Journal of Pharmacological and Toxicological Methods 2005-01-01

A rapid, sensitive electron-capture gas chromatographic procedure for analysis of metabolites of N-methyl,N-propargylphenylethylamine, a potential neuroprotective agent.

Kay Rittenbach, B Duff Sloley, Lei Ling, Ronald T Coutts, Jackie Shan, Glen B Baker

Index: J. Pharmacol. Toxicol. Methods 52(3) , 373-8, (2005)

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Abstract

N-Methyl,N-propargyphenylethylamine (MPPE) is a novel analog of (-)-deprenyl, a drug prescribed for Parkinson's disease and shown to have neuroprotective and neurorescue properties in a wide variety of in vitro and in vivo models. MPPE is also neuroprotective, but has the advantage over (-)-deprenyl of not being metabolized to amphetamine or N-methylamphetamine.In this paper, extractive derivatization with pentafluorobenzenesulfonyl chloride (PFBSC) followed by electron-capture gas chromatography was utilized to study the metabolism of MPPE.The procedure is rapid and reproducible, giving derivatives with excellent chromatographic properties. Using this procedure, it has now been shown that beta-phenylethylamine (PEA), N-methylphenylethylamine (N-methylPEA) and N-propargylphenylethylamine (N-propargylPEA) are formed from MPPE during incubation of this drug with human liver microsomes. Levels of all three metabolites were shown to increase with increasing time of incubation with the microsomes.Extractive derivatization with PFBSC followed by electron-capture gas chromatography represents an efficient means of separating and quantitating the metabolites of MPPE, a novel neuroprotective agent.