Mechanisms of transport and structure-permeability relationship of sulfasalazine and its analogs in Caco-2 cell monolayers

Pharmaceutical Research

Volumn 17, Issue 10, 2000, Pages 1168-1174

  Liang, E ^a   Proudfoot, J ^b   Yazdanian, M ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b Department of Medicinal Chemistry ^*

Author keywords

Caco 2 cells; Multiple cellular efflux mechanisms; Structure permeability relationship; Sulfasalazine

Indexed keywords

CARBOXYLIC ACID; MESALAZINE; MULTIDRUG RESISTANCE PROTEIN; SALAZOSULFAPYRIDINE; SULFANILAMIDE DERIVATIVE;

ARTICLE; CELL MEMBRANE TRANSPORT; CELL STRAIN CACO 2; CONCENTRATION RESPONSE; DIFFUSION COEFFICIENT; DRUG ABSORPTION; DRUG PENETRATION; DRUG STRUCTURE; DRUG TRANSPORT; HUMAN; HUMAN CELL; PHOSPHORYLATION; PRIORITY JOURNAL; REGULATORY MECHANISM;

EID: 0033636283     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1026450326712     Document Type: Article

References (30)

1. Novel formulation strategies for improving oral bioavailability of drugs with poor membrane permeation or presystemic metabolism
2. Transcellular transport of benzoic acid across Caco-2 cells by a pH-dependent and carrier-mediated transport mechanism
3. An experiment to determine the active therapeutic moiety of sulphasalazine
4. Clinical pharmacokinetics of sulfasalazine, its metabolites and other prodrugs of 5-aminosallcylic acid
5. Sulfasalazine and new analogues
6. Effect of sulphapyridine, 5-aminosalicylic acid, and placebo in patients with idiopathic proctitis: A study to determine active therapeutic moiety of sulphasalazine
7. Correlating partitioning and Caco-2 cell permeability of structurally diverse small molecular weight compounds
8. Sulfasalazine
9. Evidence for a polarized efflux system for peptides in the apical region of Caco-2 cells
10. Transport characteristics of peptidomimetics. Effect of the pyrrolinone bioisostere on transport across Caco-2 cell monolayers
11. Characterization of the regional intestinal kinetics of drug efflux in rat and human intestine and in Caco-2 cells
12. Transport of a large neutral amino acid (phenylalanine) in a human intestinal epithelial cell line: Caco-2
13. Effect of carbonylcyanide m-chlorophenylhydrazone on the calcium-stimulated ATPase activity of erythrocyteghosts
14. Radioligand-binding assay employing P-glycopretein-overexpressing cells: Testing drug affinities to the secretory intestinal multidrug transporter
15. Transport characteristics of diphenhydramine in human intestinal epithelial Caco-2 cells: Contribution of pH-dependent transport system
16. Structural characterization of substrates for the anion exchange transporter in Caco-2 cells
17. Structurally distinct MDR modulators show specific patterns of reversal against P-glycoproteins bearing unique mutations at Serine(939/941)
18. P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs
19. Transport properties of the multidrug resistance-associated protein (MRP) in human tumour cells
20. A comparison of rhodamine 123 accumulation and efflux in cells with P-glycoprotein-mediated and MRP-associated multidrug resistance phenotypes
21. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors
22. Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain
23. Anion transport systems in the plasma membrane of vertebrate cells
24. +-cotransport mechanism versus pH-partition hypothesis
25. 3- exchange in the basolateral membrane domain of rat jejunal enterocyte
26. - uptake in membrane vesicles
27. Cloning and functional expression of a mouse liver organic cation tranporter
28. +-dependent carnitine transport by organic cation transporter (OCTN2): Its pharmacological and toxicological relevance