The impact of efflux transporters in the brain on the development of drugs for CNS disorders

Clinical Pharmacokinetics

Volumn 41, Issue 2, 2002, Pages 81-92

  Taylor, Eve M ^a  

^a NeoTherapeutics Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,4 DIHYDROPYRIDINE DERIVATIVE; 5 [3 (4 DIPHENYLACETYL 1 PIPERAZINYL) 2 HYDROXYPROPOXY]QUINOLINE; 6 HYDROXY 2 (4 HYDROXYPHENYL) 3 [4 [2 (1 PYRROLIDINYL)ETHOXY]BENZOYL]BENZO[B]THIOPHENE; AMANTADINE; BIRICODAR; CARBAMIC ACID DERIVATIVE; CARBOXYLIC ACID TRANSPORTER; CARRIER PROTEIN; DACTINOMYCIN; DOXORUBICIN; ETOPOSIDE; GAMMA GLUTAMYL S BENZYLCYSTEINYLPHENYLGLYCINE DIETHYL ESTER; GLYCOPROTEIN P; KR 30035; LANIQUIDAR; LY 329146; MIDOSTAURIN; MULTIDRUG RESISTANCE PROTEIN; OC 144 093; ORGANIC ION TRANSPORTER; PROBENECID; PROTEIN INHIBITOR; PYRROLIDINE DERIVATIVE; SNF 4435 C; TARIQUIDAR; TAUROCHOLIC ACID; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALSPODAR; VX 853; ZOSUQUIDAR;

BLOOD BRAIN BARRIER; BRAIN CANCER; CENTRAL NERVOUS SYSTEM DISEASE; DEMENTIA; DRUG BRAIN LEVEL; DRUG EFFICACY; DRUG PENETRATION; DRUG STABILITY; DRUG TRANSPORT; EPILEPSY; HUMAN; ION TRANSPORT; MENINGITIS; MODULATION; PAIN; PRIORITY JOURNAL; REVIEW; TREATMENT PLANNING;

EID: 0036206904     PISSN: 03125963     EISSN: None     Source Type: Journal    
DOI: 10.2165/00003088-200241020-00001     Document Type: Review

References (133)

1. Active transport of diodrast and phenolsulfonphthalein from cerebrospinal fluid to blood
2. Rapid efflux of some quaternary ammonium compounds from cerebrospinal fluid
3. Spinal fluid iodide transport in dog
4. Influence of various drugs on the transport of 13II and PAH across the cerebrospinal fluid-blood barrier
5. Factors affecting distribution of iodide in brain and cerebrospinal fluid
6. Potassium exchange between cerebrospinal fluid, plasma and brain
7. Exchange of cerebrospinal fluid potassium with blood and brain. Study in normal and Ouabain perfused cats
8. Blood-brain and CSF barriers to penicillin and related organic acids
9. Physiology and pathology of the blood-brain barrier: Implication for microbial pathogenesis, drug delivery and neurodegenerative disorders
10. Contribution of probenecid-sensitive anion transport processes at the brain capillary endothelium and choroid plexus to the efficient efflux of valproic acid from the central nervous system
11. Effect of paraaminohippurate on the efflux of valproic acid from the central nervous system of the rabbit
12. Blood-brain barrier transport of valproic acid
13. Quantitative evaluation of brain distribution and blood-brain barrier efflux transport of probenecid in rats by microdialysis: Possible involvement of the monocarboxylic acid transport system
14. Brain distribution of mercaptopurine is regulated by the efflux transport system in the blood-brain barrier
15. Enhanced cerebral uptake of receptor ligands by modulation of P-glycoprotein function in the blood-brain barrier
16. Probenecid enhances central nervous system uptake of 2′,3′-dideoxyinosine by inhibiting cerebrospinal fluid efflux
17. Effect of probenecid on the renal and nonrenal clearances of zidovudine and its distribution into cerebrospinal fluid in the rabbit
18. Kinetic evidence for active efflux transport across the blood-brain barrier of quinolone antibiotics
19. The effects of salicylate and probenecid of the cerebrospinal fluid transport of penicillin, aminosalicylic acid and iodide
20. Transport of imipenem, a novel carbapenem antibiotic, in the rat central nervous system
21. Zidovudine transport in the rabbit brain during intravenous and intracerebroventricular infusion
22. Biochemistry of multidrug resistance mediated by the multidrug transporter
23. P-glycoprotein and multidrug resistance
24. Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites
25. Expression of the multidrug resistance gene product (P-glycoprotein) in human normal and tumor tissues
26. Immunohistochemical localization in normal tissues of different epitopes in the multidrug transport protein P170: Evidence for localization in brain capillaries and crossreactivity of one antibody with a muscle protein
27. MDR1 gene expression in brain of patients with medically intractable epilepsy
28. Specialized localization of P-glycoprotein recognized by MRK16 monoclonal antibody in endothelial cells of the brain and spinal cord
29. The multidrug-resistance P-glycoprotein (P-gp, mdr1) is an early marker of blood-brain barrier development in the microvessels of the developing human brain
30. Brain microvascular and astrocyte localization of P-glycoprotein
31. High levels of p-glycoprotein detected in isolated brain capillaries
32. Isoform 1 (mdr3) is the major form of p-glycoprotein expressed in mouse brain capillaries
33. Lung resistance protein (LRP) expression in human normal tissues in comparison with that of MDR1 and MRP
34. Multidrug resistance-related transport proteins in isolated human brain microvessels and in cells cultured from these isolates
35. Choroid plexus epithelial expression of mdr1 P-glycoprotein and multidrug resistance-associated protein contributes to the blood-cerebrospinal-fluid drug-permeability barrier
36. MDR1 P-glycoprotein is expressed by endothelial cells of newly formed capillaries in human gliomas but is not expressed in the neovasculature of other primary tumors
37. P-gp of blood-brain barrier: Cross-reactivity of Mab C219 with a 190kDa protein in bovine and rat isolated brain capillaries
38. Comparisons of P-glycoprotein expression in isolated rat brain microvessels and in primary cultures of endothelial cells derived from microvasculature of rat brain, epidymal fat pad and from aorta
39. Functional expression of P-glycoprotein in an immortalized cell line of rat brain endothelial cells, RBE4
40. P-glycoprotein is strongly expressed in the luminal membranes of the endothelium of blood vessels in the brain
41. Functional expression of P-glycoprotein and multidrug resistance-associated protein (Mrp1) in primary cultures of rat astrocytes
42. Developmental expression of P-glycoprotein (multidrug resistance gene product) in rat brain
43. Cellular localization of P-glycoprotein in brain versus gonadal capillaries
44. Mrp1 multidrug resistance-associated protein and p-glycoprotein expression in rat brain microvessel endothelial cells
45. The three mouse multidrug resistance (mdr) genes are expressed in a tissue-specific manner in normal mouse tissues
46. Expression and functional activity of p-glycoprotein in cultured cerebral capillary endothelial cells
47. Functional involvement of p-glycoprotein in blood-brain barrier
48. Mouse multidrug resistance 1a/3 gene is the earliest known endothelial cell differentiation marker during blood-brain barrier development
49. P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cells
50. Expression of various multidrug resistance-associated protein (MRP) homologues in brain microvessel endothelial cells
51. Functional expression of the p-glycoprotein mdr in primary cultures of bovine cerebral endothelial cells
52. Sex-dependent and independent expression of the p-glycoprotein isoforms in Chinese hamster
53. Effect of P-glycoprotein modulation with cyclosporin on cerebrospinal fluid penetration of doxorubicin in non-human primates
54. Brain microvascular P-glycoprotein and a revised model of multidrug resistance in brain
55. P-glycoprotein, a gatekeeper in the blood-brain barrier
56. Disruption of the mouse mdr1 a p-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs
57. Absence of the mdr1 a p-glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A
58. P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs
59. Substantial excretion of digoxin via the intestinal mucosa and prevention of long-term digoxin accumulation in the brain by the mdr1 a p-glycoprotein
60. Efflux transport of a new quinolone antibacterial agent, HSR-903, across the blood-brain barrier
61. The drug transporter p-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors
62. P-glycoprotein confers methotrexate resistance in 3T6 cells with deficient carrier-mediated methotrexate uptake
63. The P-glycoprotein efflux pump: How does it transport drugs?
64. The multidrug resistance protein family
65. Analysis of the expression of MRP, the gene for a new putative transmembrane drug transporter, in human multidrug resistant lung cancer cell lines
66. Structure and expression of the messenger RNA encoding the murine multidrug resistance protein, an ATP-binding cassette transporter
67. Xenobiotic transport across isolated brain microvessels studied by confocal microscopy
68. Tissue distribution of the multidrug resistance protein
69. Modulation of multidrug resistance protein expression in porcine brain capillary endothelial cells in vitro
70. Multidrug resistance protein 1 protects the choroid plexus epithelium and contributes to the blood-cerebrospinal fluid barrier
71. Expression of multidrug resistance-associated protein (MRP) in brain microvessel endothelial cells
72. Characterization of efflux transport of organic anions in a mouse brain capillary endothelial cell line
73. Transepithelial transport of organic anions across the choroid plexus: Possible involvement of organic anion transporter and multidrug resistance-associated protein
74. Increased sensitivity to anticancer drugs and decreased inflammatory response in mice lacking the multidrug resistance-associated protein
75. Disruption of the murine MRP (multidrug resistance protein) gene leads to increased sensitivity to etoposide (VP-16) and increased levels of glutathione
76. Multidrug resistance protein 1 protects the oropharyngeal mucosal layer and the testicular tubules against drug-induced damage
77. Analysis of expression of cMOAT (MRP2), MRP3, MRP4, and MRP5, homologues of the multidrug resistance-associated protein gene (MRP1), in human cancer cell lines
78. Expression of human MRP6, a homologue of the multidrug resistance protein gene MRP1, in tissues and cancer cells
79. PABC11 (also known as MOAT-C and MRP5), a member of the ABC family of proteins, has anion transporter activity but does not confer multidrug resistance when overexpressed in human embryonic kidney 293 cells
80. The proton-linked monocarboxylate transporter (MCT) family: Structure, function and regulation
81. Transport of lactate and other monocarboxylates across mammalian membranes
82. What is the blood-brain barrier? A molecular perspective
83. Aluminium citrate is transported from brain into blood via the monocarboxylic acid transporter located at the blood-brain barrier
84. Aluminum transport out of brain extracellular fluid is proton dependent and inhibited by mersalyl acid, suggesting mediation by the monocarboxylate transporter (MCT1)
85. AIT-082 is transported out of brain by a saturable mechanism: Possible involvement of multidrug resistance and monocarboxylic acid transporters
86. Cloning of the monocarboxylate transporter isoform MCT2 from rat testis provides evidence that expression in tissues is species-specific and may involve post-transcriptional regulation
87. Monocarboxylate transporter expression in mouse brain
88. Cloning and sequencing of four new mammalian monocarboxylate transporter (MCT) homologues confirms the existence of a transporter family with an ancient past
89. Expression of monocarboxylate transporter MCT1 by brain endothelium and glia in adult and suckling rats
90. DNA cloning and functional characterization of rat intestinal monocarboxylate transporter
91. Monocarboxylate transporter (MCT1) abundance in brains of suckling and adult rats: A quantitative electron microscopic immunogold study
92. Expression of the monocarboxylate transporter MCT2 by rat brain glia
93. A novel transmembrane transporter encoded by the XPCT gene in Xq13.2
94. Organic cation transporters in intestine, kidney, liver and brain
95. Cellular and molecular aspects of drug transport in the kidney
96. The multispecific organic anion transporter (OAT) family
97. Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain
98. Molecular cloning and functional expression of a multispecific organic anion transporter from human kidney
99. Cloning and functional expression of a human liver organic cation transporter
100. Human neurons express the polyspecific cation transporter hOCT2, which translocates monoamine neurotransmitters, amantadine, and memantine
101. Primary structure and functional expression of the apical organic cation transporter from kidney epithelial LLC-PK1 cells
102. Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta
103. Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain
104. Dichotomous development of the organic anion transport protein in liver and choroid plexus
105. The choroid plexus epithelium is the site of the organic anion transport protein in the brain
106. Isolation of a multispecific organic anion and cardiac glycoside transporter from rat brain
107. Molecular characterization and tissue distribution of a new organic anion transporter subtype (oatp3) that transports thyroid hormones and taurocholate and comparison with oatp2
108. Blood-brain barrier is involved in the efflux transport of a neuroactive steroid, dehydroepiandrosterone sulfate, via organic anion transporting polypeptide 2
109. Expression, transport properties, and chromosomal location of organic anion transporter subtype 3
110. Cloning and characterization of a novel human pH-dependent organic cation transporter, OCTN1
111. Molecular and functional identification of sodium ion-dependent, high affinity human carnitine transporter OCTN2
112. Molecular and functional characterization of organic cation/carnitine transporter family in mice
113. Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter
114. Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta
115. Altered expression and function of P-glycoprotein (170 kDa) encoded by the MDR1 gene, in T cell subsets from aging humans
116. Evidence of active transport of benzyl-14C-penicillin from cerebrospinal fluid to blood
117. 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
118. Distributional transport kinetics of zidovudine between plasma and brain extracellular fluid/cerebrospinal fluid in the rabbit: Investigation of the inhibitory effect of probenecid utilizing microdialysis
119. Zidovudine transport within the rabbit brain during intracerebroventricular administration and the effect of probenecid
120. Microdialysis study of zidovudine (AZT) transport in rat brain
121. Transport of GABA at the blood-CSF interface
122. Leukotriene C4 transport and metabolism in the central nervous system
123. Modulation effects of cyclosporine on etoposide pharmacokinetics and CNS distribution in the rat utilizing microdialysis
124. Role of p-glycoprotein in the blood-brain transport of colchicine and vinblastine
125. Effect of the p-glycoprotein inhibitor, SDZ PSC 833, on the blood and brain pharmacokinetics of colchicine
126. Dose-dependent brain penetration of SDZ PSC 833, a novel multidrug resistance-reversing cyclosporin, in rats
127. Full blockade of intestinal P-glycoprotein and extensive inhibition of blood-brain barrier P-glycoprotein by oral treatment of mice with PSC833
128. P-glycoprotein mediates the efflux of quinidine across the blood-brain barrier
129. Decreased biotolerability for ivermectin and cyclosporin A in mice exposed to potent P-glycoprotein inhibitors
130. Multidrug resistance and its reversal
131. Inhibitors of multidrug resistance
132. New advances in the transport of doxorubicin through the blood-brain barrier by a peptide vector-mediated strategy