Active efflux of the 5-HT1A receptor agonist flesinoxan via P-glycoprotein at the blood-brain barrier

European Journal of Pharmaceutical Sciences

Volumn 14, Issue 1, 2001, Pages 81-86

  van der Sandt, I C J ^a   Smolders, R ^a   Nabulsi, L ^a   Zuideveld, K P ^a   De Boer, A G ^a   Breimer, D D ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Blood brain barrier; Flesinoxan; LLC PK1:MDR1 cell line; Mdr1a( ) mice; P glycoprotein

Indexed keywords

BLOOD; BRAIN; POLARIZATION;

CELL LINES;

DRUG PRODUCTS;

FLESINOXAN; GLYCOPROTEIN P; SEROTONIN 1A AGONIST; VALSPODAR; ZOSUQUIDAR;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; CELL STRAIN; COCULTURE; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG TISSUE LEVEL; DRUG TRANSPORT; KIDNEY EPITHELIUM; MALE; MOUSE; MULTIDRUG RESISTANCE; NONHUMAN; PRIORITY JOURNAL; SWINE;

ANIMALS; BIOLOGICAL TRANSPORT, ACTIVE; BLOOD-BRAIN BARRIER; COCULTURE TECHNIQUES; EPITHELIAL CELLS; GENES, MDR; LLC-PK1 CELLS; MICE; MICE, INBRED STRAINS; P-GLYCOPROTEIN; PIPERAZINES; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN AGONISTS; SWINE; TISSUE DISTRIBUTION;

EID: 0034934071     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0928-0987(01)00150-6     Document Type: Article

References (21)

1. Expression of the multidrug resistance gene product (P-glycoprotein) in human and tumour tissues
2. 1A agonist flesinoxan, in three paradigms for assessing antidepressant potential in the rat
3. Effect of the P-glycoprotein inhibitor, SDZ PSC 833, on the blood and brain pharmacokinetics of colchicine
4. Characterization of binding properties to human P-glycoprotein: development of a [3H]verapamil radioligand-binding assay
5. Astrocytes increase the functional expression of P-glycoprotein in an in vitro model of the blood-brain barrier
6. 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
7. Saturable P-glycoprotein kinetics assayed by fluorescence studies of drug efflux from suspended human KB8-5 cells
8. Characterization of 5-hydroxytryptamine1A properties of flesinoxan: in vivo electrophysiology and hypothermia study
9. Role of blood-brain barrier P-glycoprotein in limiting brain accumulation and sedative side-effects of asimadoline, a peripherally acting analgesic drug
10. Cell surface P-glycoprotein associated with multidrug resistance in mammalian cells
11. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors
12. Effects of a potent and specific P-glycoprotein inhibitor on the blood-brain barrier distribution and antinociceptive effect of morphine in the rat
13. CNS as a sanctuary for HIV1 infection despite treatment with zidovudine, lamivudine and indinavir
14. Early penetration of the blood-brain barrier by HIV
15. Absence of the mdr1a P-glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin and cyclosporin A
16. Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood brain barrier and to increased sensititivity to drugs
17. Multidrug resistance and the role of P-glycoprotein knockout mice
18. P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs
19. Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone
20. Specificity of doxorubicin versus rhodamine-123 in assessing P-glycoprotein functionality in the LLC-PK1, LLC-PK1:MDR1 and Caco-2 cell lines
21. Assessment of active transport of HIV protease inhibitors in various cell lines and the in vitro blood-brain barrier