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Neuropharmacological and neurochemical properties of N‐(2‐cyanoethyl)‐2‐phenylethylamine, a prodrug of 2‐phenylethylamine
Author(s) -
Baker Glen B.,
Coutts Ronald T.,
Rao Tadimeti S.
Publication year - 1987
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1987.tb11318.x
Subject(s) - neurochemical , prodrug , pharmacology , dopamine , phenethylamine , chemistry , neurotransmitter , metabolite , biogenic amine , pharmacokinetics , biochemistry , endocrinology , biology , receptor
1 N‐(2‐cyanoethyl)‐2‐phenylethylamine (CEPEA) was examined as a possible prodrug of 2‐phenylethylamine (PEA). 2 Pharmacokinetics of PEA and CEPEA were investigated in rat brain, blood and liver by gas chromatography with electron‐capture detection (GC‐ECD). Interactions of PEA and CEPEA with putative neurotransmitter amines were investigated by use of high performance liquid chromatography with electrochemical detection (h.p.l.c.‐e.c.). 3 Administration of PEA caused transient increases in PEA concentrations which decreased rapidly in brain and blood and at a slower rate in liver. Administration of CEPEA caused sustained elevations of PEA concentrations and elimination of PEA was markedly decreased in these tissues relative to the situation after administration of PEA itself. 4 Administration of CEPEA caused more prolonged decreases in brain noradrenaline, dopamine and 5‐hydroxytryptamine concentrations than those observed after PEA administration, although values increased to control levels eventually.