Roles of Hydrophobicity, Protein Binding and the Probenecid-Sensitive Transport System in the Cerebrospinal Fluid Delivery of Nucleoside Analogues with Anti-viral Activity

Ten nucleoside analogues with anti-herpes or anti-HIV activity were investigated for their transport into the cerebrospinal fluid (CSF) following intravenous administration in rats. The novel anti-herpes agent 1-β-D-arabinofuranosyl-2-thio-5-fluorocytosine (5F-araSC) showed the highest CSF/plasma co...

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Bibliographic Details
Published in:Biological & pharmaceutical bulletin 2000/08/01, Vol.23(8), pp.979-983
Main Authors: KAWAGUCHI, Takeo, KUSUMI, Masaki, HASEGAWA, Tetsuya, NAGATA, Toshiyuki, SANEYOSHI, Mineo, NAKANO, Masahiro, HAMADA, Akinobu
Format: Article
Language:English
Subjects:
1-^b-D-arabinofuranosyl-2-thio-5-fluorocytosine
1-b-Arabinofuranosyl-2-thio-5-fluorocytosine
acyclovir
Animals
anti-viral activity
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Antiviral Agents - administration & dosage
Antiviral Agents - cerebrospinal fluid
Biological and medical sciences
Biological Transport
cerebrospinal fluid
Herpesvirus
Human immunodeficiency virus
hydrophobicity
Male
Medical sciences
nucleoside analogs
nucleoside analogue
nucleoside analogues
Nucleosides - administration & dosage
Nucleosides - cerebrospinal fluid
Pharmacology. Drug treatments
probenecid
Probenecid - pharmacology
Protein Binding
Rats
Rats, Wistar
transport
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Description
Summary:Ten nucleoside analogues with anti-herpes or anti-HIV activity were investigated for their transport into the cerebrospinal fluid (CSF) following intravenous administration in rats. The novel anti-herpes agent 1-β-D-arabinofuranosyl-2-thio-5-fluorocytosine (5F-araSC) showed the highest CSF/plasma concentration ratio (>20%), while that of acyclovir (ACV) was very low (
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.23.979