Synthesis and targeting of dihydropyridine carrier-mutual prodrug of tacrine
QU Ding
YANG Tie-hong
ZHANG Bang-le
HUAN Meng-lei
MEI Qi-bing
Abstract：Objective: To synthesize a chemical delivery system of tacrine (THA) in order to improve its brain targeting. Methods: THA was linked with chloroacetyl chloride, and then with nlcotlnamide. Finally pyri-dine quaternary ammonium was deoxidized to form the dihydropyridine carrier-mutual prodrug. Results: The struc-ture of the prodrug was determined by NMR and MS. The lipophilicity of prodrug was increased as compared with THA. The drug concentrations were higher in brain homogenates than in other tissue homogenates in vitro and in vi-vo. Conclusion: This dihydropyridine carder-mutual prodrug provides a good brain-targeting and slow release prop-erty, and is eliminated from the peripheral system easily.
Keywords：brain-targetingtacrinelipophilicitydihydropyridine carder-mutual prodrugHPLC
Publication Date：2010-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：4( 139-141,174 )