Low blood-brain barrier permeability to azidothymidine (AZT), 3TC(TM), and thymidine in the rat

Brain Research

Volumn 791, Issue 1-2, 1998, Pages 313-316

  Wu, Dafang ^a   Clement, John G ^b   Pardridge, William M ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b Shire Canada   (Canada)

Author keywords

Blood brain barrier; Lamivudine; Lipid solubility; Thymidine; Zidovudine

Indexed keywords

LAMIVUDINE; THYMIDINE; ZIDOVUDINE;

ANIMAL EXPERIMENT; ANTIVIRAL ACTIVITY; ARTICLE; BLOOD BRAIN BARRIER; DRUG PENETRATION; DRUG TRANSPORT; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; ANTI-HIV AGENTS; BLOOD-BRAIN BARRIER; DRUG EVALUATION, PRECLINICAL; LAMIVUDINE; MALE; RATS; RATS, SPRAGUE-DAWLEY; THYMIDINE; ZIDOVUDINE;

EID: 0032571761     PISSN: 00068993     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-8993(98)00139-5     Document Type: Article

References (20)

1. 14C]thymidine in mice. J. Pharmacol. Exp. Ther. 257:1991;479-486.
2. Carpenter C.C.J., Fischl M.A., Hammer S.M., Hirsch M.S., Jacobsen D.M., Katzenstein D.A., Montaner J.S.G., Richman D.D., Saag M.S., Schooley R.T., Thompson M.A., Vella S., Yeni P.G., Volberding P.A. Antiretroviral therapy for HIV infection in 1997. JAMA. 277:1997;1962-1969.
3. Cornford E.M., Oldendorf W.H. Independent blood-brain barrier transport systems for nucleic acid precursors. Biochim. Biophys. Acta. 394:1975;211-219.
4. Dykstra K.H., Arya A., Arriola D.M., Bungay P.M., Morrison P.F., Dedrick R.L. Microdialysis study of zidovudine (AZT) transport in rat brain. J. Pharamcol. Exp. Ther. 267:1993;1227-1236.
5. Ho D.D., Rota T.R., Schooley R.T., Kaplan J.C., Allan J.D., Groopman J.E., Resnick L., Felsenstein D., Andrews C.A., Hirsch M.S. Isolation of HTLV-III from cerebrospinal fluid and neural tissues of patients with neurological syndromes related to the acquired immunodeficiency syndrome. New Engl. J. Med. 313:1985;1493-1497.
6. Masereeuw R., Jaehde U., Langemeijer M.W.E., de Boer A.D., Breimer D.D. In vitro and in vivo transport of zidovudine (AZT) across the blood-brain barrier and the effect of transport inhibitors. Pharm. Res. 11:1994;324-330.
7. Merrill J.E., Chen I.S.Y. HIV-1, macrophages, glial cells and cytokines in AIDS nervous system disease. FASEB J. 5:1991;2391-2397.
8. Pang S.Y., Koyangi S., Miles S., Vinters H., Chen I.S.Y. The structure of HIV DNA in brain and blood of AIDS patients. Nature. 343:1990;85-90.
9. W.M. Pardridge, Peptide Drug Delivery to the Brain, Raven Press, New York, 1991, pp. 67-69.
10. Pardridge W.M., Mietus L.J. Transport of steroid hormones through the rat blood-brain barrier. Primary role of albumin-bound hormone. J. Clin. Invest. 64:1979;145-154.
11. Pardridge W.M., Yoshikawa T., Kang Y.-S., Miller L.P. Blood-brain barrier transport and brain metabolism of adenosine and adenosine analogs. J. Pharmacol. Exp. Ther. 268:1994;14-18.
12. Soudeyns H., Yao X.-J., Gao Q., Belleau B., Kraus J.-L., Nguyen-Ba N., Spira B., Wainberg M.A. Anti-human immunodeficiency virus type 1 activity and in vitro toxicity of 2′-deoxy-3′-thiacytidine (BCH-189), a novel heterocyclic nucleoside analog. Antimicrob. Agents Chemother. 35:1991;1386-1390.
13. Spector R., Berlinger W.G. Localization and mechanism of thymidine transport in the central nervous system. J. Neurochem. 39:1982;837-841.
14. Takasato Y., Rapoport S.I., Smith Q.R. An in situ brain perfusion technique to study cerebrovascular transport in the rat. Am. J. Physiol. 247:1984;H484-H493.
15. Takasawa K., Terasaki T., Suzuki H., Sugiyama Y. In vivo evidence for carrier-mediated efflux transport of 3′-azido-3′-deoxythymidine and 2′,3′-dideoxyinosine across the blood-brain barrier via a probenecid-sensitive transport system. J. Pharmacol. Exp. Ther. 281:1997;369-375.
16. Terasaki T., Pardridge W.M. Restricted transport of 3′-azido-3′-deoxythmidine and dideoxynucleosides through the blood-brain barrier. J. Infect. Dis. 158:1988;630-632.
17. Thomas S.A., Segal M.B. Identification of a saturable uptake system for deoxyribonucleosides at the blood-brain and blood-cerebrospinal fluid barriers. Brain Res. 741:1996;230-239.
18. Thomas S.A., Segal M.B. The passage of azidodeoxythymidine into and within the central nervous system: Does it follow the parent compound, thymidine. J. Pharmacol. Exp. Ther. 281:1997;1211-1218.
19. Triguero D., Buciak J.B., Pardridge W.M. Capillary depletion method for quantifying blood-brain barrier transcytosis of circulating peptides and plasma proteins. J. Neurochem. 54:1990;1882-1888.
20. Wiley C.A., Schrier R.D., Nelson J.A., Lampert P.W., Oldstone M.B.A. Cellular location of human immunodeficiency virus infection within the brain of acquired immune deficiency syndrome patients. Proc. Natl. Acad. Sci. U.S.A. 83:1986;7089-7093.