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. Tricarico D, Mele A, Lundquist A, Desai R, George A, Conte Camerino D. Hybrid assemblies of ATP-sensitive K+ channels determine their muscle-type-dependent biophysical and pharmacological properties. Proc Natl Acad Sci U S A. 2006;103:1118-23 pubmed
    ..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...
  2. Guo Y, Wang Y, Si D, Fawcett P, Zhong D, Zhou H. Catalytic activities of human cytochrome P450 2C9*1, 2C9*3 and 2C9*13. Xenobiotica. 2005;35:853-61 pubmed
    ..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...
  3. Babenko A, Gonzalez G, Bryan J. The tolbutamide site of SUR1 and a mechanism for its functional coupling to K(ATP) channel closure. FEBS Lett. 1999;459:367-76 pubmed
    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...
  4. Henquin J, Nenquin M, Sempoux C, Guiot Y, Bellanne Chantelot C, Otonkoski T, et al. In vitro insulin secretion by pancreatic tissue from infants with diazoxide-resistant congenital hyperinsulinism deviates from model predictions. J Clin Invest. 2011;121:3932-42 pubmed publisher
    ..The KATP channel blocker tolbutamide was consistently ineffective in stimulating insulin secretion; conversely, the KATP channel activator diazoxide ..
  5. Nagata M, Hidaka M, Sekiya H, Kawano Y, Yamasaki K, Okumura M, et al. Effects of pomegranate juice on human cytochrome P450 2C9 and tolbutamide pharmacokinetics in rats. Drug Metab Dispos. 2007;35:302-5 pubmed
    ..In addition, we investigated the effect of pomegranate juice on the pharmacokinetics of tolbutamide (substrate for CYP2C9) in rats...
  6. Ball A, McCluskey J, Flatt P, McClenaghan N. Chronic exposure to tolbutamide and glibenclamide impairs insulin secretion but not transcription of K(ATP) channel components. Pharmacol Res. 2004;50:41-6 pubmed
    ..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...
  7. Zhang C, Katoh M, Shibasaki T, Minami K, Sunaga Y, Takahashi H, et al. The cAMP sensor Epac2 is a direct target of antidiabetic sulfonylurea drugs. Science. 2009;325:607-10 pubmed publisher
    ..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...
  8. Uno Y, Fujino H, Kito G, Kamataki T, Nagata R. CYP2C76, a novel cytochrome P450 in cynomolgus monkey, is a major CYP2C in liver, metabolizing tolbutamide and testosterone. Mol Pharmacol. 2006;70:477-86 pubmed
    ..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. ..
  9. Cheng Xue R, Gómez Ruiz A, Antoine N, Noël L, Chae H, Ravier M, et al. Tolbutamide controls glucagon release from mouse islets differently than glucose: involvement of K(ATP) channels from both ?-cells and ?-cells. Diabetes. 2013;62:1612-22 pubmed publisher
    ..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)...

More Information


  1. Donato M, Hallifax D, Picazo L, Castell J, Houston J, Gomez Lechon M, et al. 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. Drug Metab Dispos. 2010;38:1449-55 pubmed publisher
    ..The kinetics of metabolite formation from phenacetin, tolbutamide, and alprazolam and midazolam, selected as substrates probes for CYP1A2, CYP2C9, and CYP3A4, respectively, were ..
  2. Rorsman P, Salehi S, Abdulkader F, Braun M, MacDonald P. K(ATP)-channels and glucose-regulated glucagon secretion. Trends Endocrinol Metab. 2008;19:277-84 pubmed publisher
    ..Here we consider the possible mechanisms involved with a focus on ATP-regulated K(+)-channels and changes in alpha-cell membrane potential. ..
  3. Gustavsson N, Larsson Nyrén G, Lindstrom P. Cell specificity of the cytoplasmic Ca2+ response to tolbutamide is impaired in beta-cells from hyperglycemic mice. J Endocrinol. 2006;190:461-70 pubmed
    ..We have now used tolbutamide and arginine to test if the cell specificity exists also for the response to non-nutrient stimulation of beta-..
  4. Uchida S, Yamada H, Li X, Maruyama S, Ohmori Y, Oki T, et al. Effects of Ginkgo biloba extract on pharmacokinetics and pharmacodynamics of tolbutamide and midazolam in healthy volunteers. J Clin Pharmacol. 2006;46:1290-8 pubmed
    ..CYP2C9 probe (tolbutamide, 125 mg) and CYP3A4 probe (midazolam, 8 mg) were orally administered to 10 male healthy volunteers before and ..
  5. Hansen T, Echwald S, Hansen L, Møller A, Almind K, Clausen J, et al. Decreased tolbutamide-stimulated insulin secretion in healthy subjects with sequence variants in the high-affinity sulfonylurea receptor gene. Diabetes. 1998;47:598-605 pubmed
    ..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...
  6. Kang L, Dunn Meynell A, Routh V, Gaspers L, Nagata Y, Nishimura T, et al. Glucokinase is a critical regulator of ventromedial hypothalamic neuronal glucosensing. Diabetes. 2006;55:412-20 pubmed
    ..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. ..
  7. Ramracheya R, Ward C, Shigeto M, Walker J, Amisten S, Zhang Q, et al. Membrane potential-dependent inactivation of voltage-gated ion channels in alpha-cells inhibits glucagon secretion from human islets. Diabetes. 2010;59:2198-208 pubmed publisher
    ..Human alpha-cells are electrically active at 1 mmol/l glucose. Inhibition of K(ATP)-channels with tolbutamide depolarized alpha-cells by 10 mV and reduced the action potential amplitude...
  8. Tsotsou G, Sideri A, Goyal A, Di Nardo G, Gilardi G. Identification of mutant Asp251Gly/Gln307His of cytochrome P450 BM3 for the generation of metabolites of diclofenac, ibuprofen and tolbutamide. Chemistry. 2012;18:3582-8 pubmed publisher
    ..The double mutant Asp251Gly/Gln307His (A2) with activities towards diclofenac, ibuprofen and tolbutamide was identified by screening with the alkali method...
  9. Quoix N, Cheng Xue R, Mattart L, Zeinoun Z, Guiot Y, Beauvois M, et al. Glucose and pharmacological modulators of ATP-sensitive K+ channels control [Ca2+]c by different mechanisms in isolated mouse alpha-cells. Diabetes. 2009;58:412-21 pubmed publisher
    ..alpha-Cell I(KATP) was inhibited by tolbutamide and activated by diazoxide or the mitochondrial poison azide, as in beta-cells...
  10. Braun M, Ramracheya R, Amisten S, Bengtsson M, Moritoh Y, Zhang Q, et al. Somatostatin release, electrical activity, membrane currents and exocytosis in human pancreatic delta cells. Diabetologia. 2009;52:1566-78 pubmed publisher
    ..Somatostatin secretion from human islets was stimulated by glucose and tolbutamide and inhibited by diazoxide...
  11. Blaisdell J, Jorge Nebert L, Coulter S, Ferguson S, Lee S, Chanas B, et al. Discovery of new potentially defective alleles of human CYP2C9. Pharmacogenetics. 2004;14:527-37 pubmed
    ..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 ..
  12. Plum L, Ma X, Hampel B, Balthasar N, Coppari R, Munzberg H, et al. Enhanced PIP3 signaling in POMC neurons causes KATP channel activation and leads to diet-sensitive obesity. J Clin Invest. 2006;116:1886-901 pubmed
    ..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. DeLozier T, Lee S, Coulter S, Goh B, Goldstein J. Functional characterization of novel allelic variants of CYP2C9 recently discovered in southeast Asians. J Pharmacol Exp Ther. 2005;315:1085-90 pubmed
    ..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...
  14. Liss B, Bruns R, Roeper J. Alternative sulfonylurea receptor expression defines metabolic sensitivity of K-ATP channels in dopaminergic midbrain neurons. EMBO J. 1999;18:833-46 pubmed
  15. Huopio H, Reimann F, Ashfield R, Komulainen J, Lenko H, Rahier J, et al. Dominantly inherited hyperinsulinism caused by a mutation in the sulfonylurea receptor type 1. J Clin Invest. 2000;106:897-906 pubmed
    ..In conclusion, we describe the first dominantly inherited SUR1 mutation that causes CHI in early life and predisposes to later insulin deficiency...
  16. Vieira E, Salehi A, Gylfe E. Glucose inhibits glucagon secretion by a direct effect on mouse pancreatic alpha cells. Diabetologia. 2007;50:370-9 pubmed
    ..In islets exposed to tolbutamide plus 8 mmol/l K(+), glucose inhibited glucagon secretion without stimulating the release of insulin and ..
  17. Hanatani T, Fukuda T, Onishi S, Funae Y, Azuma J. No major difference in inhibitory susceptibility between CYP2C9.1 and CYP2C9.3. Eur J Clin Pharmacol. 2003;59:233-5 pubmed
    ..1 and CYP2C9.3 were expressed in yeast. Using typical CYP2C9 substrates (diclofenac, tolbutamide and S-warfarin) and a potent CYP2C9 inhibitor (nicardipine), the Ki values for nicardipine on the three ..
  18. Chen K, Wang R, Wen S, Li J, Wang S. Relationship of P450 2C9 genetic polymorphisms in Chinese and the pharmacokinetics of tolbutamide. J Clin Pharm Ther. 2005;30:241-9 pubmed
    To study the relationship between P450 2C9 genetic polymorphisms and the pharmacokinetics of tolbutamide in Chinese subjects. P450 2C9 genotype was determined by oligonucleotide microarray...
  19. Tucker S, Gribble F, Zhao C, Trapp S, Ashcroft F. Truncation of Kir6.2 produces ATP-sensitive K+ channels in the absence of the sulphonylurea receptor. Nature. 1997;387:179-83 pubmed
    ..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...
  20. Veronese M, Mackenzie P, Doecke C, McManus M, Miners J, Birkett D. Tolbutamide and phenytoin hydroxylations by cDNA-expressed human liver cytochrome P4502C9. Biochem Biophys Res Commun. 1991;175:1112-8 pubmed
    ..The expressed enzyme catalysed the methylhydroxylation of tolbutamide with an apparent Km of 131.7 microM, similar to that observed in human liver microsomes...
  21. Schwanstecher C, Dickel C, Panten U. Interaction of tolbutamide and cytosolic nucleotides in controlling the ATP-sensitive K+ channel in mouse beta-cells. Br J Pharmacol. 1994;111:302-10 pubmed
    ..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+...
  22. Yamasaki I, Yamada M, Uotsu N, Teramoto S, Takayanagi R, Yamada Y. Inhibitory effects of kale ingestion on metabolism by cytochrome P450 enzymes in rats. Biomed Res. 2012;33:235-42 pubmed
    ..cocktail probe drugs, including midazolam (for CYP3A4), caffeine (for CYP1A2), dextromethorphan (for CYP2D6), tolbutamide (for CYP2C9), omeprazole (for CYP2C19), and chlorzoxazone (for CYP2E1)...
  23. Xu M, Tang H, Rong Q, Zhang Y, Li Y, Zhao L, et al. The Effects of Formaldehyde on Cytochrome P450 Isoform Activity in Rats. Biomed Res Int. 2017;2017:6525474 pubmed publisher
    ..CYP3A2 were assessed by determining changes in the pharmacokinetic parameters of the probe drugs phenacetin, tolbutamide, chlorzoxazone, and testosterone, respectively...
  24. Gorski J, Huang S, Pinto A, Hamman M, Hilligoss J, Zaheer N, et al. The effect of echinacea (Echinacea purpurea root) on cytochrome P450 activity in vivo. Clin Pharmacol Ther. 2004;75:89-100 pubmed
    ..Echinacea purpurea root) on CYP activity in vivo was assessed by use of the CYP probe drugs caffeine (CYP1A2), tolbutamide (CYP2C9), dextromethorphan (CYP2D6), and midazolam (hepatic and intestinal CYP3A)...
  25. Misaki N, Mao X, Lin Y, Suga S, Li G, Liu Q, et al. Iptakalim, a vascular ATP-sensitive potassium (KATP) channel opener, closes rat pancreatic beta-cell KATP channels and increases insulin release. J Pharmacol Exp Ther. 2007;322:871-8 pubmed
  26. Shigeto M, Ramracheya R, Tarasov A, Cha C, Chibalina M, Hastoy B, et al. GLP-1 stimulates insulin secretion by PKC-dependent TRPM4 and TRPM5 activation. J Clin Invest. 2015;125:4714-28 pubmed publisher
    ..occurred without activation of PKA, and persisted in the presence of PKA inhibitors, the KATP channel blocker tolbutamide, and the L-type Ca(2+) channel blocker isradipine; however, depolarization was abolished by lowering ..
  27. Reinhardt R, Manaenko A, Pissarek M, Wagner A, Illes P. Alterations of purine and pyrimidine nucleotide contents in rat corticoencephalic cell cultures following metabolic damage and treatment with openers and blockers of ATP-sensitive potassium channels. Neurochem Int. 2002;40:427-33 pubmed
    ..By contrast, the K(ATP) channel antagonist tolbutamide (300 microM) aggravated the hypoxic decrease of nucleotide levels in a glucose-free medium, although it was ..
  28. He N, Zhang W, Shockley D, Edeki T. Inhibitory effects of H1-antihistamines on CYP2D6- and CYP2C9-mediated drug metabolic reactions in human liver microsomes. Eur J Clin Pharmacol. 2002;57:847-51 pubmed
    To screen the inhibitory effects of H1-antihistamines on hepatic bufuralol 1'-hydroxylation and on tolbutamide 4-methylhydroxylation in human liver microsomes...
  29. Treijtel N, Barendregt A, Freidig A, Blaauboer B, van Eijkeren J. Modeling the in vitro intrinsic clearance of the slowly metabolized compound tolbutamide determined in sandwich-cultured rat hepatocytes. Drug Metab Dispos. 2004;32:884-91 pubmed
    ..Substrate depletion of tolbutamide and the formation of its metabolites hydroxytolbutamide and carboxytolbutamide were measured in the medium and ..
  30. Shah S, Sanda S, Regmi N, Sasaki K, Shimoda M. Characterization of cytochrome P450-mediated drug metabolism in cats. J Vet Pharmacol Ther. 2007;30:422-8 pubmed
    ..CYP1A, 2C, 2D and 3A activities were referred by ethoxyresorufin O-deethylation (EROD), tolbutamide hydroxylation (TBH), bufuralol 1'-hydroxylation (BLH) and midazolam 1'- and 4-hydroxylation respectively...
  31. Brown S, Abdelhafiz A. Trials review: cardiovascular outcome with intensive glycemic control and implications for patients with type 2 diabetes. Postgrad Med. 2009;121:31-41 pubmed publisher
    ..This article reviews results of earlier and recently published intervention trials of intensive glucose control and their outcomes and discusses relevant recommendations for adults with type 2 diabetes. ..
  32. Landa L, Harbeck M, Kaihara K, Chepurny O, Kitiphongspattana K, Graf O, et al. Interplay of Ca2+ and cAMP signaling in the insulin-secreting MIN6 beta-cell line. J Biol Chem. 2005;280:31294-302 pubmed
    ..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 ..
  33. Ostuni A, Lograno M, Gasbarro A, Bisaccia F, Tamburro A. Novel properties of peptides derived from the sequence coded by exon 26A of human elastin. Int J Biochem Cell Biol. 2002;34:130-5 pubmed
  34. Zhang Y, Zhang D, Ge N, Zhu G, Hao C, Zhang Y, et al. Effect of Evodiamine on CYP Enzymes in Rats by a Cocktail Method. Pharmacology. 2016;97:218-23 pubmed publisher
    ..0 mg/kg; CYP1A2 activity), tolbutamide (1...
  35. Hu S, Mazur C, Feenstra K, Lorenz J, Merritt D. Assessment of inhibition of porcine hepatic cytochrome P450 enzymes by 48 commercial drugs. Vet J. 2016;211:26-31 pubmed publisher
    ..liver microsomes for six specific CYP450 metabolisms (phenacetin o-deethylation, coumarin 7-hydroxylation, tolbutamide 4-hydroxylation, bufuralol 1-hydroxylation, chlorozoxazone 6-hydroxylation and midazolam 1'-hydroxylation)...
  36. Grangeon A, Gravel S, Gaudette F, Turgeon J, Michaud V. Highly sensitive LC-MS/MS methods for the determination of seven human CYP450 activities using small oral doses of probe-drugs in human. J Chromatogr B Analyt Technol Biomed Life Sci. 2017;1040:144-158 pubmed publisher
    ..The seven-drug cocktail was composed of caffeine, bupropion, tolbutamide, omeprazole, dextromethorphan, midazolam (all administered concomitantly) and chlorzoxazone (administered ..
  37. Huang W, Acosta Martinez M, Levine J. Ovarian steroids stimulate adenosine triphosphate-sensitive potassium (KATP) channel subunit gene expression and confer responsiveness of the gonadotropin-releasing hormone pulse generator to KATP channel modulation. Endocrinology. 2008;149:2423-32 pubmed publisher
    ..Infusion of the K(ATP) channel blocker tolbutamide into the third ventricle resulted in increased LH pulse frequency in animals treated with E(2)+P but was ..
  38. Rustenbeck I, Winkler M, Jörns A. Desensitization of insulin secretory response to imidazolines, tolbutamide, and quinine. I. Secretory and morphological studies. Biochem Pharmacol. 2001;62:1685-94 pubmed
    ..alinidine, and idazoxan (100 microM each) were compared with those of the well-characterized sulfonylurea, tolbutamide (500 microM), and those of the ion channel-blocking alkaloid, quinine (100 microM)...
  39. Schofl C, Borger J, Mader T, Waring M, von zur Muhlen A, Brabant G. Tolbutamide and diazoxide modulate phospholipase C-linked Ca(2+) signaling and insulin secretion in beta-cells. Am J Physiol Endocrinol Metab. 2000;278:E639-47 pubmed
    ..We examined whether tolbutamide and diazoxide, which close or open ATP-sensitive K(+) channels (K(ATP) channels), respectively, interact with ..
  40. Ortiz M, Medina Tato D, Sarmiento Heredia D, Palma Martínez J, Granados Soto V. Possible activation of the NO-cyclic GMP-protein kinase G-K+ channels pathway by gabapentin on the formalin test. Pharmacol Biochem Behav. 2006;83:420-7 pubmed
    ..Likewise, glibenclamide or tolbutamide (ATP-sensitive K+ channel inhibitors), 4-aminopyridine or tetraethylammonium (non-selective inward rectifier K+ ..
  41. Henquin J, Sempoux C, Marchandise J, Godecharles S, Guiot Y, Nenquin M, et al. Congenital hyperinsulinism caused by hexokinase I expression or glucokinase-activating mutation in a subset of ?-cells. Diabetes. 2013;62:1689-96 pubmed publisher
    ..Diazoxide suppressed IS and tolbutamide antagonized the inhibition. The most conspicuous anomaly was a large stimulation of IS by 1 mmol/L glucose...
  42. Geng T, Si H, Kang D, Li Y, Huang W, Ding G, et al. Influences of Re Du Ning Injection, a traditional Chinese medicine injection, on the CYP450 activities in rats using a cocktail method. J Ethnopharmacol. 2015;174:426-36 pubmed publisher comparing plasma pharmacokinetics of substrates and their metabolites (phenacetin/ paracetamol for CYP1A2, tolbutamide/4-hydroxytolbutamide for CYP2C11, dextromethorphan/ dextrorphan for CYP2D1 and dapsone/N-acetyl dapsone for ..
  43. Huopio H, Jaaskelainen J, Komulainen J, Miettinen R, Kärkkäinen P, Laakso M, et al. Acute insulin response tests for the differential diagnosis of congenital hyperinsulinism. J Clin Endocrinol Metab. 2002;87:4502-7 pubmed
    ..determining acute (1-3 min) plasma insulin and C-peptide responses to calcium (n = 18), glucose (n = 12), and tolbutamide (n = 11) in those CHI patients who were able to take part in these studies...
  44. Bal R, Ozturk G, Etem E, Him A, Cengiz N, Kuloglu T, et al. Modulation of Excitability of Stellate Neurons in the Ventral Cochlear Nucleus of Mice by ATP-Sensitive Potassium Channels. J Membr Biol. 2018;251:163-178 pubmed publisher
    ..Blockers of KATP channels, glibenclamide (0.2 mM), tolbutamide (0...
  45. Dallaporta M, Perrin J, Orsini J. Involvement of adenosine triphosphate-sensitive K+ channels in glucose-sensing in the rat solitary tract nucleus. Neurosci Lett. 2000;278:77-80 pubmed
    ..Thus, K(ATP) channels were pharmacologically identified in the caudal NTS, where they may be partly involved in glucose sensing. ..
  46. Shi R, Wu J, Meng C, Ma B, Wang T, Li Y, et al. Cyp3a11-mediated testosterone-6?-hydroxylation decreased, while UGT1a9-mediated propofol O-glucuronidation increased, in mice with diabetes mellitus. Biopharm Drug Dispos. 2016;37:433-443 pubmed publisher
    ..bupropion-hydroxylation, omeprazole-5-hydroxylation, dextromethorphan-O-demethylation, tolbutamide-4-hydroxylation, chlorzoxazone-6-hydroxylation and midazolam-1-hydroxylation and in glucuronidation reactions ..
  47. Abdelmoneim A, Hasenbank S, Seubert J, Brocks D, Light P, Simpson S. Variations in tissue selectivity amongst insulin secretagogues: a systematic review. Diabetes Obes Metab. 2012;14:130-8 pubmed publisher
    ..This study was designed to identify insulin secretagogues that selectively bind to SUR1 when given at therapeutic doses...
  48. Bryan J, Aguilar Bryan L. Sulfonylurea receptors: ABC transporters that regulate ATP-sensitive K(+) channels. Biochim Biophys Acta. 1999;1461:285-303 pubmed
    ..K(ATP) channels are a unique example of the physiologic and medical importance of a transport ATPase and provide a paradigm for how other members of the family may interact with other ion channels...
  49. Squires P, Persaud S, Hauge Evans A, Gray E, Ratcliff H, Jones P. Co-ordinated Ca(2+)-signalling within pancreatic islets: does beta-cell entrainment require a secreted messenger. Cell Calcium. 2002;31:209-19 pubmed
    ..b>Tolbutamide evoked a concentration-dependent recruitment of active cells within cell clusters, both in terms of numbers of ..
  50. Sun E, de Fontgalland D, Rabbitt P, Hollington P, Sposato L, Due S, et al. Mechanisms Controlling Glucose-Induced GLP-1 Secretion in Human Small Intestine. Diabetes. 2017;66:2144-2149 pubmed publisher
    ..KATP channels do not drive this, as tolbutamide did not trigger release...
  51. Zhang W, Han F, Guo P, Zhao H, Lin Z, Huang M, et al. Simultaneous determination of tolbutamide, omeprazole, midazolam and dextromethorphan in human plasma by LC-MS/MS--a high throughput approach to evaluate drug-drug interactions. J Chromatogr B Analyt Technol Biomed Life Sci. 2010;878:1169-77 pubmed publisher
    ..of a NCE on the pharmacokinetics of a cocktail of representative probes of CYP enzymes (midazolam for CYP3A4, tolbutamide for CYP2C9, omeprazole for CYP2C19 and dextromethorphan for CYP2D6) and the safety and tolerability of the NCE ..
  52. González J, Jensen L, Fugger L, Burdakov D. Metabolism-independent sugar sensing in central orexin neurons. Diabetes. 2008;57:2569-76 pubmed publisher
    ..Our new data suggest that behaviorally critical neurocircuits of the lateral hypothalamus contain glucose detectors that exhibit novel sugar selectivity and can operate independently of glucose metabolism. ..
  53. Rustenbeck I, Krautheim A, Jörns A, Steinfelder H. Beta-cell toxicity of ATP-sensitive K+ channel-blocking insulin secretagogues. Biochem Pharmacol. 2004;67:1733-41 pubmed
    ..insulin secretagogues, the imidazolines phentolamine, alinidine and idazoxan (100microM each), the sulfonylurea tolbutamide (500microM), or the alkaloid quinine (100microM) resulted in morphological damage of 4-18% of beta-cells ..