine Foundation, Chicago, IL. We appreciate the skilful technical assistance of Mr. Sampsom Myles.

Conflict of interest

The authors declare that they have no conflict of interest.

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Authors and Affiliations

  1. Neuroimmunopharmacology Laboratory, Department of Cellular and Molecular Pharmacology, The Chicago Medical School at Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, N. Chicago, IL, 60064, USA

    Aron D. Mosnaim

  2. Department of Biochemistry and Molecular Biology, The Chicago Medical School at Rosalind Franklin University of Medicine and Science, N. Chicago, IL, 60064, USA

    Owen H. Callaghan

  3. Abbvie, N. Chicago, IL, 60064, USA

    Thomas Hudzik

  4. International Neuropsychiatry Consultants, Highland Park, IL, 60035, USA

    Marion E. Wolf

Authors
  1. Aron D. Mosnaim
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  2. Owen H. Callaghan
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  3. Thomas Hudzik
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  4. Marion E. Wolf
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Corresponding author

Correspondence to Aron D. Mosnaim.

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Mosnaim, A.D., Callaghan, O.H., Hudzik, T. et al. Rat Brain-Uptake Index for Phenylethylamine and Various Monomethylated Derivatives. Neurochem Res 38, 842–846 (2013). https://doi.org/10.1007/s11064-013-0988-1

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  • DOI: https://doi.org/10.1007/s11064-013-0988-1

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