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Tolbutamide

Tolbutamide is a sulfonylurea medication used to treat type 2 diabetes.
It works by stimulating the release of insulin from the pancreas, helping to lower blood sugar levels.
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Most cited protocols related to «Tolbutamide»

1
Cytochrome P450 Mediated Metabolism
Cited 18 times
Tolbutamide was purchased from Dr. Ehrenstorfer GmbH (Augsburg, Germany). 4-hydroxyTolbutamide and 6-hydroxychlorzoxazone were obtained from Toronto Research Chemicals Inc. (North York, Canada). Dextromethorphan, dextrorphan and chlorzoxazone were supplied by Sigma-Aldrich Co. (St Louis, MO, USA). Testosterone was obtained from International Laboratory Limited (San Bruno, CA, USA). 6β-hydroxytestosterone was purchased from BD Biosciences Co. (Woburn, MA, USA). Phenacetin, cortisone acetate, EB and EE were from National Institute for the Control of Pharmaceutical and Biological Products (Beijing, China). NADPH was obtained from Roche Diagnostics GmbH (Mannheim, Germany). All other reagents were of HPLC or analytical grade.
Guo S., Liu Y., Lin Z., Tai S., Yin S, & Liu G. (2014). Effects of Eleutheroside B and Eleutheroside E on activity of cytochrome P450 in rat liver microsomes. BMC Complementary and Alternative Medicine, 14, 1.
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Publication 2014
4'-hydroxytolbutamide 6-hydroxychlorzoxazone Biological Products Chlorzoxazone Cortisone Acetate Dextromethorphan Dextrorphan Diagnosis High-Performance Liquid Chromatographies NADP Pharmaceutical Preparations Phenacetin Testosterone Tolbutamide
2
In vitro CYP2C9 Enzyme Kinetics
Cited 13 times
The incubation system of CYP2C9 in vitro contained phosphate buffer (100 mM, pH7.4), liver microsomal protein (0.5 mg · mL-1), MgCl2 (10 mM), tolbutamide (90 μM) and eleutherosides in a final volume of 200 μL. Pre-incubated 5 min, the reaction was initiated by adding NADPH (1 mM concentration in incubation) and the incubation systems were incubated at 37°C for 60 min. After incubation, 50 μL ice-cold acetonitrile was added to terminate the reaction, and phenacetin of a final concentration 20 μM was added as internal standard. With 5 min suspension, the mixture was centrifuged for 30 min at 12000 r · min-1. The supernatant of 20 μL was analyzed by the Waters HPLC system 2010 (Waters, USA, with 600 pump, 996PAD UV detector and Millipore Systems). Tolbutamide, 4-hydroxytolbutamide and phenacetin were separated on a Diamonsil C18 reverse phase column (5 μm, 4.6 mm × 200 mm). The column temperature was set to 35°C. The mobile phase, at a flow rate of 1 mL · min-1, consisted of methanol and 0.1% acetic acid (55:45, v/v). UV detection was at wavelength of 229 nm. The organic solvent which is at low concentration (≤0.5%) in all incubation systems wouldn’t affect the activity of enzymes. The yield of corresponding metabolites was calculated by referring to a standard curve constructed based on known concentrations of the pure metabolites.
Guo S., Liu Y., Lin Z., Tai S., Yin S, & Liu G. (2014). Effects of Eleutheroside B and Eleutheroside E on activity of cytochrome P450 in rat liver microsomes. BMC Complementary and Alternative Medicine, 14, 1.
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Publication 2014
4'-hydroxytolbutamide Acetic Acid acetonitrile Buffers Cold Temperature eleutherosides enzyme activity Exhaling High-Performance Liquid Chromatographies Magnesium Chloride Methanol Microsomes, Liver NADP Phenacetin Phosphates Proteins Solvents Tolbutamide
3
Electrophysiological Characterization of MCH Neurons
Cited 10 times

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Publication 2010
Acclimatization Action Potentials Axon Bath Brain Egtazic Acid Electricity Eye gluconate Glucose HEPES Magnesium Chloride Mice, Laboratory Neurons Osmolarity Perfusion Pulses Sucrose Tolbutamide Young Adult
4
Perifusion-based Insulin Secretion Assay
Cited 7 times

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Publication 2019
1-Methyl-3-isobutylxanthine Arginine Glucose Insulin Secretagogues Specimen Collection Tolbutamide
5
Michaelis Constant and Reaction Velocity
Cited 6 times
The apparent Km (Michaelis constant) and Vmax (maximum reaction velocity) values were determined in a range of concentrations of probe drugs. The concentrations were as follows: tolbutamide 3.5~600.0 μM, dextromethorphan 3.5~400.0 μM, chlorzoxazone 5.0~300.0 μM, and testosterone 12.5~500.0 μM. The other incubation conditions were the same as Section Cytochrome P450 probe substrate assays.
Guo S., Liu Y., Lin Z., Tai S., Yin S, & Liu G. (2014). Effects of Eleutheroside B and Eleutheroside E on activity of cytochrome P450 in rat liver microsomes. BMC Complementary and Alternative Medicine, 14, 1.
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Publication 2014
Biological Assay Chlorzoxazone Cytochrome P450 Dextromethorphan Pharmaceutical Preparations Testosterone Tolbutamide

Most recents protocols related to «Tolbutamide»

1
Isolation and Functional Assessment of Pancreatic Islets
Islets were isolated from 8- to 36-week-old male and female mice. Isolation of pancreatic islets was performed as previously described (62 (link)). In brief, pancreas was perfused by injection of 3 mM Collagenase-P (Roche) (0.3 mg/mL) in HBSS containing 25 mM HEPES and 0.5% (w/v) BSA into the common bile duct. Isolated islets were recovered for 48 hours in RPMI 1640 (Thermo Fisher Scientific) in humidified 5% CO2, at 37°C. After this period, islets were used for functional assessments. Before determination of insulin secretion, islets were equilibrated for 1 hour in KRB buffer (115 mM NaCl, 4.5 mM KCl, 1.2 mM KH2PO4, 2.6 mM CaCl2, 1 mM MgCl2, 10 mM HEPES, 20 mM NaHCO3, 0.2% w/v BSA, pH 7.4) with 2.8 mM glucose. Determination of insulin secretion from the islets was performed in 12-well plates containing 60 μL KRB (8 islets/well, 5 independent experiments performed in triplicate). After 1 hour preincubation in KRB with 2.8 mM glucose, islets were incubated for 1 hour in 20 mM glucose, 25 mM KCl, or 300 μM tolbutamide. Released insulin was measured in the supernatant using an insulin ELISA kit. Insulin content was determined from groups of 10 islets lysed in the protein extraction reagent M-PER (Thermo Fisher Scientific), using insulin ELISA kit.
Khajavi N., Beck A., Riçku K., Beyerle P., Jacob K., Syamsul S.F., Belkacemi A., Reinach P.S., Schreier P.C., Salah H., Popp T., Novikoff A., Breit A., Chubanov V., Müller T.D., Zierler S, & Gudermann T. (2023). TRPM7 kinase is required for insulin production and compensatory islet responses during obesity. JCI Insight, 8(3), e163397.
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Publication 2023
Bicarbonate, Sodium Buffers Choledochus Enzyme-Linked Immunosorbent Assay Females Glucose Hemoglobin, Sickle HEPES Insulin Insulin Secretion Islets of Langerhans Magnesium Chloride Males Matrix Metalloproteinase 13 Mice, House M protein, multiple myeloma Pancreas Sodium Chloride Tolbutamide
2
Pharmacological Modulation of Respiratory Rhythmogenesis
Heme oxygenase activity was blocked using bath application of Chromium (III) Mesoporphyrin IX chloride (ChrMP459, 20 μM; Frontiers Sciences, Newark DE). A CO donor, CORM-3 (20 μM; Sigma-Aldrich St. Louis MO) was bath applied following ChrMP459 application. NaHS (10μM to 100 μM; Sigma-Aldrich), a H2S donor, was bath applied. In all patch clamp experiments, fast synaptic glycinergic and GABAergic inhibition was blocked by bath application of strychnine (1 μM; Sigma-Aldrich) and picrotoxin (50 μM; Sigma-Aldrich), respectively. Inhibition of CSE production was accomplished by in vivo L-propargylglycine L-PAG, 30 mg/kg (Sigma-Aldrich) administered (i.p. injection) 2.5–3 hrs prior to preparation of the rhythmic brainstem slice preparation. Inhibition of potassium channels SKCaand ATP-sensitive potassium channel (KATP) was via bath application of Apamin (200 μM; Sigma-Aldrich) and Tolbutamide (100 μM; Sigma-Aldrich), respectively.
Browe B.M., Peng Y.J., Nanduri J., Prabhakar N.R, & Garcia AJ I.I.I. (2023). Gasotransmitter modulation of hypoglossal motoneuron activity. eLife, 12, e81978.
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Publication 2023
Apamin Bath Brain Stem Chlorides Chromium Heme Oxygenase (Decyclizing) KATP Channels mesoporphyrin IX Picrotoxin propargylglycine Psychological Inhibition sodium bisulfide Strychnine Tissue Donors Tolbutamide
3
In Vitro Cytochrome P450 Assay
Potassium phosphate buffer (200 µl, 0.1 M, pH 7.4) containing 1 mM NADPH, 0.5 mg/mL human liver microsomes, and a cocktail assay of seven probe substrates (Phenacetin for CYP1A2, Paclitaxel for CYP2C8, Tolbutamide for CYP2C9, Omeprazole for CYP2C19, Dextromethorphan for CYP2D6, Chlorzoxazone for CYP2E1, Dextromethorphan and Testosterone for CYP3A) or a single substrate (≤Km) were incubated at 37°C for 15 min (Supplementary Table S1). The contents of organic solvent and DMSO in incubation mixture was under 1% (v/v) and 0.1% (v/v) respectively. Reactions were terminated by adding 200 µL of an ice-cold stop solution consisting of methanol containing Rutin (2 µg/ml) as internal standard. Samples were subsequently cooled in ice bath to precipitate proteins. Supernatants were collected into clean tubes after centrifugation at 12000 rpm at 4°C for 10 min prior to inject into LC-MS/MS.
Lin F., Lin X., Wang X., Mei G., Chen B., Yao H, & Huang L. (2023). Inhibitory effect of Selaginella doederleinii hieron on human cytochrome P450. Frontiers in Pharmacology, 14, 1108867.
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Publication 2023
Bath Biological Assay Buffers Centrifugation Chlorzoxazone Cold Temperature CYP1A2 protein, human CYP2C8 protein, human CYP2C19 protein, human Cytochrome P-450 CYP2D6 Cytochrome P-450 CYP2E1 Dextromethorphan Homo sapiens Methanol Microsomes, Liver NADP Omeprazole Paclitaxel Phenacetin potassium phosphate Proteins Rutin Solvents Sulfoxide, Dimethyl Tandem Mass Spectrometry Testosterone Tolbutamide
4
Phytochemical Profiling and Enzymatic Assays
Pooled mixed gender human liver microsomes from 50 donors were purchased from XenoTech (Lenexa, United States), β-nicotinamide adenine dinucleotide phosphate (NADPH) were purchased from solarbiobiotech (Beijing, China), Omeprazole (HPLC purity> 99%), Taxol (HPLC purity> 99%), Tolbutamide (HPLC purity> 99%), Chlorzoxazone (HPLC purity> 99%), Dextromethorphan Hydrobromide (HPLC purity> 98%), Alpha-Naphthoflavone (HPLC purity> 98%), Fluconazole (HPLC purity> 98%), Quercetin (HPLC purity> 98%) and Ketoconazole (HPLC purity> 99%) were purchased from Dalian Meilunbio. Co. Ltd (Dalian, China), Phenaceti (HPLC purity> 99%), Sulfaphenazolum (HPLC purity> 99%), Quinidine (HPLC purity> 99%) were purchased from Shyuanye Biotechnology Co. Ltd (Shanghai, China), Testosterone (HPLC purity> 98%) were purchased from Derick Biotechnology Co. Ltd (Chengdu, China), 4-Methylpyrazole (HPLC purity> 97%) were purchased from J&K Scientific (San Jose, United States).
The SDEA extract was prepared following our previously described procedure (Sui et al., 2016 (link); Yao et al., 2017 (link)). Delicaflavone (purity≥ 98%, determined by the peak area normalization method using HPLC-PDA) were isolated from S. doederleinii and the structure was fully elucidated by MS, UV, 1H-NMR and 13C-NMR, which was confirmed by comparison with the literatures (Li et al., 2013 (link); Li et al., 2014 (link); Yao et al., 2017 (link); Chen et al., 2018 (link)). Amentoflavone (HPLC purity> 98%) and Apigenin (HPLC purity> 98%) were purchased from Dalian Meilunbio. Co. Ltd (Dalian, China), Palmatine (HPLC purity> 98%) was purchased from Shyuanye Biotechnology Co. Ltd (Shanghai, China).
Methanol and acetonitrile (HPLC grade) were purchased from Merck KGaA (Darmstadt, Germany), formic acid (HPLC grade) was purchased from Aladdin (Shanghai, China), ethanol (analytical grade) was obtained from Sinopharm Chemical Reagents (Shanghai, China), and ultrapure water was prepared by a Millpore Milli-Q system (Beddford, United States).
Lin F., Lin X., Wang X., Mei G., Chen B., Yao H, & Huang L. (2023). Inhibitory effect of Selaginella doederleinii hieron on human cytochrome P450. Frontiers in Pharmacology, 14, 1108867.
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Publication 2023
1H NMR acetonitrile alpha-naphthoflavone amentoflavone Apigenin Carbon-13 Magnetic Resonance Spectroscopy Chlorzoxazone Dextromethorphan Hydrobromide Donors Ethanol Fluconazole Fomepizole formic acid High-Performance Liquid Chromatographies Homo sapiens Ketoconazole Methanol Microsomes, Liver NADP Omeprazole palmatine Quercetin Quinidine Sulfaphenazole Taxol Testosterone Tolbutamide
5
CYP Inhibition Assay for Drug-Drug Interactions
The drug–drug interaction potential was evaluated using a CYP cocktail assay that involved microsomal incubation and NADPH, as described elsewhere (Lee et al., 2012 (link)). Time-dependent inhibitions of CYP2C9 (tolbutamide as a selective substrate) and CYP3A4 (midazolam and testosterone as selective substrates) were evaluated using non-dilution method (Parkinson et al., 2011 (link)) with the same concentration range of GRL0617 used direct inhibition (0–50 µM) in total volume of 180 µL per tube consisting of 0.1 M PPB (pH 7.4). The first reactions were initiated by NADPH addition, and each mixture was incubated in a shaking water bath at 37°C for 30 min. The final incubation was performed for 10 min with a total volume of 200 µL by adding substrates (tolbutamide (set B) as a CYP2C9 selective substrate, midazolam (set A) and testosterone (set B) as CYP3A4 selective substrates) and NADPH. The reaction was stopped and quenched by adding 200 µL of ice-cold acetonitrile containing 50 nM CBZ as internal standard, then centrifuged at 3,000 x g for 20 min. The supernatants were injected in LC-QTOF system. IC50 shift values were calculated as the ratio of the IC50 value obtained after pre-incubation without NADPH divided by the IC50 value obtained after 30 min incubation with NADPH. Based on IC50 shifts more than 1.5-fold, the inhibitor was determined to be time-dependent inhibitor (Berry and Zhao, 2008 (link)).
Cho H., Kim Y.J., Chae J.W., Meyer M.R., Kim S.K, & Ryu C.S. (2023). In vitro metabolic characterization of the SARS-CoV-2 papain-like protease inhibitors GRL0617 and HY-17542. Frontiers in Pharmacology, 14, 1067408.
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Publication 2023
acetonitrile Bath Berries Biological Assay Cold Temperature Cytochrome P-450 CYP3A4 Drug Interactions GRL0617 Microsomes Midazolam NADP Psychological Inhibition Technique, Dilution Testosterone Tolbutamide

Top products related to «Tolbutamide»

1
Tolbutamide by Merck Group
Sourced in United States, Germany, United Kingdom
Tolbutamide is a pharmaceutical compound used as a laboratory reagent. It is a sulfonylurea drug that acts as an antidiabetic agent by stimulating insulin secretion from the pancreas. Tolbutamide is commonly used in research and development settings to study glucose homeostasis and insulin regulation.
2
Phenacetin by Merck Group
Sourced in United States, China, Germany, United Kingdom, Poland
Phenacetin is a chemical compound used in the manufacturing of various pharmaceutical and laboratory products. It serves as a key ingredient in the production process. Phenacetin has specific functional properties that make it a valuable component in relevant applications, but a detailed description of its core function is beyond the scope of this response.
3
Chlorzoxazone by Merck Group
Sourced in United States, China, Germany, United Kingdom, Czechia
Chlorzoxazone is a laboratory chemical used as a reference standard. It is a crystalline solid with a molecular formula of C7H5ClNO. Chlorzoxazone is primarily used for analytical purposes and quality control in various industries.
4
Dextromethorphan by Merck Group
Sourced in United States, Germany, Sao Tome and Principe
Dextromethorphan is a laboratory chemical compound used as a research tool. It is a dissociative anesthetic and cough suppressant. Dextromethorphan is commonly used in scientific research, but its specific applications and intended uses should not be extrapolated or interpreted beyond its core function as a laboratory product.
5
Midazolam by Merck Group
Sourced in United States, China, Germany, United Kingdom, Australia
Midazolam is a benzodiazepine drug used as a sedative and hypnotic. It has a short half-life and is primarily used for the induction of anesthesia, procedural sedation, and the treatment of seizures.
6
Dimethyl sulfoxide (dmso) by Merck Group
Sourced in United States, Germany, United Kingdom, China, Italy, Sao Tome and Principe, France, Macao, India, Canada, Switzerland, Japan, Australia, Spain, Poland, Belgium, Brazil, Czechia, Portugal, Austria, Denmark, Israel, Sweden, Ireland, Hungary, Mexico, Netherlands, Singapore, Indonesia, Slovakia, Cameroon, Norway, Thailand, Chile, Finland, Malaysia, Latvia, New Zealand, Hong Kong, Pakistan, Uruguay, Bangladesh
DMSO is a versatile organic solvent commonly used in laboratory settings. It has a high boiling point, low viscosity, and the ability to dissolve a wide range of polar and non-polar compounds. DMSO's core function is as a solvent, allowing for the effective dissolution and handling of various chemical substances during research and experimentation.
7
Formic acid by Merck Group
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Formic acid is a colorless, pungent-smelling liquid chemical compound. It is the simplest carboxylic acid, with the chemical formula HCOOH. Formic acid is widely used in various industrial and laboratory applications.
8
Methanol by Merck Group
Sourced in Germany, United States, Italy, India, United Kingdom, China, France, Poland, Spain, Switzerland, Australia, Canada, Sao Tome and Principe, Brazil, Ireland, Japan, Belgium, Portugal, Singapore, Macao, Malaysia, Czechia, Mexico, Indonesia, Chile, Denmark, Sweden, Bulgaria, Netherlands, Finland, Hungary, Austria, Israel, Norway, Egypt, Argentina, Greece, Kenya, Thailand, Pakistan
Methanol is a clear, colorless, and flammable liquid that is widely used in various industrial and laboratory applications. It serves as a solvent, fuel, and chemical intermediate. Methanol has a simple chemical formula of CH3OH and a boiling point of 64.7°C. It is a versatile compound that is widely used in the production of other chemicals, as well as in the fuel industry.
9
Bupropion by Merck Group
Sourced in United States, Germany
Bupropion is a laboratory equipment product manufactured by Merck Group. It is a chemical compound used in various scientific and research applications. Bupropion is utilized for its specific chemical properties and functions, but a detailed description cannot be provided while maintaining an unbiased and factual approach.
10
Acetonitrile by Merck Group
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Acetonitrile is a colorless, volatile, flammable liquid. It is a commonly used solvent in various analytical and chemical applications, including liquid chromatography, gas chromatography, and other laboratory procedures. Acetonitrile is known for its high polarity and ability to dissolve a wide range of organic compounds.

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