Abstract
A novel brain-targeted catechol derivative was designed for the potential in vivo induction of nerve growth factor (NGF) biosynthesis within the central nervous system (CNS) after its peripheral administration. The dihydropyridine-pyridinium salt moiety integrated in the structure of the catechol and conferred the brain-selective delivery property to the molecule. After preliminary in vitro evaluation of this brain-targeted derivative and its pyridinium metabolite, in vivo tissue distribution studies demonstrated the selective and sustained delivery of the compound of interest to the brain of a rat. Furthermore, the significant in vitro biological activity of the novel catechol derivative that was demonstrated in the L-M cell line is encouraging for the expected NGF-inducing activity of this novel catechol derivative in vivo.
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