Brain penetration of synthetic adenosine A 1 receptor agonists in situ: Role of the rENT1 nucleoside transporter and binding to blood constituents

European Journal of Pharmaceutical Sciences

Volumn 24, Issue 1, 2005, Pages 59-66

  Schaddelee, Marloes P ^a   Read, Kevin D ^b   Cleypool, Cindy G J ^a   Ijzerman, Adriaan P ^a   Danhof, Meindert ^a   De Boer, Albertus G ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

A 1 receptor agonists; Blood brain barrier; Brain perfusion; Protein binding; rENT1 nucleoside transporter

Indexed keywords

2' DEOXY N6 CYCLOPENTYLADENOSINE; 5' DEOXY N6 CYCLOPENTYLADENOSINE; 6 N CYCLOPENTYLADENOSINE; 8 METHYLAMINO N6 CYCLOPENTYLADENOSINE; ADENOSINE A1 RECEPTOR AGONIST; BUFFER; NITROBENZYLTHIOINOSINE; NUCLEOSIDE TRANSPORTER; PHOSPHATE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BLOOD BRAIN BARRIER; BLOOD SAMPLING; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG BINDING; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; EXPERIMENTAL TEST; HEMOCONCENTRATION; IN SITU HYBRIDIZATION; ISOMER; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; STATISTICAL SIGNIFICANCE;

ADENOSINE; ANIMALS; BRAIN; EQUILIBRATIVE NUCLEOSIDE TRANSPORTER 1; MALE; PERMEABILITY; PROTEIN BINDING; RATS; RATS, WISTAR; RECEPTOR, ADENOSINE A1; THIOINOSINE;

EID: 11144235832     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2004.09.010     Document Type: Article

References (30)

1. C.M. Anderson, W. Xiong, J.D. Young, C.E. Cass, and F.E. Parkinson Demonstration of the existence of mRNAs encoding N1/cif and N2/cit sodium/nucleoside cotransporters in rat brain Brain Res. Mol. Brain Res. 42 2 1996 358 361
2. M.W. Bradbury The blood-brain barrier Exp. Physiol. 78 1993 453 472
3. A.M. Butt, H.C. Jones, and N.J. Abbott Electrical resistance across the blood-brain barrier in anaesthetized rats: a development study J. Physiol. 429 1990 47 62
4. E.M. Cornford, and W.H. Oldendorf Independent blood-brain barrier transport systems for nucleic acid precursors Biochim. Biophys. Acta 394 1975 211 219
5. A.G. De Boer, I.C.J. van der Sandt, and P.J. Gaillard The role of drug transporters at the BBB Ann. Rev. Pharmacol. Toxicol. 43 2003 629 656
6. J.D. Geiger, F.E. Parkinson, and E.A. Kowaluk Regulators of endogenous adenosine levels as therapeutic agents K.A. Jacobson M.F. Jarvis Purinergic Approaches in Experimental Therapeutics 1997 Wiley-Liss New York 55 84
7. M. Gibaldi, and D. Perrier Non-compartmental analysis based on statistical moment theory M. Gibaldi D. Perrier Pharmacokinetics second ed. 1982 Marcel Dekker New York, Basel 409 424
8. R.J. Hyde, C.E. Cass, J.D. Young, and S.A. Baldwin The ENT family of eukaryote nucleoside and nucleobase transporters: recent advances in the investigation of structure/function relationships and the identification of novel isoforms Mol. Membr. Biol. 18 2001 53 63
9. S.M. Jarvis Adenosine transporters D.M.F. Cooper C. Londos Adenosine Receptors 1988 Alan R. Liss Inc. New York 113 123
10. L.L. Jennings, C. Hao, M.A. Cabrita, M.F. Vickers, S.A. Baldwin, J.D. Young, and C.E. Cass Distinct regional distribution of human equilibrative nucleoside transporter proteins 1 and 2 (hENT1 and hENT2) in the central nervous system Neuropharmacology 40 2001 722 731
11. R.N. Kalaria, and S.I. Harik Adenosine receptors and the nucleoside transporter in human brain vasculature J. Cereb. Blood Flow Metab. 8 1988 32 39
12. G. Lee, S. Dallas, M. Hong, and R. Bendayan Drug Transporters in the central nervous system: brain barriers and brain parenchyma considerations Pharmacol. Rev. 53 2001 569 596
13. R.H. Levy, and T.A. Moreland Rationale for monitoring free drug levels Clin. Pharmacokinet. 9 1984 1 9
14. J. Malhotra, and Y.K. Gupta Effect of adenosine receptor modulation on pentylenetetrazole-induced seizure in rats Br. J. Pharmacol. 120 1997 282 288
15. B. Pavan, and A.P. IJzerman Processing of adenosine receptor agonists in rat and human whole blood Biochem. Pharm. 56 1998 1625 1632
16. P.G. Plagemann, R.M. Wohlhueter, and C. Woffendin Nucleoside and nucleobase transport in animal cells Biochim. Biophys. Acta 947 1988 405 443
17. M.W. Ritzel, S.Y. Yao, A.M. Ng, J.R. Mackey, C.E. Cass, and J.D. Young Molecular cloning, functional expression and chromosomal localization of a cDNA encoding a human Na+/nucleoside cotransporter (hCNT2) selective for purine nucleosides and uridine Mol. Membr. Biol. 15 4 1998 203 211
18. 1 receptor J. Med. Chem. 39 1996 1463 1471
19. M.P. Schaddelee, H.L. Voorwinden, E.W. van Tilburg, A.J.P. Pateman, A.P. IJzerman, M. Danhof, and A.G. de Boer The functional role of adenosine receptor subtypes in the regulation of blood-brain barrier permeability: possible implications for the design of synthetic adenosine derivatives Eur. J. Pharm. Sci. 19 2003 13 22
20. 1 receptor agonists: structure-in vitro transport relationships Eur. J. Pharm. Sci. 20 2003 347 356
21. K.F. Sjölund, M. Belfrage, R. Karlsten, M. Segerdahl, S. Arner, T. Gordh, and A. Solevi Systemic adenosine infusion reduces the area of tactile allodynia in neuropathic pain following peripheral nerve injury: a multi-centre, placebo-controlled study Eur. J. Pain 5 2001 199 207
22. Q.R. Smith Brain perfusion systems for studies of drug uptake and metabolism in the central nervous system R.T. Borchardt Models for assessing drug absorption and metabolism 1996 Plenum Press New York
23. R.E. Strecker, S. Morairty, M.M. Thakkar, T. Porkka-Heiskanen, R. Basheer, L.J. Dauphin, D.G. Rainnie, C.M. Portas, R.W. Greene, and R.W. McCarley Adenosinergic modulation of basal forebrain and preoptic/anterior hypothalamic neuronal activity in the control of behavioral state Behav. Brain Res. 115 2000 183 204
24. Y. Takasato, S.I. Rapoport, and Q.R. Smith An in situ brain perfusion technique to study cerebrovascular transport in the rat Am. J. Physiol. 247 1984 H484 H493
25. S.A. Thomas, and M.B. Segal Saturation kinetics, specificity and NBMPR sensitivity of thymidine entry into the central nervous system Brain Res. 760 1997 59 67
26. J.A. Thorn, and S.M. Jarvis Adenosine transporters Gen. Pharmacol. 27 1996 613 620
27. E.M. Van der Wenden, H.R. Hartog-Witte, H.C.P.F. Roelen, J.K. Von Frijtag Drabbe Künzel, R.A.A. Mathôt, and A.P. IJzerman Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor J. Med. Chem. 38 1995 4000 4006
28. 6- cyclopentyladenosine in vivo: haemodynamic versus anti-lipolytic responses in rats Br. J. Pharmacol. 124 1998 607 618
29. D.K. Von Lubitz Adenosine in the treatment of stroke: yes, maybe, or absolutely not? Expert Opin. Investig. Drugs 10 2001 619 632
30. S.Y. Yao, A.M. Ng, W.R. Muzyka, M. Griffiths, C.E. Cass, S.A. Baldwin, and J.D. Young Molecular cloning and functional characterization of nitrobenzylthioinosine (NBMPR)-sensitive (es) and NBMPR-insensitive (ei) equilibrative nucleoside transporter proteins (rENT1 and rENT2) from rat tissues J. Biol. Chem. 272 45 1997 28423 28430