To improve the entry of certain drugs into brain, ascorbic acid (AA) conjugates of these drugs were synthesized and their capacity to interact with SVCT2 ascorbate transporters was explored. Kinetic studies clearly indicate that all of the conjugates were able to competitively inhibit ascorbate transport in human retinal pigment epithelial cells (HRPE). In vivo studies, in a mouse model system, demonstrate that conjugate 3 is better absorbed compared to the nonconjugated parent drug.

Design, synthesis and activity of ascorbic acid prodrugs of nipecotic, kynurenic and diclophenamic acids, liable to increase neurotropic activity.

MANFREDINI, Stefano;PAVAN, Barbara;VERTUANI, Silvia;BIONDI, Carla;SCATTURIN, Angelo;TANGANELLI, Sergio;FERRARO, Luca Nicola;DALPIAZ, Alessandro
2002

Abstract

To improve the entry of certain drugs into brain, ascorbic acid (AA) conjugates of these drugs were synthesized and their capacity to interact with SVCT2 ascorbate transporters was explored. Kinetic studies clearly indicate that all of the conjugates were able to competitively inhibit ascorbate transport in human retinal pigment epithelial cells (HRPE). In vivo studies, in a mouse model system, demonstrate that conjugate 3 is better absorbed compared to the nonconjugated parent drug.
2002
Manfredini, Stefano; Pavan, Barbara; Vertuani, Silvia; Scaglianti, M.; Compagnone, D.; Biondi, Carla; Scatturin, Angelo; Tanganelli, Sergio; Ferraro, Luca Nicola; Prasad, P.; Dalpiaz, Alessandro
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/516426
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