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. After intravenous administration in rats, 1 was converted quickly and completely to L-dopa in the systemic circulation. It was also noted that the oral LD50 value of 1 was greater than 6 g/kg in mice. These data suggest that 1 will offer long-lasting L-dopa therapy for the treatment of Parkinson's disease with little concern about toxicity.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Ihara M,Tsuchiya Y,Sawasaki Y,Hisaka A,Takehana H,Tomimoto K,Yano Mdoi
10.1002/jps.2600780703subject
Has Abstractpub_date
1989-07-01 00:00:00pages
525-9issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(15)48020-7journal_volume
78pub_type
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