Compounds > bis(1-3-dibutylbarbiturate)trimethine-oxonol

bis(1-3-dibutylbarbiturate)trimethine-oxonol and squalamine

bis(1-3-dibutylbarbiturate)trimethine-oxonol has been researched along with squalamine* in 1 studies

Other Studies

1 other study(ies) available for bis(1-3-dibutylbarbiturate)trimethine-oxonol and squalamine

Article	Year
Differential inhibition of AE1 and AE2 anion exchangers by oxonol dyes and by novel polyaminosterol analogs of the shark antibiotic squalamine. Biochemistry and cell biology = Biochimie et biologie cellulaire, 1998, Volume: 76, Issue:5 Oxonol and polyaminosterol drugs were examined as inhibitors of recombinant mouse AE1 and AE2 anion exchangers expressed in Xenopus laevis oocytes and were compared as inhibitors of AE1-mediated anion flux in red cells and in HL-60 cells that express AE2. The oxonols WW-781, diBA(5)C4, and diBA(3)C4 inhibited HL-60 cell Cl-/Cl- exchange with IC50 values from 1 to 7 microM, 100-1000 times less potent than their IC50 values for red cell Cl-/anion exchange. In Xenopus oocytes, diBA(5)C4 inhibited AE1-mediated Cl- efflux several hundred times more potently than that mediated by AE2. Several novel squalamine-related polyaminosterols were also evaluated as anion exchange inhibitors. In contrast to diBA(5)C4, polyaminosterol 1361 inhibited oocyte-expressed AE2 8-fold more potently than AE1 (IC50 0.6 versus 5.2 microM). The 3-fold less potent desulfo-analog, 1360, showed similar preference for AE2. It was found that 1361 also partially inhibited Cl- efflux from red cells, whereas neither polyaminosterol inhibited Cl efflux from HL60 cells. Thus, the oxonol diBA(5)C4 is >100-fold more potent as an inhibitor of AE1 than of AE2, whereas the polyaminosterols 1360 and 1361 are 8-fold more potent as inhibitors of AE2 than of AE1. Assay conditions and cell type influenced IC50 values for both classes of compounds. Topics: Animals; Anion Transport Proteins; Anti-Bacterial Agents; Antiporters; Barbiturates; Chloride-Bicarbonate Antiporters; Cholestanols; Dihydropyridines; Dose-Response Relationship, Drug; Erythrocytes; Fluorescent Dyes; HL-60 Cells; Humans; Inhibitory Concentration 50; Isoxazoles; Kinetics; Membrane Proteins; Mice; Oocytes; Polyamines; Sharks; SLC4A Proteins; Xenopus	1998

Article

Year

Differential inhibition of AE1 and AE2 anion exchangers by oxonol dyes and by novel polyaminosterol analogs of the shark antibiotic squalamine.

Biochemistry and cell biology = Biochimie et biologie cellulaire, 1998, Volume: 76, Issue:5

Oxonol and polyaminosterol drugs were examined as inhibitors of recombinant mouse AE1 and AE2 anion exchangers expressed in Xenopus laevis oocytes and were compared as inhibitors of AE1-mediated anion flux in red cells and in HL-60 cells that express AE2. The oxonols WW-781, diBA(5)C4, and diBA(3)C4 inhibited HL-60 cell Cl-/Cl- exchange with IC50 values from 1 to 7 microM, 100-1000 times less potent than their IC50 values for red cell Cl-/anion exchange. In Xenopus oocytes, diBA(5)C4 inhibited AE1-mediated Cl- efflux several hundred times more potently than that mediated by AE2. Several novel squalamine-related polyaminosterols were also evaluated as anion exchange inhibitors. In contrast to diBA(5)C4, polyaminosterol 1361 inhibited oocyte-expressed AE2 8-fold more potently than AE1 (IC50 0.6 versus 5.2 microM). The 3-fold less potent desulfo-analog, 1360, showed similar preference for AE2. It was found that 1361 also partially inhibited Cl- efflux from red cells, whereas neither polyaminosterol inhibited Cl efflux from HL60 cells. Thus, the oxonol diBA(5)C4 is >100-fold more potent as an inhibitor of AE1 than of AE2, whereas the polyaminosterols 1360 and 1361 are 8-fold more potent as inhibitors of AE2 than of AE1. Assay conditions and cell type influenced IC50 values for both classes of compounds.

Topics: Animals; Anion Transport Proteins; Anti-Bacterial Agents; Antiporters; Barbiturates; Chloride-Bicarbonate Antiporters; Cholestanols; Dihydropyridines; Dose-Response Relationship, Drug; Erythrocytes; Fluorescent Dyes; HL-60 Cells; Humans; Inhibitory Concentration 50; Isoxazoles; Kinetics; Membrane Proteins; Mice; Oocytes; Polyamines; Sharks; SLC4A Proteins; Xenopus

1998