Experts and Doctors on sulfonamides in Sweden


Locale: Sweden
Topic: sulfonamides

Top Publications

  1. Hjorth S, Karlsson C, Jucaite A, Varnäs K, Wählby Hamrén U, Johnström P, et al. A PET study comparing receptor occupancy by five selective cannabinoid 1 receptor antagonists in non-human primates. Neuropharmacology. 2016;101:519-30 pubmed publisher
  2. Famer D, Wahlund L, Crisby M. Rosuvastatin reduces microglia in the brain of wild type and ApoE knockout mice on a high cholesterol diet; implications for prevention of stroke and AD. Biochem Biophys Res Commun. 2010;402:367-72 pubmed publisher
    ..The results from our study show that rosuvastatin reduces inflammatory cells in the brain. This finding is essential for furthering the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease (AD) and stroke. ..
  3. Berg S, Bergh M, Hellberg S, Högdin K, Lo Alfredsson Y, Söderman P, et al. Discovery of novel potent and highly selective glycogen synthase kinase-3? (GSK3?) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines. J Med Chem. 2012;55:9107-19 pubmed publisher
    ..The inhibitors are suitable for in vivo efficacy testing and may serve as a new treatment strategy for Alzheimer's disease. ..
  4. Malmström J, Viklund J, Slivo C, Costa A, Maudet M, Sandelin C, et al. Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors. Bioorg Med Chem Lett. 2012;22:5919-23 pubmed publisher
    ..The synthesis and SAR around this hit is described. The X-ray coordinates of ligand 4a with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water molecule. ..
  5. Bohm F, Settergren M, Gonon A, Pernow J. The endothelin-1 receptor antagonist bosentan protects against ischaemia/reperfusion-induced endothelial dysfunction in humans. Clin Sci (Lond). 2005;108:357-63 pubmed
    ..Bosentan may thus be a feasible therapeutic agent in the treatment of ischaemia/reperfusion injury in humans. ..
  6. Krjukova J, Holmqvist T, Danis A, Akerman K, Kukkonen J. Phospholipase C activator m-3M3FBS affects Ca2+ homeostasis independently of phospholipase C activation. Br J Pharmacol. 2004;143:3-7 pubmed
    ..m-3M3FBS also interfered with store-operated Ca(2+) influx and Ca(2+) extrusion. In conclusion, m-3M3FBS cannot be considered either potent or specific PLC activator. ..
  7. Borgegard T, Jureus A, Olsson F, Rosqvist S, Sabirsh A, Rotticci D, et al. First and second generation ?-secretase modulators (GSMs) modulate amyloid-? (A?) peptide production through different mechanisms. J Biol Chem. 2012;287:11810-9 pubmed publisher
    ..Combined, these data provide compelling evidence of a growing class of in vivo active GSMs, which are selective for A? modulation and have a different mechanism of action compared with the original class of GSMs described. ..
  8. Lönnroth C, Andersson M, Arvidsson A, Nordgren S, Brevinge H, Lagerstedt K, et al. Preoperative treatment with a non-steroidal anti-inflammatory drug (NSAID) increases tumor tissue infiltration of seemingly activated immune cells in colorectal cancer. Cancer Immun. 2008;8:5 pubmed
    ..These findings agree with previous information that high prostanoid activities in colorectal cancer increase the risk for reduced disease-specific survival following tumor resection. ..
  9. Andersson C, Forsgren N, Akfur C, Allgardsson A, Berg L, Engdahl C, et al. Divergent structure-activity relationships of structurally similar acetylcholinesterase inhibitors. J Med Chem. 2013;56:7615-24 pubmed publisher
    ..The divergent SARs will be utilized to develop reversible inhibitors of AChE into reactivators of nerve agent-inhibited AChE. ..

More Information


  1. Lönnroth C, Andersson M, Nordgren S, Lundholm K. Downregulation of Prominin 1/CD133 expression in colorectal cancer by NSAIDs following short-term preoperative treatment. Int J Oncol. 2012;41:15-23 pubmed publisher
    ..Our results show that short-term preoperative NSAID treatment downregulates colon cancer tissue expression of Prominin 1/CD133, a stem cell marker indicative of survival prognosis as confirmed. ..
  2. Bäck M, Yin L, Ingelsson E. Cyclooxygenase-2 inhibitors and cardiovascular risk in a nation-wide cohort study after the withdrawal of rofecoxib. Eur Heart J. 2012;33:1928-33 pubmed publisher
    ..79-1.11). Whereas safety measures appear to have limited serious cardiovascular consequences of COX-2 inhibitors, the risk of developing atrial fibrillation may have been overlooked and may necessitate consideration and precautions. ..
  3. Sisask G, Marsell R, Sundgren Andersson A, Larsson S, Nilsson O, Ljunggren O, et al. Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone. 2013;54:126-32 pubmed publisher
    ..The fractures healed with a bony callus without an obvious endochondral component, suggesting that AZD2858 drives mesenchymal cells into the osteoblastic pathway. This leads to direct bone repair in an unstable fracture milieu. ..
  4. Hardebo J. Subcutaneous sumatriptan in cluster headache: a time study of the effect on pain and autonomic symptoms. Headache. 1993;33:18-21 pubmed
  5. Uller L, Mathiesen J, Alenmyr L, Korsgren M, Ulven T, Hogberg T, et al. Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation. Respir Res. 2007;8:16 pubmed
    ..Our data suggest that CRTH2 antagonism alone is effective in mouse allergic airway inflammation even to the extent that this mechanism can explain the efficacy of ramatroban. ..
  6. Maddahi A, Edvinsson L. Cerebral ischemia induces microvascular pro-inflammatory cytokine expression via the MEK/ERK pathway. J Neuroinflammation. 2010;7:14 pubmed publisher
  7. Meunier A, Aspenberg P, Good L. Celecoxib does not appear to affect prosthesis fixation in total knee replacement: A randomized study using radiostereometry in 50 patients. Acta Orthop. 2009;80:46-50 pubmed publisher
    ..Confidence intervals were narrow. It is unlikely that Celecoxib increases the risk of loosening, and it may be used safely in conjunction with TKR. ..
  8. Frenckner B, Broomé M, Lindström M, Radell P. Platelet-derived growth factor inhibition--a new treatment of pulmonary hypertension in congenital diaphragmatic hernia?. J Pediatr Surg. 2008;43:1928-31 pubmed publisher
    ..After administration of the platelet-derived growth factor (PDGF) receptor antagonist imatinib, pulmonary artery pressure gradually decreased to acceptable levels and the patient's clinical condition gradually improved. ..
  9. Massoumi R, Nielsen C, Azemovic D, Sjölander A. Leukotriene D4-induced adhesion of Caco-2 cells is mediated by prostaglandin E2 and upregulation of alpha2beta1-integrin. Exp Cell Res. 2003;289:342-51 pubmed
    ..This suggests that inflammatory mediators such as LTD4 can be involved in the dissemination and survival of colon cancer cells. ..
  10. Hoa N, Norberg A, Sillard R, Van Phan D, Thuan N, Dzung D, et al. The possible mechanisms by which phanoside stimulates insulin secretion from rat islets. J Endocrinol. 2007;192:389-94 pubmed
    ..Phanoside stimulated insulin secretion from Wand GK rat islets. This effect seems to be exerted distal to K-ATP channels and L-type Ca2+ channels, which is on the exocytotic machinery of the B-cells. ..
  11. Eriksson L, Erdogdu O, Nystrom T, Zhang Q, Sjoholm A. Effects of some anti-diabetic and cardioprotective agents on proliferation and apoptosis of human coronary artery endothelial cells. Cardiovasc Diabetol. 2012;11:27 pubmed publisher
    ..This may add yet another valuable property to their therapeutic effect, increasing their clinical utility in type 2 diabetic patients in whom endothelial dysfunction is a prominent feature that adversely affect their survival. ..
  12. Rosendahl A, Gundewar C, Said K, Karnevi E, Andersson R. Celecoxib synergizes human pancreatic ductal adenocarcinoma cells to sorafenib-induced growth inhibition. Pancreatology. 2012;12:219-26 pubmed publisher
    ..These results suggest that combined treatment with sorafenib and celecoxib synergistically induce growth inhibition and apoptosis in pancreatic adenocarcinoma cells through a process involving p21(WAF1/Cip1) suppression. ..
  13. Johansson D, Falk A, Marcus M, Svensson T. Celecoxib enhances the effect of reboxetine and fluoxetine on cortical noradrenaline and serotonin output in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2012;39:143-8 pubmed publisher
    ..These findings provide, in principle, novel experimental support for the clinical utility of combined treatment with antidepressant and anti-inflammatory drugs, such as COX-2 inhibitors, in MDD. ..
  14. Wang F, Appelkvist P, Klason T, Gissberg O, Bogstedt A, Eliason K, et al. Decreased axonal transport rates in the Tg2576 APP transgenic mouse: improvement with the gamma-secretase inhibitor MRK-560 as detected by manganese-enhanced MRI. Eur J Neurosci. 2012;36:3165-72 pubmed publisher
    ..Chronic treatment in vivo with a gamma-secretase inhibitor, MRK-560, significantly reduces soluble and insoluble forms of A?, and fully reverses the axonal transport dysfunction...
  15. Sörenson S, Fohlin H, Lindgren A, Lindskog M, Bergman B, Sederholm C, et al. Predictive role of plasma vascular endothelial growth factor for the effect of celecoxib in advanced non-small cell lung cancer treated with chemotherapy. Eur J Cancer. 2013;49:115-20 pubmed publisher
    ..64 [confidence interval (CI) 0.43-0.95], p=0.028). Low pretreatment plasma levels of VEGF appear to be predictive of a positive effect of celecoxib on survival. ..
  16. Sundstrom L, Radstrom P, Swedberg G, Skold O. Site-specific recombination promotes linkage between trimethoprim- and sulfonamide resistance genes. Sequence characterization of dhfrV and sulI and a recombination active locus of Tn21. Mol Gen Genet. 1988;213:191-201 pubmed
    ..Similar structures were found at the 3' ends of the antibiotic resistance genes in Tn7, which could indicate similar recombination mechanisms to be effective in the evolutionary construction of all these different resistance elements. ..
  17. Bergman E, Matsson E, Hedeland M, Bondesson U, Knutson L, Lennernas H. Effect of a single gemfibrozil dose on the pharmacokinetics of rosuvastatin in bile and plasma in healthy volunteers. J Clin Pharmacol. 2010;50:1039-49 pubmed publisher
    ..This study demonstrates the value of monitoring the plasma pharmacokinetics of the inhibitor, and not only the drug under investigation, to improve the mechanistic interpretation...
  18. Waldsee R, Ahnstedt H, Eftekhari S, Edvinsson L. Involvement of calcium-calmodulin-dependent protein kinase II in endothelin receptor expression in rat cerebral arteries. Am J Physiol Heart Circ Physiol. 2010;298:H823-32 pubmed publisher
    ..CAMKII is involved in the upregulation of the endothelin ET(B) receptor and interacts with the ERK1/2 pathway to enhance receptor expression. CAMKII has no effect on the contractile apparatus in rat cerebral arteries...
  19. Carlsson L, Andersson B, Linhardt G, Löfberg L. Assessment of the ion channel-blocking profile of the novel combined ion channel blocker AZD1305 and its proarrhythmic potential versus dofetilide in the methoxamine-sensitized rabbit in vivo. J Cardiovasc Pharmacol. 2009;54:82-9 pubmed publisher
  20. Johansson M, Johansson N, Lund B. Xenobiotics and the glucocorticoid receptor: additive antagonistic effects on tyrosine aminotransferase activity in rat hepatoma cells. Basic Clin Pharmacol Toxicol. 2005;96:309-15 pubmed
    ..Thus, co-exposure to such different chemicals as persistent organic pollutants and pesticides may affect cells additively. Chemical interference with the glucocorticoid hormone system therefore deserves further attention in vivo. ..
  21. Voytyuk O, Lennartsson J, Mogi A, Caruana G, Courtneidge S, Ashman L, et al. Src family kinases are involved in the differential signaling from two splice forms of c-Kit. J Biol Chem. 2003;278:9159-66 pubmed
    ..In summary, the two splice forms show, despite only a four-amino acid sequence difference, remarkable differences in their signaling capabilities. ..
  22. Huss U, Ringbom T, Perera P, Bohlin L, Vasänge M. Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay. J Nat Prod. 2002;65:1517-21 pubmed
    ..This study showed that a COX-2-catalyzed PGE(2) assay using SPA is suitable for screening natural compounds with respect to COX-2 inhibition. ..
  23. Qvarnstr m Y, Swedberg G. Sulphonamide resistant commensal Neisseria with alterations in the dihydropteroate synthase can be isolated from carriers not exposed to sulphonamides. BMC Microbiol. 2002;2:34 pubmed
    ..meningitidis. Sulphonamide resistant commensal Neisseria were isolated from an environment not exposed to sulphonamides, suggesting that resistant Neisseria has become a natural part of the commensal throat flora...
  24. Skold O. Resistance to trimethoprim and sulfonamides. Vet Res. 2001;32:261-73 pubmed
    ..This means that susceptibility will not return after suspending the use of sulfonamide and trimethoprim. ..
  25. Swedberg G, Ringertz S, Sk ld O. Sulfonamide resistance in Streptococcus pyogenes is associated with differences in the amino acid sequence of its chromosomal dihydropteroate synthase. Antimicrob Agents Chemother. 1998;42:1062-7 pubmed
    ..Kinetic measurements established different affinities for sulfathiazole for DHPS enzymes isolated from resistant and susceptible strains...
  26. Swedberg G, Fermer C, Skold O. Point mutations in the dihydropteroate synthase gene causing sulfonamide resistance. Adv Exp Med Biol. 1993;338:555-8 pubmed
  27. Fermer C, Kristiansen B, Skold O, Swedberg G. Sulfonamide resistance in Neisseria meningitidis as defined by site-directed mutagenesis could have its origin in other species. J Bacteriol. 1995;177:4669-75 pubmed
    ..This observation supports the idea of an interspecies transfer of genetic material in Neisseria species as a mechanism for the development of chromosomally mediated resistance. ..
  28. Radstrom P, Fermer C, Kristiansen B, Jenkins A, Skold O, Swedberg G. Transformational exchanges in the dihydropteroate synthase gene of Neisseria meningitidis: a novel mechanism for acquisition of sulfonamide resistance. J Bacteriol. 1992;174:6386-93 pubmed
    ..The origin of the resistance-mediating segment of the gene is unknown, but hybridization results showed the presence of homologous dhps genes in Neisseria gonorrhoeae and N. lactamica but not in N. subflava or Branhamella catarrhalis. ..
  29. Swahn B, Macsari I, Viklund J, Ohberg L, Sjödin J, Neelissen J, et al. Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides. Bioorg Med Chem Lett. 2009;19:2009-12 pubmed publisher
    ..The effort to optimize these hits into LXRbeta selectivity is described. Compound 20 displayed desirable pharmacokinetic profile and up regulation of ABCA1 and ABCG1 mRNA in the brain were achieved when evaluated in vivo in mice...
  30. Alberts P, Nilsson C, Selén G, Engblom L, Edling N, Norling S, et al. Selective inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains. Endocrinology. 2003;144:4755-62 pubmed
    ..The results support previous suggestions that selective 11 beta-HSD1 inhibitors lower blood glucose levels and improve insulin sensitivity in different mouse models of type 2 diabetes. ..
  31. Gisslen M, Fuchs D, Hagberg L, Svennerholm B, Zetterberg H. Cerebrospinal fluid viral breakthrough in two HIV-infected subjects on darunavir/ritonavir monotherapy. Scand J Infect Dis. 2012;44:997-1000 pubmed publisher
    ..These 2 cases raise concerns about the effectiveness of darunavir/ritonavir monotherapy in HIV CNS infection. Thus, we recommend caution with protease inhibitor monotherapy until CNS results have been obtained from clinical studies. ..