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Titolo:
Functional characterization of organic cation drug transport in the pigmented rabbit conjunctiva
Autore:
Ueda, H; Horibe, Y; Kim, KJ; Lee, VHL;
Indirizzi:
Univ So Calif, Sch Pharm, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 eut Sci, Los Angeles, CA 90089 USA Univ So Calif, Sch Pharm, Dept Med, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 ept Med, Los Angeles, CA 90089 USA Univ So Calif, Sch Pharm, Dept Ophthalmol, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 thalmol, Los Angeles, CA 90089 USA Univ So Calif, Sch Pharm, Dept Physiol & Biophys, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 Biophys, Los Angeles, CA 90089 USA Univ So Calif, Sch Pharm, Dept Biomed Engn, Los Angeles, CA 90089 USA UnivSo Calif Los Angeles CA USA 90089 ed Engn, Los Angeles, CA 90089 USA Univ So Calif, Sch Pharm, Dept Mol Pharmacol & Toxicol, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 Toxicol, Los Angeles, CA 90089 USA Univ So Calif, Sch Pharm, Will Rogers Inst, Pulm Res Ctr, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 Res Ctr, Los Angeles, CA 90089 USA Univ So Calif, Sch Med, Will Rogers Inst Pulm, Res Ctr, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 Res Ctr, Los Angeles, CA 90089 USA Univ So Calif, Sch Med, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 eut Sci, Los Angeles, CA 90089 USA Univ So Calif, Sch Med, Dept Med, Los Angeles, CA 90089 USA Univ So CalifLos Angeles CA USA 90089 ept Med, Los Angeles, CA 90089 USA Univ So Calif, Sch Med, Dept Ophthalmol, Los Angeles, CA 90089 USA Univ SoCalif Los Angeles CA USA 90089 thalmol, Los Angeles, CA 90089 USA Univ So Calif, Sch Med, Dept Physiol & Biophys, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 Biophys, Los Angeles, CA 90089 USA Univ So Calif, Sch Med, Dept Biomed Engn, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 ed Engn, Los Angeles, CA 90089 USA Univ So Calif, Sch Med, Dept Mol Pharmacol & Toxicol, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 Toxicol, Los Angeles, CA 90089 USA Univ So Calif, Sch Engn, Will Rogers Inst, Pulm Res Ctr, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 Res Ctr, Los Angeles, CA 90089 USA Univ So Calif, Sch Engn, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 eut Sci, Los Angeles, CA 90089 USA Univ So Calif, Sch Engn, Dept Med, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 ept Med, Los Angeles, CA 90089 USA Univ So Calif, Sch Engn, Dept Ophthalmol, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 thalmol, Los Angeles, CA 90089 USA Univ So Calif, Sch Engn, Dept Physiol & Biophys, Los Angeles, CA 90089 USAUniv So Calif Los Angeles CA USA 90089 Biophys, Los Angeles, CA 90089 USA Univ So Calif, Sch Engn, Dept Biomed Engn, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 ed Engn, Los Angeles, CA 90089 USA Univ So Calif, Sch Engn, Dept Mol Pharmacol & Toxicol, Los Angeles, CA 90089 USA Univ So Calif Los Angeles CA USA 90089 Toxicol, Los Angeles, CA 90089 USA
Titolo Testata:
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE
fascicolo: 3, volume: 41, anno: 2000,
pagine: 870 - 876
SICI:
0146-0404(200003)41:3<870:FCOOCD>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
RENAL BRUSH-BORDER; CARRIER-MEDIATED TRANSPORT; NA+-GLUCOSE COTRANSPORT; MEMBRANE-VESICLES; GUANIDINE TRANSPORT; BILIARY-EXCRETION; EPITHELIAL-CELLS; HEPATIC-UPTAKE; L-ARGININE; MECHANISMS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
47
Recensione:
Indirizzi per estratti:
Indirizzo: Lee, VHL Univ So Calif, Sch Pharm, Dept Pharmaceut Sci, 1985 Zonal Ave, Los Angeles, CA 90089 USA Univ So Calif 1985 Zonal Ave Los Angeles CA USA 90089 A 90089 USA
Citazione:
H. Ueda et al., "Functional characterization of organic cation drug transport in the pigmented rabbit conjunctiva", INV OPHTH V, 41(3), 2000, pp. 870-876

Abstract

PURPOSE. TO characterize carrier-mediated organic cation drug transport inthe rabbit conjunctiva. METHODS. The transport of [C-14]guanidine, the model substrate, in the excised pigmented rabbit conjunctiva was evaluated in the modified Ussing chamber. Tetraethylammonium (TEA) transport also was investigated to determine substrate specificity. RESULTS. The apparent permeability coefficient for guanidine and TEA in the mucosal-to-serosal (ms) direction was 5.4 and 49.6 times greater than that in the serosal-to-mucosal (sm) direction, respectively. Guanidine transport in the ms (but not sm) direction revealed temperature and concentration dependency over 0.02 to 10 mM with an apparent Michaelis-Menten constant of3.1 mM and a maximal flux of 11.4 nmol/(cm(2) . h). Net guanidine transport measured at 0.1 mM across the conjunctiva was decreased by 71% or 82%, respectively, on the addition of 1 mu M valinomycin (a K+ ionophore) in both bathing fluids or in a high K+ buffer in the mucosal fluid. Interestingly, net guanidine transport was reduced, rather than enhanced, by 63% upon acidifying the mucosal bathing fluid. By contrast, net guanidine transport was not affected by the serosal presence of 0.5 mM ouabain (a Na+,K+-ATPase inhibitor), by the mucosal and serosal presence of 0.1 mu M monensin (a Na+ ionophore) or 0.3 mu M carbonyl cyanide p-(trifluoromethoxy)phenyl-hydrazone (FCCP, a H+ ionophore). Guanidine transport in the ms direction was polyspecific, as indicated by the 48% to 82% inhibition by structurally diverse amines. In particular, guanidine ms transport was inhibited by the antiglaucoma drugs dipivefrine (72%), brimonidine (70%), and carbachol (78%). CONCLUSIONS. A carrier-mediated organic cation transport process appears to exist in the conjunctiva, mediating the absorption of organic amines, including certain amine-type ophthalmic drugs. This process may be driven by an inside-negative apical membrane potential difference.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/10/20 alle ore 04:04:43