Evaluation of drug penetration into the brain: A double study by in vivo imaging with positron emission tomography and using an in vitro model of the human blood-brain barrier

Journal of Pharmacology and Experimental Therapeutics

Volumn 316, Issue 1, 2006, Pages 79-86

  Josserand, Véronique ^a,b   Pélerin, Hélène ^a,d   De Bruin, Béatrice ^a,c   Jego, Benoît ^a,b   Kuhnast, Bertrand ^a,c   Hinnen, Françoise ^a,c   Ducongé, Frédéric ^a,b   Boisgard, Raphaël ^a,b   Beuvon, Frédéric ^a,e   Chassoux, Francine ^a,e   Daumas Duport, Catherine ^a,e   Ezan, Eric ^a,d   Dollé, Frédéric ^a,c   Mabondzo, Aloïse ^a,d   Tavitian, Bertrand ^a,b  

^a DIF   (France)

^b INSERM   (France)

^c Radiochemistry Group   (France)

^d Institut National de la Recherche Agronomique   (France)

^e CENTRE HOSPITALIER SAINTE ANNE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

3 (2 AZETIDINYLMETHOXY)PYRIDINE; AMIDE; FLUORINE 18; RADIOPHARMACEUTICAL AGENT; THIOUREA; UREA;

ARTICLE; BLOOD BRAIN BARRIER; CALCULATION; CELL CULTURE; DIFFUSION; DRUG PENETRATION; DRUG SCREENING; DRUG STRUCTURE; DRUG TARGETING; EFFUSION; ENDOTHELIUM CELL; EVALUATION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MEASUREMENT; PERMEABILITY; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; SUBSTITUTION REACTION;

ALGORITHMS; ANIMALS; ASTROCYTES; AZETIDINES; BIOLOGICAL TRANSPORT, ACTIVE; BLOOD-BRAIN BARRIER; BRAIN; BUFFERS; CHEMISTRY, PHYSICAL; COCULTURE TECHNIQUES; HUMANS; MICROSCOPY, FLUORESCENCE; MODELS, BIOLOGICAL; MOLECULAR WEIGHT; PHARMACEUTICAL PREPARATIONS; POSITRON-EMISSION TOMOGRAPHY; PYRIDINES; RADIOPHARMACEUTICALS; RATS; RECEPTORS, NICOTINIC;

EID: 29244490903     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.105.089102     Document Type: Article

References (42)

1. Audus KL and Borchardt RT (1986) Characteristics of the large neutral amino acid transport system of bovine brain microvessel endothelial cell monolayers. J Neurochem 47:484-488.
2. Begley DJ, Lechardeur D, Chen ZD, Rollinson C, Bardoul M, Roux F, Scherman D, and Abbott NJ (1996) Functional expression of P-glycoprotein in an immortalised cell line of rat brain endothelial cells, RBE4. J Neurochem 67:988-995.
3. Bendayan R, Lee G, and Bendayan M (2002) Functional expression and localization of P-glycoprotein at the blood brain barrier. Microsc Res Tech 57:365-380.
4. Bottlaender M, Valette H, Roumenov D, Dolle F, Coulon C, Ottaviani M, Hinnen F, and Ricard M (2003) Biodistribution and radiation dosimetry of 18F-fluoro-A-85380 in healthy volunteers. J Nucl Med 44:596-601.
5. Crone C (1963) The permeability of capillaries in various organs as determined by use of the indicator diffusion method. Acta Physiol Scand 58:292-305.
6. Davies B and Morris T (1993) Physiological parameters in laboratory animals and humans. Pharm Res (NY) 10:1093-1095.
7. DeBault LE and Cancilia PA (1980) Gamma-glutamyl transpeptidase in isolated brain endothelial cells: induction by glial cells in vitro. Science (Wash DC) 207:653-655.
8. Dehouck MP, Jolliet-Riant P, Bree F, Fruchart JC, Cecchelli R, and Tillement JP (1992) Drug transfer across the blood-brain barrier: correlation between in vitro and in vivo models. J Neurochem 58:1790-1797.
9. Deli MA and Joo F (1996) Cultured vascular endothelial cells of the brain. Keio J Med 45:183-198.
10. Dishino DD, Welch MJ, Kilbourn MR, and Raichle ME (1983) Relationship between lipophilicity and brain extraction of C-11-labeled radiopharmaceuticals. J Nucl Med 24:1030-1038.
11. Dollé F, Dolci L, Valette H, Hinnen F, Vaufrey F, Guenther I, Fuseau C, Coulon C, Bottlaender M, and Crouzel C (1999) Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2- azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors. J Med Chem 42:2251-2259.
12. 18F]fluoro-3-[2(S)-2- azetidinylmethoxy]pyridine, a highly potent radioligand for in vivo imaging central nicotinic acetylcholine receptors. J Labelled Compd Radiopharm 41:451-463.
13. el-Bacha RS and Minn A (1999) Drug metabolizing enzymes in cerebrovascular endothelial cells afford a metabolic protection to the brain. Cell Mol Biol 45:15-23.
14. Elmquist WF and Sawchuk RJ (1997) Application of microdialysis in pharmacokinetic studies. Pharm Res (NY) 14:267-288.
15. Franke H, Galla HJ, and Beuckmann CT (1999) An improved low-permeability in vitro-model of the blood-brain barrier: transport studies on retinoids, sucrose, haloperidol, caffeine and mannitol. Brain Res 818:65-71.
16. Friebe M, Suda K, Spies H, Syhre R, Berger R, Johannsen B, Chiotellis E, Kramer SD, and Wunderli-Allenspach H (2000) Permeation studies in vitro and in vivo of potential radiopharmaceuticals with affinity to neuro receptors. Pharm Res (NY) 17:754-760.
17. Gaillard PJ, Voorwinden LH, Nielsen JL, Ivanov A, Atsumi R, Engman H, Ringbom C, de Boer AG, and Breimer DD (2001) Establishment and functional characterization of an in vitro model of the blood-brain barrier, comprising a co-culture of brain capillary endothelial cells and astrocytes. Eur J Pharm Sci 12:215-222.
18. Gupta N, Price PM, and Aboagye EO (2002) PET for in vivo pharmacokinetic and pharmacodynamic measurements. Eur J Cancer 38:2094-2107.
19. Hendrikse NH, Bart J, de Vries EG, Groen HJ, van der Graaf WT, and Vaalburg W (2001) P-glycoprotein at the blood-brain barrier and analysis of drug transport with positron-emission tomography. J Clin Pharmacol (Suppl):48S-54S.
20. Huai-Yun H, Secrest DT, Mark KS, Carney D, Brandquist C, Elmquist WF, and Miller DW (1998) Expression of multidrug resistance-associated protein (MRP) in brain microvessel endothelial cells. Biochem Biophys Res Commun 243:816-820.
21. Hughes CC and Lantos PL (1989) Uptake of leucine and alanine by cultured cerebral capillary endothelial cells. Brain Res 480:126-132.
22. Jeliazkova-Mecheva VV and Bobilya DJ (2003) A porcine astrocyte/endothelial cell co-culture model of the blood-brain barrier. Brain Res Brain Res Protoc 12:91-98.
23. Kakee A, Terasaki T, and Sugiyama Y (1996) Brain efflux index as a novel method of analyzing efflux transport at the blood-brain barrier. J Pharmacol Exp Ther 277:1550-1559.
24. Kimes AS, Horti AG, London ED, Chefer SI, Contoreggi C, Ernst M, Friello P, Koren AO, Kurian V, Matochik JA, et al. (2003) 2-[18F]F-A-85380: PET imaging of brain nicotinic acetylcholine receptors and whole body distribution in humans. FASEB J 17:1331-1333.
25. 11C]aminocyclohexanecarboxylate for the measurement of amino acid uptake and distribution volume in human brain. J Cereb Blood Flow Metab 10:727-739.
26. Laruelle M, Slifstein M, and Huang Y (2003) Relationships between radiotracer properties and image quality in molecular imaging of the brain with positron emission tomography. Mol Imaging Biol 5:363-375.
27. Lundquist S, Renftel M, Brillault J, Fenart L, Cecchelli R, and Dehouck MP (2002) Prediction of drug transport through the blood-brain barrier in vivo: a comparison between two in vitro cell models. Pharm Res (NY) 19:976-981.
28. Mégard I, Garrigues A, Orlowski S, Jorajuria S, Clayette P, Ezan E, and Mabondzo A (2002) A co-culture-based model of human blood-brain barrier: application to active transport of indinavir and in vivo-in vitro correlation. Brain Res 927:153-167.
29. Oldendorf WH (1970) Measurement of brain uptake of radiolabeled substances using a tritiated water internal standard. Brain Res 24:372-376.
30. Pardridge WM, Triguero D, Yang J, and Cancilla PA (1990) Comparison of in vitro and in vivo models of drug transcytosis through the blood-brain barrier. J Pharmacol Exp Ther 253:884-891.
31. Parkinson FE, Friesen J, Krizanac-Bengez L, and Janigro D (2003) Use of a three-dimensional in vitro model of the rat blood-brain barrier to assay nucleoside efflux from brain. Brain Res 980:233-241.
32. Pirro JP, Di Rocco RJ, Narra RK, and Nunn AD (1994) Relationship between in vitro transendothelial permeability and in vivo single-pass brain extraction. J Nucl Med 35:1514-1519.
33. Rubin LL, Hall DE, Porter S, Barbu K, Cannon C, Horner HC, Janatpour M, Liaw CW, Manning K, Morales J, et al (1991) A cell culture model of the blood-brain barrier. J Cell Biol 115:1725-1735.
34. Schellens JH, Malingre MM, Kruijtzer CM, Bardelmeijer HA, van Tellingen O, Schinkel AH, and Beijnen JH (2000) Modulation of oral bioavailability of anticancer drugs: from mouse to man. Eur J Pharm Sci 12:103-110.
35. Schinkel AH, Smit JJ, van Tellingen O, Beijnen JH, Wagenaar E, van Deemter L, Mol CA, van der Valk MA, Robanus-Maandag EC, te Riele HP, et al (1994) Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell 77:491-502.
36. Takasato Y, Rapoport SI, and Smith QR (1984) An in situ brain perfusion technique to study cerebrovascular transport in the rat. Am J Physiol 247:484-493.
37. Tanaka H and Mizojiri K (1999) Drug-protein binding and blood-brain barrier permeability. J Pharmacol Exp Ther 288:912-918.
38. Valette H, Bottlaender M, Dolle F, Guenther I, Fuseau C, Coulon C, Ottaviani M, and Crouzel C (1999) Imaging central nicotinic acetylcholine receptors in baboons with [18F]fluoro-A-85380. J Nucl Med 40:1374-1380.
39. Van Bree JB, de Boer AG, Danhof M, Ginsel LA, and Breimer DD (1988) Characterization of an "in vitro" blood-brain barrier: effects of molecular size and lipophilicity on cerebrovascular endothelial transport rates of drugs. J Pharmacol Exp Ther 247:1233-1239.
40. Weber SJ, Abbruscato TJ, Brownson EA, Lipkowski AW, Polt R, Misicka A, Haaseth RC, Bartosz H, Hruby VJ, and Davis TP (1993) Assessment of an in vitro bloodbrain barrier model using several [Met5]enkephalin opioid analogs. J Pharmacol Exp Ther 266:1649-1655.
41. Wiesel FA, Blomqvist G, Halldin C, Sjogren I, Bjerkenstedt L, Venizelos N, and Hagenfeldt L (1991) The transport of tyrosine into the human brain as determined with L-[1-11C]tyrosine and PET. J Nucl Med 32:2043-2049.
42. Wong DF and Pomper MG (2003) Predicting the success of a radiopharmaceutical for in vivo imaging of central nervous system neuroreceptor systems. Mol Imaging Biol 5:350-362.