tolbutamide

Summary

Summary: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)

Top Publications

  1. ncbi Truncation of Kir6.2 produces ATP-sensitive K+ channels in the absence of the sulphonylurea receptor
    S J Tucker
    University Laboratory of Physiology, Oxford, UK
    Nature 387:179-83. 1997
  2. ncbi The cAMP sensor Epac2 is a direct target of antidiabetic sulfonylurea drugs
    Chang Liang Zhang
    Division of Cellular and Molecular Medicine, Department of Physiology and Cell Biology, Kobe University Graduate School of Medicine, 7 5 1 Kusunoki cho, Chuo Ku, Kobe 650 0017, Japan
    Science 325:607-10. 2009
  3. pmc Glucose and pharmacological modulators of ATP-sensitive K+ channels control [Ca2+]c by different mechanisms in isolated mouse alpha-cells
    Nicolas Quoix
    Unit of Endocrinology and Metabolism, University of Louvain Faculty of Medicine, Brussels, Belgium
    Diabetes 58:412-21. 2009
  4. pmc Tolbutamide controls glucagon release from mouse islets differently than glucose: involvement of K(ATP) channels from both α-cells and δ-cells
    Rui Cheng-Xue
    pôle d endocrinologie, diabète et nutrition, Institut de Recherche Expérimentale et Clinique, Universite Catholique de Louvain, Brussels, Belgium
    Diabetes 62:1612-22. 2013
  5. pmc In vitro insulin secretion by pancreatic tissue from infants with diazoxide-resistant congenital hyperinsulinism deviates from model predictions
    Jean Claude Henquin
    Unit of Endocrinology and Metabolism, Faculty of Medicine, University of Louvain, Brussels, Belgium
    J Clin Invest 121:3932-42. 2011
  6. ncbi Tolbutamide reduces glioma cell proliferation by increasing connexin43, which promotes the up-regulation of p21 and p27 and subsequent changes in retinoblastoma phosphorylation
    Rosa Sánchez-Alvarez
    Departamento de Bioquimica y Biologia Molecular, INCYL, Universidad de Salamanca, Spain
    Glia 54:125-34. 2006
  7. ncbi Effects of pomegranate juice on human cytochrome P450 2C9 and tolbutamide pharmacokinetics in rats
    Masashi Nagata
    School of Pharmaceutical Sciences, Kyushu University of Health and Welfare, 1714 1 Yoshino, Nobeoka City, Miyazaki, 882 8508, Japan
    Drug Metab Dispos 35:302-5. 2007
  8. ncbi Chronic exposure to tolbutamide and glibenclamide impairs insulin secretion but not transcription of K(ATP) channel components
    Andrew J Ball
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Pharmacol Res 50:41-6. 2004
  9. pmc Tolbutamide stimulation of pancreatic beta-cells involves both cell recruitment and increase in the individual Ca(2+) response
    F C Jonkers
    , University of Louvain Faculty of Medicine, Brussels, Belgium
    Br J Pharmacol 133:575-85. 2001
  10. ncbi Dual mechanism of the potentiation by glucose of insulin secretion induced by arginine and tolbutamide in mouse islets
    Nobuyoshi Ishiyama
    Unité d Endocrinologie et Métabolisme, University of Louvain Faculty of Medicine, Brussels, Belgium
    Am J Physiol Endocrinol Metab 290:E540-9. 2006

Detail Information

Publications224 found, 100 shown here

  1. ncbi Truncation of Kir6.2 produces ATP-sensitive K+ channels in the absence of the sulphonylurea receptor
    S J Tucker
    University Laboratory of Physiology, Oxford, UK
    Nature 387:179-83. 1997
    ..We show here that the primary site at which ATP acts to mediate K-ATP channel inhibition is located on Kir6.2, and that SUR1 is required for sensitivity to sulphonylureas and diazoxide and for activation by Mg-ADP...
  2. ncbi The cAMP sensor Epac2 is a direct target of antidiabetic sulfonylurea drugs
    Chang Liang Zhang
    Division of Cellular and Molecular Medicine, Department of Physiology and Cell Biology, Kobe University Graduate School of Medicine, 7 5 1 Kusunoki cho, Chuo Ku, Kobe 650 0017, Japan
    Science 325:607-10. 2009
    ..reduced both in vitro and in vivo in mice lacking Epac2, and the glucose-lowering effect of the sulfonylurea tolbutamide was decreased in these mice. Epac2 thus contributes to the effect of sulfonylureas to promote insulin secretion...
  3. pmc Glucose and pharmacological modulators of ATP-sensitive K+ channels control [Ca2+]c by different mechanisms in isolated mouse alpha-cells
    Nicolas Quoix
    Unit of Endocrinology and Metabolism, University of Louvain Faculty of Medicine, Brussels, Belgium
    Diabetes 58:412-21. 2009
    ..We studied how glucose and ATP-sensitive K(+) (K(ATP)) channel modulators affect alpha-cell [Ca(2+)](c)...
  4. pmc Tolbutamide controls glucagon release from mouse islets differently than glucose: involvement of K(ATP) channels from both α-cells and δ-cells
    Rui Cheng-Xue
    pôle d endocrinologie, diabète et nutrition, Institut de Recherche Expérimentale et Clinique, Universite Catholique de Louvain, Brussels, Belgium
    Diabetes 62:1612-22. 2013
    ..Diazoxide did not reverse the glucagonostatic effect of glucose. Tolbutamide decreased glucagon secretion at 1 mmol/L glucose (G1) but stimulated it at 7 mmol/L glucose (G7)...
  5. pmc In vitro insulin secretion by pancreatic tissue from infants with diazoxide-resistant congenital hyperinsulinism deviates from model predictions
    Jean Claude Henquin
    Unit of Endocrinology and Metabolism, Faculty of Medicine, University of Louvain, Brussels, Belgium
    J Clin Invest 121:3932-42. 2011
    ..The KATP channel blocker tolbutamide was consistently ineffective in stimulating insulin secretion; conversely, the KATP channel activator diazoxide ..
  6. ncbi Tolbutamide reduces glioma cell proliferation by increasing connexin43, which promotes the up-regulation of p21 and p27 and subsequent changes in retinoblastoma phosphorylation
    Rosa Sánchez-Alvarez
    Departamento de Bioquimica y Biologia Molecular, INCYL, Universidad de Salamanca, Spain
    Glia 54:125-34. 2006
    Our previous work has shown that tolbutamide increases gap junctional permeability in poorly coupled C6 glioma cells and that this effect is similar and additive to that found with dbcAMP, a well-known activator of gap junctional ..
  7. ncbi Effects of pomegranate juice on human cytochrome P450 2C9 and tolbutamide pharmacokinetics in rats
    Masashi Nagata
    School of Pharmaceutical Sciences, Kyushu University of Health and Welfare, 1714 1 Yoshino, Nobeoka City, Miyazaki, 882 8508, Japan
    Drug Metab Dispos 35:302-5. 2007
    ..In addition, we investigated the effect of pomegranate juice on the pharmacokinetics of tolbutamide (substrate for CYP2C9) in rats...
  8. ncbi Chronic exposure to tolbutamide and glibenclamide impairs insulin secretion but not transcription of K(ATP) channel components
    Andrew J Ball
    School of Biomedical Sciences, University of Ulster, Coleraine BT52 1SA, Northern Ireland, UK
    Pharmacol Res 50:41-6. 2004
    ..BRIN-BD11 cells were used to examine effects of chronic 72-144 h exposure to the sulphonylureas tolbutamide and glibenclamide on insulin release, cellular insulin content, and mRNA levels of the Kir6...
  9. pmc Tolbutamide stimulation of pancreatic beta-cells involves both cell recruitment and increase in the individual Ca(2+) response
    F C Jonkers
    , University of Louvain Faculty of Medicine, Brussels, Belgium
    Br J Pharmacol 133:575-85. 2001
    ..In 4 mM glucose, the threshold concentration of tolbutamide inducing a [Ca(2+)](i) rise was variable (5 - 50 microM)...
  10. ncbi Dual mechanism of the potentiation by glucose of insulin secretion induced by arginine and tolbutamide in mouse islets
    Nobuyoshi Ishiyama
    Unité d Endocrinologie et Métabolisme, University of Louvain Faculty of Medicine, Brussels, Belgium
    Am J Physiol Endocrinol Metab 290:E540-9. 2006
    ..glucose (G3-G15, respectively) and pulse or stepwise stimulation with 1-10 mmol/l arginine or 5-250 micromol/l tolbutamide. In G3, arginine induced small increases in [Ca(2+)](i) but no IS...
  11. ncbi No major difference in inhibitory susceptibility between CYP2C9.1 and CYP2C9.3
    Tadaaki Hanatani
    Clinical Evaluation of Medicines and Therapeutics, Graduate School of Pharmaceutical Sciences, Osaka University, 1 6 Yamada oka, Suita, Osaka 565 0871, Japan
    Eur J Clin Pharmacol 59:233-5. 2003
    ..CYP2C9 is a polymorphic enzyme, and CYP2C9*3 is associated with decreased metabolic activity. In addition to the impaired metabolism, we investigated whether the CYP2C9*3 exhibited altered inhibitory susceptibility compared with CYP2C9*1...
  12. pmc Enhanced PIP3 signaling in POMC neurons causes KATP channel activation and leads to diet-sensitive obesity
    Leona Plum
    Department of Mouse Genetics and Metabolism, Institute for Genetics, University of Cologne and Center of Molecular Medicine Cologne CMMC, Cologne, Germany
    J Clin Invest 116:1886-901. 2006
    ..electrical activity in PPKO POMC neurons, but application of the PI3K inhibitor LY294002 and the KATP blocker tolbutamide restored electrical activity and leptin-evoked firing of POMC neurons in these mice...
  13. ncbi Differences between the tolbutamide-boosted and the insulin-modified minimal model protocols
    M F Saad
    Department of Medicine, University of Southern California Medical School, Los Angeles 90033, USA
    Diabetes 46:1167-71. 1997
    ..sampled intravenous glucose tolerance test (FSIGTT) with minimal model analysis (MINMOD) was compared with the tolbutamide protocol and the glucose clamp in 35 nondiabetic subjects (age 38 +/- 2 years [mean +/- SE], BMI 27.2 +/- 0...
  14. ncbi Catalytic activities of human cytochrome P450 2C9*1, 2C9*3 and 2C9*13
    Y Guo
    College of Life Science, Jilin University, Changchun, China
    Xenobiotica 35:853-61. 2005
    ..CYP2C9*13 exhibited an 11-fold increase in Km but no change in Vmax with tolbutamide as the substrate, a five-fold increase in Km and an 88.8% reduction in Vmax with diclofenac...
  15. ncbi Functional characterization of novel allelic variants of CYP2C9 recently discovered in southeast Asians
    Tracy C DeLozier
    Human Metabolism Section, Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, NIH, Research Triangle Park, NC 27709, USA
    J Pharmacol Exp Ther 315:1085-90. 2005
    ..CYP2C9.14 and CYP2C9.16 exhibited 80 to 90% lower catalytic activity toward tolbutamide at two substrate concentrations compared with wild-type CYP2C9.1. Kinetic analysis confirmed that CYP2C9...
  16. ncbi Effect of albumin on phenytoin and tolbutamide metabolism in human liver microsomes: an impact more than protein binding
    Cuyue Tang
    Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486 0004, USA
    Drug Metab Dispos 30:648-54. 2002
    The cytochrome P450 (P450)-dependent conversion of phenytoin (PHT) to p-hydroxy phenytoin (pHPPH), and tolbutamide (TLB) to 4-hydroxy tolbutamide (hydroxy-TLB), in human liver microsomes was studied in the presence of increasing ..
  17. pmc Hybrid assemblies of ATP-sensitive K+ channels determine their muscle-type-dependent biophysical and pharmacological properties
    Domenico Tricarico
    Department of Pharmacobiology, Faculty of Pharmacy, University of Bari, via Orabona no 4, 70120 Bari, Italy
    Proc Natl Acad Sci U S A 103:1118-23. 2006
    ..showed that the channel response to the SUR1 agonist diazoxide, SUR2A/B agonist cromakalim, SUR1 antagonist tolbutamide, and the SUR1/SUR2A/B-antagonist glibenclamide matched the SURs expression pattern...
  18. ncbi Metabolite formation kinetics and intrinsic clearance of phenacetin, tolbutamide, alprazolam, and midazolam in adenoviral cytochrome P450-transfected HepG2 cells and comparison with hepatocytes and in vivo
    M Teresa Donato
    Unidad de Hepatologia Experimental, Centro de Investigacion, Hospital La Fe, Avenida Campanar 21, Valencia, Spain
    Drug Metab Dispos 38:1449-55. 2010
    ..The kinetics of metabolite formation from phenacetin, tolbutamide, and alprazolam and midazolam, selected as substrates probes for CYP1A2, CYP2C9, and CYP3A4, respectively, were ..
  19. ncbi Impact of CYP2C9 and CYP2C19 polymorphisms on tolbutamide kinetics and the insulin and glucose response in healthy volunteers
    Julia Kirchheiner
    Institute of Clinical Pharmacology, University Medical Center Charite, Humboldt University, Berlin, Germany
    Pharmacogenetics 12:101-9. 2002
    b>Tolbutamide is known to be metabolized by cytochrome P450 2C9 (CYP2C9), and the effects of the CYP2C9 amino acid polymorphisms *2 (Arg144Cys) and *3 (Ile359Leu) could be important for drug treatment with tolbutamide and for use of ..
  20. ncbi CYP2C9 polymorphism: impact on tolbutamide pharmacokinetics and response
    John Miners
    Department of Clinical Pharmacology, Flinders Medical Centre and Flinders University, Bedford Park, Adelaide, SA, Australia
    Pharmacogenetics 12:91-2. 2002
  21. ncbi Cell specificity of the cytoplasmic Ca2+ response to tolbutamide is impaired in beta-cells from hyperglycemic mice
    Natalia Gustavsson
    Department of Integrative Medical Biology, Section for Histology and Cell Biology, Umea University, Umeå S 901 87, Sweden
    J Endocrinol 190:461-70. 2006
    ..We have now used tolbutamide and arginine to test if the cell specificity exists also for the response to non-nutrient stimulation of beta-..
  22. ncbi Acute insulin responses to calcium and tolbutamide do not differentiate focal from diffuse congenital hyperinsulinism
    Irina Giurgea
    Department of Pediatrics, Hopital Necker Enfants Malades, 75743 Paris, France
    J Clin Endocrinol Metab 89:925-9. 2004
    ..v. injections of glucose, calcium, and tolbutamide have been reported as potential means to distinguish between these histological forms...
  23. ncbi Glucose inhibits glucagon secretion by a direct effect on mouse pancreatic alpha cells
    E Vieira
    Department of Medical Cell Biology, Uppsala University, BMC Box 571, SE 751 23, Uppsala, Sweden
    Diabetologia 50:370-9. 2007
    ..The mechanisms by which glucose regulates glucagon release are poorly understood. The present study aimed to clarify the direct effects of glucose on the glucagon-releasing alpha cells and those effects mediated by paracrine islet factors...
  24. ncbi Discovery of new potentially defective alleles of human CYP2C9
    Joyce Blaisdell
    Laboratory of Pharmacology and Chemistry, Human Metabolism Section, National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina, USA, DNA
    Pharmacogenetics 14:527-37. 2004
    ..exhibiting a three-fold increase in the Km and more than a two-fold decrease in the intrinsic clearance for tolbutamide. Examination of the crystal structure of human CYP2C9 reveals that R335 is located in the turn between the J ..
  25. ncbi Ginkgo biloba extract modifies hypoglycemic action of tolbutamide via hepatic cytochrome P450 mediated mechanism in aged rats
    Tomomi Sugiyama
    National Institute of Health and Nutrition, 1 23 1 Toyama, Shinjuku, Tokyo 162 8636, Japan
    Life Sci 75:1113-22. 2004
    We examined hepatic cytochrome P450 (CYP)-mediated interactions between Ginkgo biloba extract (GBE) and tolbutamide, an oral anti-diabetic agent, in aged and young rats...
  26. ncbi Somatostatin release, electrical activity, membrane currents and exocytosis in human pancreatic delta cells
    M Braun
    Oxford Centre for Diabetes, Endocrinology and Metabolism, Churchill Hospital, Oxford OX37 LJ, UK
    Diabetologia 52:1566-78. 2009
    ..The aim of this study was to characterise electrical activity, ion channels, exocytosis and somatostatin release in human delta cells/pancreatic islets...
  27. ncbi Cytochrome P450 2C9 phenotyping using low-dose tolbutamide
    Alexander Jetter
    Department of Pharmacology, Clinical Pharmacology, University of Cologne, Gleueler Strasse 24, 50931 Cologne, Germany
    Eur J Clin Pharmacol 60:165-71. 2004
    The hypoglycaemic drug tolbutamide is used for assessment of CYP2C9 activity in vivo...
  28. ncbi Tolbutamide, flurbiprofen, and losartan as probes of CYP2C9 activity in humans
    Craig R Lee
    Divisions of Pharmacotherapy, CB 7360, Beard Hall, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599 7360, USA
    J Clin Pharmacol 43:84-91. 2003
    ..Single oral doses of tolbutamide, flurbiprofen, and losartan were administered in a randomized, crossover design...
  29. ncbi Tolbutamide and phenytoin hydroxylations by cDNA-expressed human liver cytochrome P4502C9
    M E Veronese
    Department of Clinical Pharmacology, School of Medicine, Flinders University of South Australia, Adelaide
    Biochem Biophys Res Commun 175:1112-8. 1991
    ..The expressed enzyme catalysed the methylhydroxylation of tolbutamide with an apparent Km of 131.7 microM, similar to that observed in human liver microsomes...
  30. pmc Alternative sulfonylurea receptor expression defines metabolic sensitivity of K-ATP channels in dopaminergic midbrain neurons
    B Liss
    Institute for Neural Signal Transduction, Centre for Molecular Neurobiology, Martinistrasse 52, 20246 Hamburg, Germany
    EMBO J 18:833-46. 1999
    ....
  31. ncbi K(ATP)-channels and glucose-regulated glucagon secretion
    Patrik Rorsman
    Oxford Centre for Diabetes, Endocrinology and Metabolism, University of Oxford, Churchill Hospital, Oxford OX3 7LJ, UK
    Trends Endocrinol Metab 19:277-84. 2008
    ..Here we consider the possible mechanisms involved with a focus on ATP-regulated K(+)-channels and changes in alpha-cell membrane potential...
  32. ncbi Glucokinase is a critical regulator of ventromedial hypothalamic neuronal glucosensing
    Ling Kang
    Department of Neurology and Neuroscience, New Jersey Medical School, Newark, USA
    Diabetes 55:412-20. 2006
    ..98 mmol/l) and a decrease in glucose-inhibited neurons (IC(50) = 0.025 micromol/l) held at 0.5 mmol/l glucose. Together, these data support a critical role for glucokinase in neuronal glucosensing...
  33. pmc Dominantly inherited hyperinsulinism caused by a mutation in the sulfonylurea receptor type 1
    H Huopio
    Department of Pediatrics, Kuopio University Hospital, Kuopio, Finland
    J Clin Invest 106:897-906. 2000
    ..In conclusion, we describe the first dominantly inherited SUR1 mutation that causes CHI in early life and predisposes to later insulin deficiency...
  34. ncbi Leptin fully suppresses acetylcholine-induced insulin secretion and is reversed by tolbutamide in isolated perfused chicken pancreas
    Y Benomar
    Station de Recherches Avicoles, INRA, F37380 Nouzilly, France
    Horm Metab Res 35:81-5. 2003
    ..insulin secretion induced by acetylcholine stimulation without any change in volume outflow rate, iii) tolbutamide (100 micro M) introduced 10 min after leptin and perfused for 10 min fully reversed the suppressive effect of ..
  35. ncbi Effects of Ginkgo biloba extract on pharmacokinetics and pharmacodynamics of tolbutamide and midazolam in healthy volunteers
    Shinya Uchida
    Department of Pharmacokinetics, Center of Excellence Program in the 21st Century, School of Pharmaceutical Sciences, University of Shizuoka, 52 1 Yada, Suruga ku, Shizuoka, 422 8526, Japan
    J Clin Pharmacol 46:1290-8. 2006
    ..CYP2C9 probe (tolbutamide, 125 mg) and CYP3A4 probe (midazolam, 8 mg) were orally administered to 10 male healthy volunteers before and ..
  36. ncbi Effects of tolbutamide and N-benzoyl-D-phenylalanine (NBDP) on the regulation of [Ca2+]i oscillations in mouse pancreatic islets
    S Lenzen
    Institute of Clinical Biochemistry, Hannover Medical School, D-30623, Hannover, Germany
    Biochem Pharmacol 62:923-8. 2001
    The sulfonylurea derivative, tolbutamide, and the phenylalanine derivative, N-benzoyl-D-phenylalanine (NBDP), both of which stimulate insulin secretion through interaction with the sulfonylurea receptor (SUR1), were studied for their ..
  37. ncbi CYP2C76, a novel cytochrome P450 in cynomolgus monkey, is a major CYP2C in liver, metabolizing tolbutamide and testosterone
    Yasuhiro Uno
    Laboratory of Translational Research, Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita 14 Nishi 6, Kita ku, Sapporo, 060 0812, Japan
    Mol Pharmacol 70:477-86. 2006
    ..These results suggest that CYP2C76 contributes to overall drug-metabolizing activity in the monkey liver and might account for species difference occasionally seen in drug metabolism between monkeys and humans...
  38. ncbi Characterization of the physiological spaces and distribution of tolbutamide in the perfused rat pancreas
    Kent John Fanning
    Department of Medicine, Princess Alexandra Hospital, University of Queensland, Woolloongabba, Queensland 4102, Australia
    Pharm Res 24:512-20. 2007
    ..To set up and validate a viable perfused rat pancreas model suitable for pharmacokinetic studies...
  39. ncbi Influence of the preparation method on the physicochemical properties of tolbutamide/cyclodextrin binary systems
    F Veiga
    Laboratorio de Tecnologia Farmaceutica, Faculdade de Farmacia, Universidade de Coimbra, Portugal
    Drug Dev Ind Pharm 27:523-32. 2001
    b>Tolbutamide (TBM) was found to form an inclusion complex with beta cyclodextrin (beta-CD) in solution and in solid state...
  40. ncbi Identification of mutant Asp251Gly/Gln307His of cytochrome P450 BM3 for the generation of metabolites of diclofenac, ibuprofen and tolbutamide
    Georgia E Tsotsou
    Department of Life Sciences and Systems Biology, University of Torino via Accademia Albertina 13, 10123, Torino, Italy
    Chemistry 18:3582-8. 2012
    ..The double mutant Asp251Gly/Gln307His (A2) with activities towards diclofenac, ibuprofen and tolbutamide was identified by screening with the alkali method...
  41. pmc Membrane potential-dependent inactivation of voltage-gated ion channels in alpha-cells inhibits glucagon secretion from human islets
    Reshma Ramracheya
    Oxford Centre for Diabetes Endocrinology and Metabolism, University of Oxford, Churchill Hospital, Oxford, UK
    Diabetes 59:2198-208. 2010
    ..To document the properties of the voltage-gated ion channels in human pancreatic alpha-cells and their role in glucagon release...
  42. ncbi Modeling the in vitro intrinsic clearance of the slowly metabolized compound tolbutamide determined in sandwich-cultured rat hepatocytes
    Nicoline Treijtel
    Institute for Risk Assessment Sciences, Utrecht University, Yalelaan 2, P O Box 80176, 3508 TD Utrecht, The Netherlands
    Drug Metab Dispos 32:884-91. 2004
    ..Substrate depletion of tolbutamide and the formation of its metabolites hydroxytolbutamide and carboxytolbutamide were measured in the medium and ..
  43. pmc Interaction of tolbutamide and cytosolic nucleotides in controlling the ATP-sensitive K+ channel in mouse beta-cells
    C Schwanstecher
    Institute of Pharmacology and Toxicology, , Germany
    Br J Pharmacol 111:302-10. 1994
    ..In the presence of Mg2+, the KATP-channels were activated by dADP, GTP, GDP and UDP. 4. Tolbutamide inhibited the KATP-channels not only in the presence but also in the prolonged absence of Mg2+...
  44. ncbi Tolbutamide uptake via pH- and membrane-potential-dependent transport mechanism in mouse brain capillary endothelial cell line
    Noriko Koyabu
    Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Drug Metab Pharmacokinet 19:270-9. 2004
    The purpose of this study was to investigate the transport mechanism of tolbutamide across the blood-brain barrier (BBB) using MBEC4 cells as an in vitro BBB model.
  45. ncbi Decreased tolbutamide-stimulated insulin secretion in healthy subjects with sequence variants in the high-affinity sulfonylurea receptor gene
    T Hansen
    Steno Diabetes Center and Hagedorn Research Institute, Glostrup University Hospital, Copenhagen, Denmark
    Diabetes 47:598-605. 1998
    ..with NIDDM and for a possible influence on insulin and C-peptide secretion after intravenous glucose and tolbutamide loads in a random sample of unrelated, healthy, young Danish Caucasians...
  46. ncbi Relationship of P450 2C9 genetic polymorphisms in Chinese and the pharmacokinetics of tolbutamide
    K Chen
    Marin Drug and Food Institute, Ocean University of China, Qingdao, China
    J Clin Pharm Ther 30:241-9. 2005
    To study the relationship between P450 2C9 genetic polymorphisms and the pharmacokinetics of tolbutamide in Chinese subjects.
  47. ncbi The tolbutamide site of SUR1 and a mechanism for its functional coupling to K(ATP) channel closure
    A P Babenko
    Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA
    FEBS Lett 459:367-76. 1999
    Micromolar concentrations of tolbutamide will inhibit (SUR1/K(IR)6. 2)(4) channels in pancreatic beta-cells, but not (SUR2A/K(IR)6.2)(4) channels in cardiomyocytes...
  48. ncbi Interaction of drugs and Chinese herbs: pharmacokinetic changes of tolbutamide and diazepam caused by extract of Angelica dahurica
    K Ishihara
    Faculty of Pharmaceutical Sciences, Chiba University, Japan
    J Pharm Pharmacol 52:1023-9. 2000
    ..In addition, treatment with the extract inhibited the metabolism of tolbutamide, nifedipine and bufuralol...
  49. ncbi BPDZ 154 activates adenosine 5'-triphosphate-sensitive potassium channels: in vitro studies using rodent insulin-secreting cells and islets isolated from patients with hyperinsulinism
    Karen E Cosgrove
    Department of Biomedical Science, Institute of Molecular Physiology, University of Sheffield, Western Bank, Sheffield S10 2TN, UK
    J Clin Endocrinol Metab 87:4860-8. 2002
    ..insulin secretion from isolated perifused islets and the secretion of insulin induced by glucose and tolbutamide. These effects were mediated by the activation of ATP-sensitive potassium channels because BPDZ 154 induced a ..
  50. ncbi The cytoplasmic C-terminus of the sulfonylurea receptor is important for KATP channel function but is not key for complex assembly or trafficking
    Jonathan P Giblin
    Centre for Clinical Pharmacology, Department of Medicine, University College London, The Rayne Institute, UK
    Eur J Biochem 269:5303-13. 2002
    ..recordings indicate that ATP sensitivity is normal but the response of the mutant channel complexes to tolbutamide, MgADP and diazoxide is disturbed...
  51. ncbi The peripheral antinociceptive effect of resveratrol is associated with activation of potassium channels
    V Granados-Soto
    Departamento de Farmacobiologia, Centro de Investigacion y de Estudios Avanzados del Instituto Politecnico Nacional, Mexico, DF, Mexico
    Neuropharmacology 43:917-23. 2002
    ..Local pretreatment of the injured paw with glibenclamide, tolbutamide or glipizide (ATP-sensitive K(+) channel inhibitors) did not modify resveratrol-induced antinociception...
  52. ncbi Nateglinide, a non-sulfonylurea rapid insulin secretagogue, increases pancreatic islet blood flow in rats
    Masanori Iwase
    Department of Medicine and Clinical Science, Graduate School of Medical Sciences, Kyushu University, Maidashi 3 1 1, Higashi ku, Fukuoka 812 8582, Japan
    Eur J Pharmacol 518:243-50. 2005
    ..nateglinide with glucose acutely increased islet blood flow to levels greater than those after glucose alone or tolbutamide with glucose in conscious Sprague-Dawley rats (percent increase at 10 min after oral administration; ..
  53. ncbi Glucose- and interleukin-1beta-induced beta-cell apoptosis requires Ca2+ influx and extracellular signal-regulated kinase (ERK) 1/2 activation and is prevented by a sulfonylurea receptor 1/inwardly rectifying K+ channel 6.2 (SUR/Kir6.2) selective potassiu
    Kathrin Maedler
    Division of Endocrinology and Diabetes, Department of Medicine, University Hospital, CH 8091 Zurich, Switzerland
    Diabetes 53:1706-13. 2004
    ..1 and 33.3 mmol/l glucose, 2 ng/ml IL-1beta, or 10 and 100 micromol/l of the sulfonylurea tolbutamide induced beta-cell apoptosis and impaired glucose-stimulated insulin secretion...
  54. ncbi A genetic and physiological study of impaired glucose homeostasis control in C57BL/6J mice
    A A Toye
    Medical Research Council, Harwell, Didcot, Oxfordshire, UK
    Diabetologia 48:675-86. 2005
    ..C57BL/6J mice exhibit impaired glucose tolerance. The aims of this study were to map the genetic loci underlying this phenotype, to further characterise the physiological defects and to identify candidate genes...
  55. ncbi Similarities of K+ATP channel expression and Ca2+ changes in pancreatic beta cells and hypothalamic neurons
    Paul E Squires
    Molecular Physiology, Department of Biological Sciences, University of Warwick, Coventry, United Kingdom
    Pancreas 30:227-32. 2005
    ..functional data suggesting that both pancreatic and a subpopulation of hypothalamic cells exhibit glucose- and tolbutamide-evoked changes in cytosolic calcium and consider some clinical implications of different glucose sensors using ..
  56. ncbi A novel simple method for the investigation of drug binding to the K(ATP) channel sulfonylurea receptor
    Ellina A Mikhailova
    Nuffield Department of Clinical Laboratory Sciences, John Radcliffe Hospital, Headington, Oxford, UK
    Anal Biochem 307:383-5. 2002
  57. pmc Interplay of Ca2+ and cAMP signaling in the insulin-secreting MIN6 beta-cell line
    Luis R Landa
    Department of Medicine, The University of Chicago, Chicago, Illinois 60637, USA
    J Biol Chem 280:31294-302. 2005
    ..We report that depolarization with high external K+, tolbutamide, or glucose caused a rapid increase in cAMP that was dependent on extracellular Ca2+ and inhibited by ..
  58. ncbi Functional coupling between sulfonylurea receptor type 1 and a nonselective cation channel in reactive astrocytes from adult rat brain
    Mingkui Chen
    Department of Neurosurgery, University of Maryland at Baltimore, Baltimore, Maryland 21201, USA
    J Neurosci 23:8568-77. 2003
    ..observed in patch-clamp experiments using Cs+ as the charge carrier: (1) the sulfonylureas, glibenclamide and tolbutamide, inhibited NCCa-ATP channels with EC50 values of 48 nm and 16...
  59. ncbi Glucose-sensing in glucagon-like peptide-1-secreting cells
    Frank Reimann
    Department of Clinical Biochemistry, University of Cambridge, Addenbrooke s Hospital, Hills Road, Cambridge, U K
    Diabetes 51:2757-63. 2002
    ..Action potentials were also triggered by tolbutamide (500 micro mol/l) and were suppressed by diazoxide (340 micro mol/l) or the metabolic inhibitor azide (3 mmol/l)..
  60. pmc Glucose-dependent regulation of rhythmic action potential firing in pancreatic beta-cells by K(ATP)-channel modulation
    T Kanno
    Department of Physiology, Hirosaki University School of Medicine, Japan
    J Physiol 545:501-7. 2002
    ..Application of the K(ATP)-channel blocker tolbutamide produced uninterrupted action potential firing and reduced I(K,slow) by approximately 50 %...
  61. ncbi Taurine block of cloned ATP-sensitive K+ channels with different sulfonylurea receptor subunits expressed in Xenopus laevis oocytes
    Jeong Geun Lim
    Department of Neurology, Keimyung University School of Medicine, 194 Dongsan dong, Jung Gu, Daegu 700 712, South Korea
    Biochem Pharmacol 68:901-10. 2004
    ..The high-affinity binding of tolbutamide or gliclazide on SUR was not modified by taurine...
  62. ncbi Novel and established potassium channel openers stimulate hair growth in vitro: implications for their modes of action in hair follicles
    Gareth C Davies
    Department of Biomedical Sciences, University of Bradford, Bradford, West Yorkshire, UK
    J Invest Dermatol 124:686-94. 2005
    ..Therefore, the in vitro effects of established potassium channel openers and inhibitors (tolbutamide and glibenclamide), plus a novel, selective Kir6...
  63. ncbi Two distinct effects of cGMP on cytosolic Ca2+ concentration of rat pancreatic beta-cells
    Tomohisa Ishikawa
    Department of Pharmacology, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan
    J Pharmacol Sci 91:41-6. 2003
    ....
  64. ncbi Diabetogenic effect of cyclosporin A is mediated by interference with mitochondrial function of pancreatic B-cells
    M Dufer
    Department of Pharmacology, Institute of Pharmacy, University of Tubingen, Tubingen, Germany
    Mol Pharmacol 60:873-9. 2001
    ..Interestingly, the observed reduction in [Ca(2+)](c) could be counteracted by the K(+)(ATP) channel blocker tolbutamide, indicating that the stimulus-secretion coupling was interrupted before the closure of K(+)(ATP) channels...
  65. ncbi Inhibition of glucose-induced electrical activity in rat pancreatic beta-cells by DCPIB, a selective inhibitor of volume-sensitive anion currents
    Leonard Best
    Department of Medicine, University of Manchester, Manchester, M13 9WL, UK
    Eur J Pharmacol 489:13-9. 2004
    ..a net increase in beta-cell input conductance and evoked an outward current that was sensitive to inhibition by tolbutamide, suggesting KATP channel activation...
  66. pmc Analysis of the differential modulation of sulphonylurea block of beta-cell and cardiac ATP-sensitive K+ (K(ATP)) channels by Mg-nucleotides
    Frank Reimann
    University Laboratory of Physiology, Parks Road, Oxford OX1 3PT, UK
    J Physiol 547:159-68. 2003
    ..This effect was not specific for meglitinide, as tolbutamide was also unable to prevent MgADP activation of Kir6.2/SUR128 currents...
  67. ncbi Insulin resistance and impaired insulin secretion in prenatally androgenized male rhesus monkeys
    Cristin M Bruns
    Department of Medicine, University of Wisconsin, Madison, Wisconsin 53792, USA
    J Clin Endocrinol Metab 89:6218-23. 2004
    ..52, 711.89); P < 0.02]. PA males do not exhibit elevated androgens during adulthood, suggesting that insulin resistance and impaired pancreatic beta-cell function may result from fetal reprogramming of key metabolic tissues...
  68. ncbi How does glucose evoke electrical activity in the pancreatic beta-cell?
    L Best
    Department of Medicine, University of Manchester, Oxford Road, Manchester, M13 9WL, UK
    Diabetes Metab 28:3S18-24; discussion 3S108-12. 2002
    ..5 mM tolbutamide. Glucose-induced electrical and secretory activity were, however, sensitive to inhibition by the anion channel ..
  69. ncbi [3T3-L1 adipocytes reduces Kir6.2 channel expression in MIN6 insulin-secreting cells in vitro]
    Yu Feng Zhao
    Department of Physiology, Fourth Military Medical University, Xi an 710032, China
    Sheng Li Xue Bao 56:253-7. 2004
    ..MIN6 cells cocultured with 3T3-L1 adipocytes lost the ability to increase [Ca(2+)](i) when stimulated by tolbutamide (0.1 mmol/L), a highly selective KATP channel closer...
  70. ncbi Both triggering and amplifying pathways contribute to fuel-induced insulin secretion in the absence of sulfonylurea receptor-1 in pancreatic beta-cells
    Myriam Nenquin
    Unité d Endocrinologie et Métabolisme, University of Louvain Faculty of Medicine UCL 55 30, Ave Hippocrate 55, B 1200 Brussels, Belgium
    J Biol Chem 279:32316-24. 2004
    ..Unlike controls, Sur1KO islets were insensitive to diazoxide and tolbutamide, which rules out effects of either drug at sites other than K(ATP) channels...
  71. ncbi Preoperative evaluation of infants with focal or diffuse congenital hyperinsulinism by intravenous acute insulin response tests and selective pancreatic arterial calcium stimulation
    Charles A Stanley
    Division of Endocrinology, The Children s Hospital of Philadelphia, Pennsylvania 19104, USA
    J Clin Endocrinol Metab 89:288-96. 2004
    ..Positive AIR calcium occurred in 17 of 30 focal and 10 of 13 diffuse cases (P < 0.04). Positive AIR tolbutamide occurred in 27 of 30 focal vs. seven of 13 diffuse cases (P < 0...
  72. ncbi Possible involvement of potassium channels in peripheral antinociception induced by metamizol: lack of participation of ATP-sensitive K+ channels
    Mario I Ortiz
    Seccion Externa de Farmacologia, Centro de Investigacion y de Estudios Avanzados del Instituto Politecnico Nacional, Mexico, D F, Mexico
    Pharmacol Biochem Behav 74:465-70. 2003
    ..4-aminopyridine and tetraethylammonium (voltage-dependent K+ channel inhibitors), but not glibenclamide or tolbutamide (ATP-sensitive K+ channel inhibitors), dose-dependently prevented metamizol-induced antinociception...
  73. ncbi Study of the involvement of K+ channels in the peripheral antinociception of the kappa-opioid receptor agonist bremazocine
    Luiz H Amarante
    Department of Pharmacology, Institute of Biological Sciences, Universidade Federal de Minas Gerais UFMG, Av Antonio Carlos 6627, Belo Horizonte MG, 31 270 100, Brazil
    Eur J Pharmacol 494:155-60. 2004
    ..Prior treatment with the ATP-sensitive K(+) channel blockers glibenclamide (40, 80 and 160 microg) and tolbutamide (40, 80 and 160 microg) did not antagonise the antinociceptive effect of bremazocine (50 microg)...
  74. ncbi Co-ordinated Ca(2+)-signalling within pancreatic islets: does beta-cell entrainment require a secreted messenger
    P E Squires
    Molecular Physiology, Department of Biological Sciences, University of Warwick, Coventry CV4 7AL, UK
    Cell Calcium 31:209-19. 2002
    ..b>Tolbutamide evoked a concentration-dependent recruitment of active cells within cell clusters, both in terms of numbers of ..
  75. pmc Mg(2+)-dependent inhibition of KATP by sulphonylureas in CRI-G1 insulin-secreting cells
    K Lee
    Department of Pharmacology, University of Cambridge
    Br J Pharmacol 111:632-40. 1994
    1 Patch-clamp recording techniques were used to examine the effects of tolbutamide, glibenclamide, meglitinide and thiopentone on KATP in CRI-GI insulin-secreting cells in the presence and absence of Mg2+...
  76. pmc Loss of annexin A7 leads to alterations in frequency-induced shortening of isolated murine cardiomyocytes
    C Herr
    Institute of Biochemistry I, University of Cologne, 50931 Cologne, Germany
    Mol Cell Biol 21:4119-28. 2001
    ..This suggests a function for annexin A7 in electromechanical coupling, probably through Ca(2+) homoeostasis...
  77. ncbi Inhibition of protein synthesis sequentially impairs distinct steps of stimulus-secretion coupling in pancreatic beta cells
    M J Garcia-Barrado
    , University of Louvain Faculty of Medicine, B-1200 Brussels, Belgium
    Endocrinology 142:299-307. 2001
    ..After long (18-20 h) CHX-treatment, the strong (80%) inhibition of glucose-, tolbutamide-, and K(+)-induced insulin secretion was not due to lower insulin stores, to any marked impairment of glucose ..
  78. pmc Mitochondrial priming modifies Ca2+ oscillations and insulin secretion in pancreatic islets
    E K Ainscow
    Department of Biochemistry, School of Medical Sciences, University Walk, University of Bristol, Bristol BS8 1TD
    Biochem J 353:175-80. 2001
    ..Ca(2+)](m) increases provoked by KCl or tolbutamide evoked an immediate increase in cytosolic and mitochondrial free ATP concentration ([ATP](c) and [ATP](m) ..
  79. pmc Sulfonylurea receptors type 1 and 2A randomly assemble to form heteromeric KATP channels of mixed subunit composition
    Kim W Chan
    Department of Physiology and Biophysics, Case Western Reserve University, Cleveland, OH 44106, USA
    J Gen Physiol 131:43-58. 2008
    ..Further pharmacological characterization confirmed coassembly of not only S1-WT and S2-ND, but also of coexpressed free SUR1, SUR2A, and Kir6.2 into functional heteromeric channels...
  80. ncbi An ATP-binding mutation (G334D) in KCNJ11 is associated with a sulfonylurea-insensitive form of developmental delay, epilepsy, and neonatal diabetes
    Ricard Masia
    Department of Cell Biology and Physiology, Washington University School of Medicine, 660 South Euclid Avenue, St Louis, MO 63110, USA
    Diabetes 56:328-36. 2007
    ....
  81. ncbi Iptakalim, a vascular ATP-sensitive potassium (KATP) channel opener, closes rat pancreatic beta-cell KATP channels and increases insulin release
    Naoko Misaki
    Department of Physiology, Hirosaki University School of Medicine, Zaifucho, Japan
    J Pharmacol Exp Ther 322:871-8. 2007
    ....
  82. pmc A novel ABCC8 (SUR1)-dependent mechanism of metabolism-excitation uncoupling
    Andrey P Babenko
    Pacific Northwest Research Institute, 720 Broadway, Seattle, WA 98122, USA
    J Biol Chem 283:8778-82. 2008
    ..I uncovered an attenuated tolbutamide inhibition of the hyperstimulated mutant, which is normally sensitive to the drug under non-stimulatory ..
  83. ncbi Defective pancreatic beta-cell glycolytic signaling in hepatocyte nuclear factor-1alpha-deficient mice
    I D Dukes
    Department of Molecular Endocrinology, Glaxo Wellcome Research Institute, Research Triangle Park, North Carolina 27709, USA
    J Biol Chem 273:24457-64. 1998
    ..We conclude that hepatocyte nuclear factor-1alpha diabetes results from defective beta-cell glycolytic signaling, which is potentially correctable using substrates that bypass the defect...
  84. pmc Defective insulin secretion and enhanced insulin action in KATP channel-deficient mice
    T Miki
    Department of Molecular Medicine, Chiba University Graduate School of Medicine, 1 8 1, Inohana, Chuo Ku, Chiba 260, Japan
    Proc Natl Acad Sci U S A 95:10402-6. 1998
    ..2(+/+)), neither glucose at high concentrations nor the sulfonylurea tolbutamide elicits a rise in [Ca2+]i, and no significant insulin secretion in response to either glucose or tolbutamide is ..
  85. ncbi Glucose modulation of ATP-sensitive K-currents in wild-type, homozygous and heterozygous glucokinase knock-out mice
    H Sakura
    University Laboratory of Physiology, Oxford, UK
    Diabetologia 41:654-9. 1998
    ..In contrast, 20 mmol/l ketoisocaproic acid or 0.5 mmol/ l tolbutamide depolarised all three types of beta-cell...
  86. ncbi Insulin secretion from isolated rat islets induced by the novel hypoglycemic agent A-4166, a derivative of D-phenylalanine
    K Tsukuda
    Institute for Adult Diseases, Asahi Life Foundation, Tokyo, Japan
    Horm Metab Res 30:42-9. 1998
    ..8 mmol/l glucose. Both A-4166 and tolbutamide evoke a prompt rise in insulin secretion followed by a sustained gradually decreasing release from perfused ..
  87. ncbi Effects of tolbutamide on vascular ATP-sensitive potassium channels in humans. Comparison with literature data on glibenclamide and glimepiride
    P J Bijlstra
    Department of Internal Medicine, University Hospital Nijmegen, The Netherlands
    Horm Metab Res 28:512-6. 1996
    ..The aim of this study was to determine whether the first generation SU derivative tolbutamide has KATP channel blocking properties in humans...
  88. ncbi Sulfonylurea receptors inhibit the epithelial sodium channel (ENaC) by reducing surface expression
    A A Konstas
    University Laboratory of Physiology, Parks Road, Oxford OX1 3PT, UK
    Pflugers Arch 442:752-61. 2001
    ..Co-expression of SURs did not confer sensitivity of DeltaIami to diazoxide, pinacidil, tolbutamide, or glibenclamide...
  89. ncbi Carriers of an inactivating beta-cell ATP-sensitive K(+) channel mutation have normal glucose tolerance and insulin sensitivity and appropriate insulin secretion
    Hanna Huopio
    Department of Pediatrics, University of Kuopio, Kuopio, Finland
    Diabetes Care 25:101-6. 2002
    ..The aim of our study was to investigate in vivo the glucose homeostasis of heterozygous SUR1 mutation carriers...
  90. ncbi Chemical anoxia activates ATP-sensitive and blocks Ca(2+)-dependent K(+) channels in rat dorsal vagal neurons in situ
    A Kulik
    II Physiologisches Institut, Universitat Gottingen, Germany
    Neuroscience 110:541-54. 2002
    ..The cyanide-evoked persistent outward current was abolished by the K(ATP) channel blocker tolbutamide, but not changed by the SK and BK channel blockers apamin or tetraethylammonium...
  91. ncbi Functional expression of Kir 6.1/SUR1-K(ATP) channels in frog retinal Müller glial cells
    Serguei N Skatchkov
    CMBN, Department of Biochemistry, School of Medicine, Universidad Central del Caribe, Bayamon, Puerto Rico
    Glia 38:256-67. 2002
    ..First, using the patch-clamp technique in whole-cell recordings, tolbutamide, a blocker of K(ATP) channels, blocks nearly 100% of the transient and about 30% of the steady-state inward ..
  92. ncbi Inhibition of glucose-induced electrical activity by 4-hydroxytamoxifen in rat pancreatic beta-cells
    Leonard Best
    Department of Medicine, University of Manchester, Oxford Road, Manchester M13 9WL, UK
    Cell Signal 14:69-73. 2002
    ..This effect was slowly reversible upon withdrawal of the drug. In cells stimulated by tolbutamide (100 microM), application of 4-hydroxytamoxifen again inhibited action-potential generation but failed to ..
  93. ncbi Membrane potential dependent modulations of calcium oscillations in insulin-secreting INS-1 cells
    M Herbst
    Physiologisches Institut II, Universitat Freiburg, Freiburg, Germany
    Cell Calcium 31:115-26. 2002
    ..Glucose, tolbutamide and forskolin elevated [Ca(2+)](i) and induced [Ca(2+)] oscillations...
  94. ncbi Activating mutations in the ABCC8 gene in neonatal diabetes mellitus
    Andrey P Babenko
    Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, USA
    N Engl J Med 355:456-66. 2006
    ..We hypothesized that activating mutations in ABCC8, which encodes SUR1, cause neonatal diabetes...
  95. ncbi Switching from insulin to oral sulfonylureas in patients with diabetes due to Kir6.2 mutations
    Ewan R Pearson
    Institute of Biomedical and Clinical Sciences, Peninsula Medical School, Exeter, United Kingdom
    N Engl J Med 355:467-77. 2006
    ..Diabetes results from impaired insulin secretion caused by a failure of the beta-cell K(ATP) channel to close in response to increased intracellular ATP. Sulfonylureas close the K(ATP) channel by an ATP-independent route...
  96. ncbi Clinical features and insulin regulation in infants with a syndrome of prolonged neonatal hyperinsulinism
    Francis M Hoe
    Divisions of Endocrinology and Neonatology, Department of Pediatrics, Children s Hospital of Philadelphia, 34th Street and Civic Center Boulevard, Philadelphia, PA 19104, USA
    J Pediatr 148:207-12. 2006
    ..To characterize the clinical features and insulin regulation in infants with hypoglycemia due to prolonged neonatal hyperinsulinism...
  97. ncbi The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide
    Y Sunaga
    Department of Cellular and Molecular Medicine, Graduate School of Medicine, Chiba University 1-8-1 Inohana, Chuo-ku, 260-8670, Chiba, Japan
    Eur J Pharmacol 431:119-25. 2001
    ..The insulin responses to glucose, mitiglinide, tolbutamide, and glibenclamide in MIN6 cells after chronic mitiglinide, nateglinide, or repaglinide treatment were ..
  98. ncbi Genetic variability of the SUR1 promoter in relation to beta-cell function and Type II diabetes mellitus
    T Hansen
    Steno Diabetes Center, Gentofte, Denmark
    Diabetologia 44:1330-4. 2001
    ..We aimed to examine the promoter of SUR1 for genetic variation and to determine if variants were associated with Type II (non-insulin-dependent) diabetes mellitus or measures of beta-cell function...
  99. ncbi First phase of glucose-stimulated insulin secretion from MIN 6 cells does not always require extracellular calcium influx
    Makoto Shigeto
    Division of Diabetes and Endocrinology, Department of Medicine, Kawasaki Medical School, Kurashiki, Okayama, Japan
    J Pharmacol Sci 101:293-302. 2006
    ..Both 10 microM diazoxide and 3 microM verapamil completely inhibited tolbutamide- or glibenclamide-induced insulin secretion and suppressed the peak of the first phase of GSIS, but did not ..
  100. ncbi Free radical-mediated tolbutamide desensitization of K+ATP channels in rat pancreatic beta-cells
    N Koriyama
    First Department of Internal Medicine, Faculty of Medicine, Kagoshima University, Japan
    Endocr J 48:337-44. 2001
    To study the effects of hydroxyl radicals on the sensitivity of the ATP-sensitive K+ (K+ ATP) channel to tolbutamide, we used patch clamp and microfluorometric techniques in pancreatic beta-cells isolated from rats...
  101. ncbi K+-ATP-channel-related protein complexes: potential transducers in the regulation of epithelial tight junction permeability
    Thomas Jöns
    Charite Universitatsmedizin Berlin, Centrum für Anatomie, Institut für Integrative Neuroanatomie, Philippstr 12, 10115 Berlin, Germany
    J Cell Sci 119:3087-97. 2006
    ..Variations in the lumenal glucose concentrations and regulators of Kir6.1/SUR2A activity, such as tolbutamide or diazoxide, specifically modulate paracellular permeability...

Research Grants31

  1. Intraocular pressure regulation via ATP-sensitive potassium channels
    Michael F Romero; Fiscal Year: 2013
    ..activation of KATP channels by the pharmacologic openers can be blocked by KATP channel closers, glyburide, and tolbutamide. In addition, treatment with the KATP channel opener diazoxide and the prostaglandin analogue latanoprost ..
  2. Cardiovascular Safety of Combination Therapies for Type 2 Diabetes Mellitus
    James S Floyd; Fiscal Year: 2013
    ..safety of oral diabetes therapies first emerged over forty years ago, when the first-generation sulfonylurea tolbutamide was found to increase the risk of cardiovascular death in the University Group Diabetes Program clinical trial...
  3. Secretagogue induced mechanisms regulating islet electrical activity
    DAVID AARON JACOBSON; Fiscal Year: 2012
    ..I have determined that GLP-1 stimulation of islets causes a significant reduction in glucose and/or tolbutamide (to block KATP) induced (-cell action potential (AP) firing frequency while increasing AP duration, which ..
  4. Cellular Efflux and Metabolism of Protease Inhibitors
    Ashim Mitra; Fiscal Year: 2004
    ..The theoretical model will be first validated using model compound in each class: Tolbutamide - Class-A, Rhodamine 123 - Class-B, Carbamazepine - Class-C, and Cortisol - Class-D...
  5. Garlic Metabolism and Cytochrome P450 Modulation
    Danny Shen; Fiscal Year: 2007
    ..cocktails" of CYP and Pgp probe substrates, including caffeine (1A2), buproprion (2B6), chlorzoxazone (2E1), tolbutamide (2C9), omeprazole (2C19), metoprolol (2D6), midazolam (3A4/5), and digoxin (Pgp), will be administered to a ..
  6. ION DEREGULATION IN VIVO AND INJURY BY ALKYLATING DRUGS
    George Corcoran; Fiscal Year: 1990
    ..Calcium Hypothesis testing will feature agents that up-regulate (alpha-adrenergic drugs, hormones, tolbutamide) and down-regulate Ca2+ (calcium chelators, channel blockers, antagonists), that inhibit specific Ca2+ effects (..
  7. POSTMENOPAUSAL HORMONE THERAPY AND INTRA ABDOMINAL FAT
    Barbara Gower; Fiscal Year: 2000
    ..Insulin sensitivity and glucose tolerance will be assessed with the tolbutamide- modified, frequently-sampled, intravenous, glucose tolerance test and minimal modeling...
  8. CHEMOPREVENTIVE AGENTS AND HUMAN CYTOCHROME P450 IN VIVO
    GRANT WILKINSON; Fiscal Year: 2002
    ..isoforms of interest and the associated in vivo probes will be CYP1A2 (caffeine), CYP2A6 (coumarin), CYP2C9 (tolbutamide), CYP2C19 (mephenytoin), CYP2D6 (debrisoquine), CYP2E1(chlorzoxazone) and CYP3A(midazolam)...
  9. THE EFFECT OF TOLBUTAMIDE ON THE ISCHEMIC MYOCARDIUM
    Stephen Schaffer; Fiscal Year: 1980
    Oral hypoglycemic agents such as tolbutamide have been widely used to treat diabetes-induced hyperglycemia since their clinical introduction 20 years ago...
  10. Long-term follow-up of postobese black and white women
    Barbara Gower; Fiscal Year: 2008
    ..abstract_text> ..
  11. ETHNIC DIFFERENCES IN INSULIN SENSITIVITY
    Barbara Gower; Fiscal Year: 2003
    ..The chronic hyperinsulinemia that results from this defect will ultimately result in peripheral (skeletal muscle) insulin resistance. ..
  12. Reduced Carbohydrate Diet Intervention for PCOS
    Barbara A Gower; Fiscal Year: 2010
    ..the lower GL diet will be more effective in decreasing insulin secretion, increasing insulin sensitivity, decreasing ectopic adipose tissue, decreasing inflammation, and improvin% (<10% saturated fat) saturated fat) ..
  13. Intramuscular lipid and insulin action: ethnic aspects
    Barbara Gower; Fiscal Year: 2006
    ..abstract_text> ..
  14. GABAergic excitation in human hypothalamic hamartoma
    Jie Wu; Fiscal Year: 2007
    ..Knowledge about excitatory GABAA receptor function of HH neurons will also aid selection of superior strategies for pharmaceutical development to prevent and control human gelastic seizures. [unreadable] [unreadable]..
  15. GI MUCOSAL BARRIER IN HEALTH AND SURGICAL DISEASE
    Susan Hagen; Fiscal Year: 2008
    ..abstract_text> ..
  16. INTRA-ABDOMINAL FAT AND RISK OF DISEASE IN ADOLESCENTS
    Michael Goran; Fiscal Year: 2008
    ....
  17. ABCC8/KCNJ11 Mechanisms and Diabetes
    Andrey P Babenko; Fiscal Year: 2010
    ..b>Tolbutamide (~10-4 M) reduced the activity of NDSUR1 channels, indicating that many NDABCC8 cases are treatable with oral ..
  18. ISLET DYSREGULATION IN INFANTS
    Charles Stanley; Fiscal Year: 2008
    ..The results of this research will provide essential information for improving the diagnosis and treatment of HI children and for understanding the basis of insulin regulation in normal humans. ..
  19. Ped Endocrine Career Development in Diabetes Research
    Charles Stanley; Fiscal Year: 2007
    ..The Program is strongly supported by access to a superb range of institutional resources, including the CHOP GCRC and the UPenn DERC. Request is made for 2 Appointee slots in this Program each year. ..
  20. Reactive astrocytes from gliotic capsule
    J Marc Simard; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  21. PATHOPHYSIOLOGY OF NICOTINE IN CEREBRAL BLOOD VESSELS
    J Simard; Fiscal Year: 2004
    ....
  22. Mechanism and Assessment of Hypoxia-Induced Islet Death
    IAN SWEET; Fiscal Year: 2005
    ..abstract_text> ..
  23. A cell-free system for exocytosis in the beta-cell
    SUSANNE STRAUB SHARP; Fiscal Year: 2005
    ..physiological mechanisms such as time-dependent potentiation and biphasic insulin release. The method will also allow the study of some aspects of endocytosis. ..
  24. PHOSPHOINOSITIDE HYDROLYSIS AND BETA CELL SECRETION
    Walter Zawalich; Fiscal Year: 2006
    ..These aims will be accomplished by using sound principles of experimentation and employing isolated islets that retain their in vivo sensitivity to glucose. ..
  25. CEREBROVASCULAR ION CHANNELS IN HYPERTENSION
    J Marc Simard; Fiscal Year: 2007
    ..abstract_text> ..
  26. ANDROGENIZED FEMALE AS A MODEL FOR P0LYCYSTIC OVARIAN SY
    David Abbott; Fiscal Year: 2002
    ..Such results would offer novel insights into the origin and mechanism of PCOS, and would provide a unifying determinant for a multifactorial syndrome. ..
  27. Confocal Microscope for the BIDMC Imaging Core Facility
    Susan Hagen; Fiscal Year: 2006
    ..The instrumentation is requested because no like equipment is currently available to members of the major or minor user groups within the applicant institution or in the Longwood Medical area. [unreadable] [unreadable] [unreadable]..
  28. MOLECULAR BASIS OF A NEW FORM OF HYPERINSULINISM
    CHARLES ALFRED STANLEY; Fiscal Year: 2010
    ....
  29. International Medical Conference of Congenital Hyperinsulinism
    Charles Stanley; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable]..