In Brief

Abstract

To the blood–brain barrier, drugs are just another foreign material that needs to be excluded from the constant chemical milieu that bathes the brain. A new strategy for sneaking drugs past this barrier uses a drug–vitamin C conjugate. Vitamin C is found in the brain in high concentrations, and researchers at the University of Ferrara in Italy, have discovered the vitamin C transport-regulating receptor (SVCT2) responsible for this transfer. In a recent study, three drugs that normally exhibit slow uptake into the brain (nipecotic acid, kynurenic acid and diclofenamic acid) were conjugated to vitamin C [J. Med. Chem. (2002) 45, 559–562]. All three conjugates competitively inhibited the transport of vitamin C in human retinal pigment epithelial cells rich in SVCT2. An initial mouse model study, using the nipecotic acid conjugate to allay convulsions appears promising, but clinical trials are yet to be arranged. Stefano Manfredini, lead investigator in the study and a professor of pharmaceutical chemistry at the University, hopes the study will lead to a way of delivering Alzheimer's, antiretroviral, antiepileptic and other CNS medication. S de B