Literature DB >> 1772533

Simultaneous delivery of valproic acid and glycine to the brain. Deamination of 2-propylpentylglycinamide by monoamine oxidase B.

P H Yu1, B A Davis.   

Abstract

2-Propylpentylglycinamide (2-PPG), a branched aliphatic amine derivative, was found to be readily deaminated by rat liver monoamine oxidase B in vitro and in vivo. The deamination leads to production of 2-propyl-1-pentaldehyde, which can be subsequently converted to valproic acid (VPA), and glycinamide, which is then subsequently converted to glycine. Absorption and biotransformation of a single ip dose of 2-PPG into blood as well as transfer of the drug and its metabolite into the brain were rapid processes. Although VPA (an anticonvulsant) and glycine (an inhibitory neurotransmitter) can be detected in the brain following administration of 2-PPG, its anticonvulsant action cannot be determined. 2-PPG at relatively low doses exhibited distinct tremor effects. Furthermore, 2-PPG appeared to potentiate the convulsant effect induced by pentylenetetrazol.

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Year:  1991        PMID: 1772533     DOI: 10.1007/bf03161055

Source DB:  PubMed          Journal:  Mol Chem Neuropathol        ISSN: 1044-7393


  1 in total

Review 1.  Progress in drug delivery to the central nervous system by the prodrug approach.

Authors:  Barbara Pavan; Alessandro Dalpiaz; Nunzia Ciliberti; Carla Biondi; Stefano Manfredini; Silvia Vertuani
Journal:  Molecules       Date:  2008-05-01       Impact factor: 4.411

  1 in total

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