A. Kourounakis et al., SYNTHESIS AND EVALUATION OF A BRAIN-TARGETED CATECHOL DERIVATIVE AS APOTENTIAL NGF-INDUCER, International journal of pharmaceutics, 141(1-2), 1996, pp. 239-250
A novel brain-targeted catechol derivative was designed for the potent
ial 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 structur
e of the catechol and conferred the brain-selective delivery property
to the molecule. After preliminary in vitro evaluation of this brain-t
argeted derivative and its pyridinium metabolite, in vivo tissue distr
ibution studies demonstrated the selective and sustained delivery of t
he compound of interest to the brain of a rat. Furthermore, the signif
icant in vitro biological activity of the novel catechol derivative th
at was demonstrated in the L-M cell line is encouraging for the expect
ed NGF-inducing activity of this novel catechol derivative in vivo.