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A new potential prodrug to improve the duration of L??dopa: L??3??(3??hydroxy??4??pivaloyloxyphenyl) alanine

…, Y Sawasaki, A Hisaka, H Takehana…

文献索引:Ihara; Tsuchiya; Sawasaki; Hisaka; Takehana; Tomimoto; Yano Journal of Pharmaceutical Sciences, 1989 , vol. 78, # 7 p. 525 - 529

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被引用次数: 20

摘要

Abstract L-3-(3-Hydroxy-4-pivaloyloxyphenyl) alanine (1, NB-355) is a novel L-dopa prodrug. After oral administration with carbidopa in rats, 1 demonstrated 2.3 times longer duration (MRT) and 1.4 times larger bioavailability (AUC) on plasma L-dopa concentrations than those of L-dopa itself. Similar results were obtained in dogs. The prolonged profile of L- dopa was parallel to that of carbidopa, and the intact ester was undetectable in rat plasma. ...