Document Detail

Efflux mechanism of taurocholate across the rat intestinal basolateral membrane.
MedLine Citation:
PMID:  16749859     Owner:  NLM     Status:  MEDLINE    
We investigated the contribution of multidrug resistance associated protein 3 (Mrp3/ABCC3) to the transport of bile acids across the rat intestinal basolateral membrane using the everted sacs. The permeability-surface area (PS) products of taurocholate in the everted sacs of rat jejunum, ileum, and colon were determined in the absence or presence of inhibitors for Mrp3. The results were analyzed to determine the PS product for the uptake across the apical membrane (PS1) and that for the efflux across the basolateral membrane (PS3). The mucosal-to-serosal transport of taurocholate in the ileum was the highest. The concentration-dependent inhibitory effects by all inhibitors in the ileum were observed on both PS1 and PS3 for taurocholate. However, even in the presence of 1 mM of each inhibitor, the decrease of PS3 was low. Additionally, PS3 in the colon, where Mrp3 is expressed at a high level, was not inhibited by MK571 and taurolithocholate-3-sulfate. Unlike PS1, PS3 did not exhibit saturation at the concentration examined. These results suggest that Mrp3 makes only a minor contribution to the efflux of bile acids across the basolateral membrane. Ostalpha-Ostbeta heteromeric transporter is certainly one of the good candidates for such a transporter.
Shingo Sakamoto; Hiroshi Suzuki; Hiroyuki Kusuhara; Yuichi Sugiyama
Related Documents :
11918969 - Effects of different oxidizing agents on neutral amino acid transport systems in isolat...
16657409 - Effect of ethylene on the uptake, distribution, and metabolism of indoleacetic acid-1-c...
6829029 - Effects of diethyl maleate on protein synthesis in isolated hepatocytes.
17235609 - The amino acid l-lysine blocks the disruptive effect of phencyclidine on prepulse inhib...
10948179 - Amino acid transport into cultured mccoy cells infected with chlamydia trachomatis.
7702599 - Expression of a novel insulin-activated amino acid transporter gene during differentiat...
1252919 - Effects of glutamic acid relatives on the electrical activity of an identified mollusca...
24932839 - Photochemical behavior of sethoxydim in presence of vegetable oils.
7962699 - Gamma-aminobutyric acid in the nervous system of a planarian.
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Molecular pharmaceutics     Volume:  3     ISSN:  1543-8384     ISO Abbreviation:  Mol. Pharm.     Publication Date:    2006 May-Jun
Date Detail:
Created Date:  2006-06-05     Completed Date:  2006-08-08     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101197791     Medline TA:  Mol Pharm     Country:  United States    
Other Details:
Languages:  eng     Pagination:  275-81     Citation Subset:  IM    
Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Basement Membrane / metabolism*
Biological Transport* / drug effects
Colon / metabolism
Digoxin / metabolism
Ileum / metabolism
Intestines / metabolism*
Jejunum / metabolism
Multidrug Resistance-Associated Proteins / antagonists & inhibitors,  metabolism*
Quinidine / pharmacology
Rats, Sprague-Dawley
Taurocholic Acid / metabolism*,  pharmacokinetics
Reg. No./Substance:
0/Multidrug Resistance-Associated Proteins; 0/multidrug resistance-associated protein 3; 20830-75-5/Digoxin; 56-54-2/Quinidine; 81-24-3/Taurocholic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Hepatobiliary disposition in primary cultures of dog and monkey hepatocytes.
Next Document:  Influence of charge and steric bulk in the C-24 region on the interaction of bile acids with human a...