title: Rat brain-uptake index for phenylethylamine and various monomethylated derivatives.
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 C(14)-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.
authors: 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.Mosnaim@rosalindfranklin.edu
authors: Aron D
authors: AD
authors: Mosnaim
authors: Owen H
authors: OH
authors: Callaghan
authors: Thomas
authors: T
authors: Hudzik
authors: Marion E
authors: ME
authors: Wolf
mesh_terms: D000661:Amphetamine / Q000493:pharmacokinetics*; D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism*; D001921:Brain / Q000378:metabolism*; D002250:Carbon Radioisotopes; D008297:Male; D008694:Methamphetamine / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D010627:Phenethylamines / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014316:Tritium
chemical_list: D002250:Carbon Radioisotopes; D010627:Phenethylamines; C027141:N-methylphenethylamine; D014316:Tritium; D008694:Methamphetamine; D000661:Amphetamine
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