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Sulfinpyrazone (0):
Recent article
Sulfinpyrazone
Abstract
We identified persons using two integrated delivery systems aged 18 years or older with a diagnosis of gout who initiated use of allopurinol, probenecid or sulfinpyrazone from 1 January 2000 to 30 June 2006. Non-adherence was measured using the medication possession ratio (MPR) over the first year o...
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PMID: 19327147
PDF is available here.
PDF is available here.
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Abstract
The mean (SD) PDC was 54% (36%) with 64% of patients considered poorly compliant over the study period. A total of 56% had experienced an extended break in UALT. Predictors of poor adherence included younger age (odds ratio (OR) 1.50, 95% CI 1.33-1.69 for ages 65-74 compared with 85 and above) and A...
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PMID: 17728328
PDF is available here.
PDF is available here.
Abstract
In vitro pyrimethamine response of Plasmodium falciparum isolates and dihydrofolate reductase (dhfr) gene sequences were analyzed in 2004-2005 and compared with our previous data. Most isolates (n = 103, all dhfr mutants) had 50% inhibitory concentrations (IC(50)s) > or = 119 nM, and six isolates ha...
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PMID: 17690390
PDF is available here.
PDF is available here.
Abstract
Our previous study (J Pharmacol Exp Ther (2006) 316:169-175) has demonstrated that morin (3,5,7,2',4'-pentahydroxyflavone), which occurs in the twigs of Morus alba L. documented in traditional Chinese medicinal literature for treatment of conditions akin to gout, is a potent inhibitor of urate uptak...
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PMID: 17325024
PDF is available here.
PDF is available here.
European Journal of Pharmacology (560)2-3 2007
Block of CFTR-dependent chloride currents by inhibitors of multidrug resistance-associated proteins.
Abstract
We have tested the ability of known inhibitors of multidrug resistance-associated proteins to affect CFTR Cl- currents. We have found that sulfinpyrazone, probenecid, and benzbromarone are also inhibitors of CFTR activity, with a mechanism involving blockage of the channel pore....
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PMID: 17320853
PDF is available here.
PDF is available here.
Abstract
Cryopreserved, transiently transfected HepG2 cells were compared to freshly transfected HepG2 cells for use in a pregnane X receptor (PXR) transactivation assay. Assay performance was similar for both cell preparations; however, cryopreserved cells demonstrated less interassay variation. Validation w...
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PMID: 17259590
PDF is available here.
PDF is available here.
Abstract
The uricosuric agent sulfinpyrazone (SFZ) is metabolized via C-glucuronidation, an uncommon metabolic pathway, in humans. The present study aimed to characterize SFZ glucuronidation by human liver microsomes (HLMs) and identify the hepatic forms of UDP-glucuronosyltransferase responsible for this pa...
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PMID: 16985098
PDF is available here.
PDF is available here.
Abstract
Cytochrome P4503A4 (CYP3A4) is the principal drug-metabolizing enzyme in human liver. Drug-drug interactions (DDIs) caused by induction of CYP3A4 can result in decreased exposure to coadministered drugs, with potential loss of efficacy. Immortalized hepatocytes (Fa2N-4 cells) have been proposed as a...
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PMID: 16837568
PDF is available here.
PDF is available here.
Abstract
Abstract
We studied ascorbate uptake and recycling by quiescent and lipopolysaccharide-activated RAW264.7 murine macrophages. These cells concentrated ascorbate 100-fold in overnight culture, achieving steady-state concentrations of more than 10 mM at extracellular concentrations of 20-100 muM. This steep gr...
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PMID: 16274880
PDF is available here.
PDF is available here.
Biochimica et Biophysica Acta (1712)2 2005
Abstract
We have characterized the transport of the reduced form of ascorbic acid in passaged primary human chondrocytes to discern the physiologically relevant pathways of ascorbic acid transport in cartilage. We have found that chondrocytes are robust concentrators of ascorbic acid, capable of transporting...
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PMID: 15921655
PDF is available here.
PDF is available here.
Molecular and Cellular Biochemistry (271)1-2 2005
Abstract
We examined ascorbate transport and mRNA expression of sodium-dependent vitamin C transporters (SVCT) by RT-PCR in the pig coronary artery endothelial cell cultures. When 14C-ascorbate uptake in endothelial cells was examined as 14C or by HPLC, the two values did not differ from each other. 14C-asco...
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PMID: 15881654
PDF is available here.
PDF is available here.
Abstract
We show that renal excretion of PAH in isolated perfused kidneys from wild-type and Mrp2-deficient (TR(-)) rats is not significantly different. Uptake of [(14)C]PAH in membrane vesicles expressing two different MRP2 clones isolated from Sf9 and MDCKII cells exhibited a low affinity for PAH (Sf9, 5 +...
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PMID: 15504935
PDF is available here.
PDF is available here.
Abstract
Sulfinpyrazone increased the mean exposure of nateglinide by 28% when both drugs were administered in combination. Nateglinide, given as a single dose or co-administered with multiple doses of sulfinpyrazone, was safe and well tolerated in healthy subjects....
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PMID: 15197517
PDF is available here.
PDF is available here.
Brain Research (993)1-2 2003
Abstract
We evaluated the hypothesis that glucose regulates DHAA uptake and reduction to ascorbate (i.e., recycling) by skeletal muscle cells and cerebral astrocytes. DHAA uptake was inhibited partially by glucose added simultaneously with DHAA. Comparison of wild type L6 skeletal muscle cells with an L6-der...
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PMID: 14642847
PDF is available here.
PDF is available here.
Abstract
This study examined the accumulation and transport of two related systemic opioids used as antidiarrhoeal drugs and compared their rates of transport with known P-glycoprotein (P-gp) substrates used in our in vitro environment. Cellular uptake and efflux and transcellular transport were all determin...
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PMID: 14613723
PDF is available here.
PDF is available here.
Abstract
We demonstrated that UVB as well as X-ray irradiation inhibit the export function of the ABC transporters in a dose-dependent fashion. For PBL, this effect did not correlate with an apoptotic phenotype. In the case of the tumor cell lines, even though the irradiation-induced inhibition of membrane t...
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PMID: 14509956
PDF is available here.
PDF is available here.
Abstract
These results are consistent with a novel mechanism of astrocytic ascorbate accumulation that is inhibited by lipophilic radicals and protected by lipophilic antioxidants such as propofol.
Copyright 2002 Wiley-Liss, Inc....
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PMID: 12112364
PDF is available here.
PDF is available here.
Free Radical Research (36)6 2002
Abstract
Our results suggest a new direction for the pharmacological actions of sulfinpyrazone in free radical scavenging properties....
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PMID: 12180194
PDF is available here.
PDF is available here.
Pharmacology (64)3 2002
Abstract
We compared directional permeability in the wild-type cell lines, MDCK strains I and II, and LLC-PK1, vs. cell lines that overexpress a single transporter, in both the presence and absence of various inhibitors, for furosemide as compared to vinblastine. Sulfinpyrazone significantly inhibited the tr...
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PMID: 11834888
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (276)41 2001
Abstract
We recently identified a highly conserved tryptophan residue in the related MRP1 that is critical for the substrate specificity of this protein. In the present study, we have examined the effect of replacing the analogous tryptophan residue at position 1254 of MRP2. We found that only nonconservativ...
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PMID: 11500505
PDF is available here.
PDF is available here.
Cancer Research (61)14 2001
Abstract
We examined the role of multidrug resistance protein (MRP) 1 (ABCC1) in the emergence of mitoxantrone (MX) cross-resistance in a MCF7 breast cancer cell line selected for resistance to etoposide. The resistant cell line, MCF7/VP, expresses high levels of MRP1, whereas the parental cell line, MCF7/WT...
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PMID: 11454692
PDF is available here.
PDF is available here.
Abstract
These results provide evidence that the metabolism of both (S)-WARF and SPZS is mediated by a common enzyme, P450 2C9, which is central to understanding the WARF-SPZ interaction and SPZS-mediated drug interactions in general....
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PMID: 11302937
PDF is available here.
PDF is available here.
Abstract
Mean uricemia decreased with allopurinol (0.58+/-0.12 vs. 0.41+/-0.07 mmol/liter, p = 0.0001) as well as with sulfinpyrazone (0.51+/-0.13 vs. 0.40+/-0.12 mmol/liter, p = 0.0001). Mean creatinine increased (171+/-42 and 164+/-35 micromol/liter, p = 0.01) with allopurinol, whereas it tended to decreas...
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PMID: 11124491
PDF is available here.
PDF is available here.
Molecular Carcinogenesis (29)3 2000
Abstract
We examined the effect of regulatable GSTP1-1 expression in MRP2-rich HepG2 cells on 4-nitroquinoline 1-oxide (4NQO)-induced cytotoxicity and genotoxicity (nucleic-acid adduct formation). Expression of GSTP1-1 was associated with a fourfold to tenfold protection from 4NQO-induced cytotoxicity. Inhib...
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PMID: 11108662
PDF is available here.
PDF is available here.
Abstract
We demonstrate that glutathione transport in MDCKII-MRP1 cells is inhibited by the inhibitors of organic anion transporters sulfinpyrazone, indomethacin, probenecid and benzbromarone. In MDCKII-MRP2 cells, GSH export is stimulated by low concentrations of sulfinpyrazone or indomethacin, whereas expo...
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PMID: 10917554
PDF is available here.
PDF is available here.
Abstract
We further characterized ascorbate uptake in the cultured cells. The data fitted best with a Hill coefficient of 1 for ascorbate (K(asc) = 22 +/- 2 microM) and 2 for Na(+) (K(Na) = 84 +/- 10 mM). The anion transport inhibitors sulfinpyrazone and 4,4'-diisothiocyanatostilbene-2,2'-disulfonate (DIDS)...
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PMID: 11025402
PDF is available here.
PDF is available here.
BioTechniques (26)2 1999
Abstract
We describe a rapid and sensitive method to assay intracellular calcium ions in human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells from multi-well plates using a fluorometer equipped with on-line injectors. We examine the compatibility of visible-light excitable dyes Calcium Green...
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PMID: 10023544
PDF is available here.
PDF is available here.
Abstract
Aspirin (325 and 900 mg/d) is effective for a period of 1 year in reducing the frequency of saphenous vein bypass graft occlusion when begun 1 day before operation or on the day of operation. Aspirin in combination with dipyridamole is not more effective than aspirin alone in the prevention of saphe...
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PMID: 9822069
PDF is available here.
PDF is available here.
Cell Calcium (24)3 1998
Abstract
We used two alternative techniques of dye loading to examine the changes of intracellular calcium induced in rat osteoclasts by three stimuli. Osteoclasts loaded with the calcium indicator Fura-2 by the acetoxymethyl (AM) ester technique appeared to display marked nuclear calcium amplification. Duri...
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PMID: 9883275
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (273)32 1998
Abstract
These results are the first demonstration that GST A1-1 and MRP1 can act in synergy to protect cells from the cytotoxicity of a nitrogen mustard, chlorambucil....
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PMID: 9685354
PDF is available here.
PDF is available here.
Pharmacological Research (38)2 1998
Abstract
The protective activity of the phenylbutazone derivative, sulfinpyrazone on retinal lesions has been assessed in rabbits with severe streptozotocin-induced diabetes. Sulfinpyrazone (8 mg kg-1 per day per os) was administered in diabetic animals in two different experimental procedures: for 135 days...
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PMID: 9721595
PDF is available here.
PDF is available here.
Abstract
We have compared the expression of P-gp and Mrp1 in homogenates, isolated capillaries, primary cultured endothelial cells, and RBE4 immortalized endothelial cells from rat brain. Whereas the mdr1a P-gp-encoding mRNA was specifically detected in brain microvessels and mdr1b mRNA in brain parenchyma,...
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PMID: 9681461
PDF is available here.
PDF is available here.
Abstract
We report that BCECF localizes to hydrogenosomes (hydrogen-generating organelles found in several phylogenetically separate groups of anaerobic protists) in Trichomonas vaginalis, where it was observable by fluorescence microscopy. Its cellular location was confirmed by treatment of BCECF-loaded cel...
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PMID: 9696354
PDF is available here.
PDF is available here.
Abstract
A case of sulfinpyrazone-associated acute renal failure is reported. Sulfinpyrazone can cause reversible acute renal failure from acute tubular necrosis in patients with volume depletion. Brown tubular casts on urine microscopy and a fractional excretion of sodium greater than 1 are helpful in the d...
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PMID: 9587090
PDF is available here.
PDF is available here.
Abstract
Abstract
Inhibition of [14C]-urate uptake by uricosuric and antiuricosuric agents was investigated in human brush-border membrane vesicles, urate being transported either by anion exchange mechanisms or by voltage sensitive pathway. The IC50 for drugs on [14C]-urate uptake in vesicles loaded with 1 mM cold u...
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PMID: 9023298
PDF is available here.
PDF is available here.
Chemistry & Biology (3)9 1996
Abstract
Photodegradation processes like that observed for indo-1 are likely to be possible for all cation indicators that contain bis(carboxymethyl)anilino moieties, which include essentially all fluorescent indicators for Ca2+ and Mg2+ currently in biological use. If unrecognized, this photochemical dealky...
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PMID: 8939693
PDF is available here.
PDF is available here.
FEBS Letters (391)1-2 1996
Abstract
We demonstrate that the glutathione S-conjugate of the diuretic drug ethacrynic acid, which is an efficient inhibitor of glutathione S-transferases, is a high-affinity substrate and inhibitor of the glutathione S-conjugate pump associated with MRP. This implies that ethacrynic acid may modulate drug...
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PMID: 8706899
PDF is available here.
PDF is available here.
Microcirculation (3)2 1996
Abstract
Microvascular cells derived from rat hindlimb muscles demonstrated endothelial characteristics. These cells accumulated reduced vitamin C by means of Na+-dependent ascorbate transporters, which are distinct from hexose carriers. The high endothelial ascorbate concentration at steady-state is consist...
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PMID: 8839443
PDF is available here.
PDF is available here.
Abstract
The properties of silica gel as stationary phase are determined mainly by siloxane, silanol and metal-silanate functional groups. The metals (Na, Ca etc.) getting into the product as trace elements in the course of manufacture may cause the appearance of artefacts. In our previous studies the ion ex...
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PMID: 8975540
PDF is available here.
PDF is available here.
Abstract
Our results demonstrate the uselessness of applying these drugs in order to conceal the illegal use of clenbuterol in meat production....
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PMID: 8871117
PDF is available here.
PDF is available here.
Abstract
From 1983 to 1987, the Department of Veterans Affairs (DVA) Cooperative Studies Program (CSP) conducted a multicenter clinical trial (CSP #207) to determine whether four different antiplatelet regimens compared to placebo could prevent the occlusion of grafts following coronary artery bypass surgery...
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PMID: 8582151
PDF is available here.
PDF is available here.
Abstract
Sulfinpyrazone markedly potentiates the anticoagulant effect of warfarin. The increased clotting time is accompanied by a marked decrease in the clearance of (S)-warfarin by virtue of a decrease in the P4502C9-catalyzed formation clearance to its major and inactive metabolite (S)-7-hydroxywarfarin....
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PMID: 7587949
PDF is available here.
PDF is available here.
Biochemical Pharmacology (49)11 1995
Abstract
The caecal microflora from female rats show a greater ability to reduce the sulphoxide group of sulindac than either the liver or kidneys. Studies on sulphoxide reduction by Escherichia coli showed that NADH, NADPH and dithiothreitol (DTT), but not acetaldehyde could act as cofactors. The cytosolic...
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PMID: 7786297
PDF is available here.
PDF is available here.
Biochemical Pharmacology (49)11 1995
Abstract
The reduction of sulindac, sulphinpyrazone and diphenyl sulphoxide to their thioether analogues has been studied in vitro using rat and rabbit tissues. Sulindac reduction was about 10-fold higher in homogenates of rat kidney and liver than in other tissues although the tissue differences decreased w...
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PMID: 7786296
PDF is available here.
PDF is available here.
Drug Safety (11)4 1994
Abstract
Nonsteroidal anti-inflammatory drugs (NSAIDs) are now commonly used for the treatment of acute gout, but caution is required in view of their adverse effects, especially in the elderly. Colchicine is still an effective acute agent, but care must be taken to monitor toxicity. Intra-articular glucocor...
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PMID: 7848545
PDF is available here.
PDF is available here.
Abstract
Abstract
We have found that the addition of sulfinpyrazone, a known organic-anion transporter inhibitor in epithelial cells and in macrophages, severely impairs the leakage of the Fluo-3 probe from the cytoplasmic matrix. Under appropriate conditions, sulfinpyrazone has little effect on the cell physiology a...
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PMID: 8034984
PDF is available here.
PDF is available here.
Abstract
Our observations strongly suggest that exogenously applied, nonderivatized cAMP can gain access to the cytoplasm of isolated RPE cells via organic anion transporters. Thus, if cAMP were secreted by retinal cells into the subretinal space, it could be taken up by RPE cells and subsequently act as an...
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PMID: 8300345
PDF is available here.
PDF is available here.
Agents and Actions (40)3-4 1993
Abstract
These results indicated that an important component of the PAF-induced systemic effects is mediated by reactions which can be inhibited by sulfinpyrazone. Furthermore, PAF-induced thrombocytopenia is not a direct PAF effect since it can be inhibited by sulfinpyrazone....
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PMID: 8023738
PDF is available here.
PDF is available here.
Abstract
We selected probenecid-resistant (PBR) J774 cells by growing them in medium containing increasing concentrations of probenecid. When PBR and unselected J774 cells were loaded with LY by ATP4- permeabilization, the amount of LY accumulated by the PBR cells was about half that in the unselected cells....
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PMID: 7909709
PDF is available here.
PDF is available here.
Cardiology (83)4 1993
Abstract
We have done a random-order, double-blind, crossover study of the effect of the platelet-active drug sulfinpyrazone on treadmill exercise-induced angina pectoris in 30 men with coronary artery disease. The mean duration of exercise before onset of angina was 43 s longer after taking sulfinpyrazone t...
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PMID: 8281538
PDF is available here.
PDF is available here.
Abstract
We adapted this strategy to the study organic anion transport in lymphocytes. Cloned lymphoma cells and normal and activated human T cells were loaded with a membrane-impermeant, organic anion dye (Lucifer Yellow) by electroporation. Dye efflux in lymphocytes was rapid, energy-dependent, and inhibit...
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PMID: 1431154
PDF is available here.
PDF is available here.
Abstract
Abstract
Abstract
Monoisoamyl meso-2,3-dimercaptosuccinate (Mi-ADMS) and the unesterified 2,3-dimercaptosuccinic acid (DMSA) were evaluated for relative reactivities against metallothionein (MT)-bound cadmium (Cd) in vitro by elution of the reaction products through Sephadex G-75 gel. After 3 hr of incubation, Mi-ADM...
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PMID: 1636055
PDF is available here.
PDF is available here.
Abstract
Abstract