Effects of NPPB (5-nitro-2-(3-phenylpropylamino)benzoic acid) on chloride transport in intestinal tissues and the T84 cell line.
作者： David J. Keeling , Amanda G. Taylor , Philip L. Smith
DOI: 10.1016/0304-4165(91)90009-6
关键词: Chloride channel 、 Efflux 、 Ileum 、 Metabolism 、 Biophysics 、 Ussing chamber 、 Chemistry 、 Biochemistry 、 Na+/K+-ATPase 、 Endogeny 、 Channel blocker
摘要: Abstract NPPB (5-nitro-2-(3-phenylpropylamino)benzoic acid) has been reported to block Cl− channels in isolated rabbit nephrons with high potency (IC50 = 80 nM). The effects of this compound on Cl−-mediated transport processes intestinal tissues have studied using agonist-stimulated short-circuit current (T84) Ussing chamber experiments and 36Cl− fluxes monolayers a colonic cell line (T84. inhibited PGE1-stimulated Isc distal colon ileum at concentrations the range 20 100 μM. However, same also glucose-stimulated ileum, suggesting that its were not restricted those transport. Consistent this, exposure μM was found reduce endogenous ATP levels by 69%, implying that, these concentrations, could impair active an effect cellular energy metabolism. Clear evidence for direct epithelial chloride studies T84 monolayers. VIP-stimulated uptake into cells IC50 414 (1 mM) efflux from pre-loaded confirming as weak channel blocker system.
sci-hub.se 参考文章(16)
K G Mandel, J A McRoberts, K Dharmsathaphorn, Characterization of a cyclic AMP-activated Cl-transport pathway in the apical membrane of a human colonic epithelial cell line. Journal of Biological Chemistry. ,vol. 261, pp. 704- 712 ,(1986) , 10.1016/S0021-9258(17)36150-1
A. Lewis Farr, Oliver H. Lowry, Rose J. Randall, Nira J. Rosebrough, Protein Measurement with the Folin Phenol Reagent Journal of Biological Chemistry. ,vol. 193, pp. 265- 275 ,(1951)
H. Oberleithner, M. Ritter, F. Lang, W. Guggino, Antracene-9-carboxylic acid inhibits renal chloride reabsorption Pfl�gers Archiv European Journal of Physiology. ,vol. 398, pp. 172- 174 ,(1983) , 10.1007/BF00581068
D W Landry, M Reitman, E J Cragoe, Q Al-Awqati, Epithelial chloride channel. Development of inhibitory ligands. The Journal of General Physiology. ,vol. 90, pp. 779- 798 ,(1987) , 10.1085/JGP.90.6.779
S. Golf, T. Jahnsen, H. Attramadal, T. Frøysaker, V. Hansson, Catecholamine Responsive Adenylate Cyclase in Human Myocardial Preparations Properties and Optimalization of Assay Conditions Scandinavian Journal of Clinical & Laboratory Investigation. ,vol. 44, pp. 317- 327 ,(1984) , 10.3109/00365518409083814
Jörg Dreinhöfer, Heinz Gögelein, Rainer Greger, Blocking kinetics of Cl− channels in colonic carcinoma cells (HT29) as revealed by 5-nitro-2-(3-phenylpropylamino)benzoic acid (NPPB) Biochimica et Biophysica Acta (BBA) - Biomembranes. ,vol. 946, pp. 135- 142 ,(1988) , 10.1016/0005-2736(88)90466-X
Heinz Gögelein, Chloride channels in epithelia Biochimica et Biophysica Acta (BBA) - Reviews on Biomembranes. ,vol. 947, pp. 521- 547 ,(1988) , 10.1016/0304-4157(88)90006-8
William Breuer, Characterization of chloride channels in membrane vesicles from the kidney outer medulla. The Journal of Membrane Biology. ,vol. 107, pp. 35- 42 ,(1989) , 10.1007/BF01871081
P. Wangemann, M. Wittner, A. Di Stefano, H. C. Englert, H. J. Lang, E. Schlatter, R. Greger, Cl(-)-channel blockers in the thick ascending limb of the loop of Henle. Structure activity relationship. Pflügers Archiv: European Journal of Physiology. ,vol. 407, ,(1986) , 10.1007/BF00584942
J D McCann, M Li, M J Welsh, Identification and regulation of whole-cell chloride currents in airway epithelium. The Journal of General Physiology. ,vol. 94, pp. 1015- 1036 ,(1989) , 10.1085/JGP.94.6.1015