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Unbound Medicine.
(Apo Tolbutamide)
6,797 results
  • [Effect of Laportea bulbifera extract on CYP450 enzyme activities in rats by Cocktail probe drug method]. [Journal Article]
    Zhongguo Zhong Yao Za Zhi. 2022 Dec; 47(23):6320-6332.Yang HL, Li Y, … Gong ZP
  • The Cocktail probe drug method was used to evaluate the effect of Laportea bulbifera extract on the different subtypes of CYP450 enzyme activities in rats, and to provide references for its clinical rational drug use. The rats were randomly divided into a high-dose L. bulbifera group(0.45 g·kg~(-1)·d~(-1)) and a low-dose L. bulbifera group(0.09 g·kg~(-1)·d~(-1)). After continuous gavage for 7 and…
  • Determination of CYP450 activities in diabetes mellitus rats by a UHPLC-MS/MS method. [Journal Article]
    J Pharm Biomed Anal. 2023 Feb 05; 224:115191.Wang Z, Li QQ, … Zhang XD
  • In this study, we investigated the effect of type 1 diabetes mellitus on the modulation of the activities of CYP450s in dynamics by a UHPLC-MS/MS method. The diabetic rat model was constructed by an intraperitoneal single injection of streptozotocin. Fasting blood glucose levels > 16.7 mmol/L were considered as diabetic. The rats were given a cocktail of four probe drugs (10 mg/kg phenacetin, 1 m…
  • Cisapride induced hypoglycemia via the KCNH6 potassium channel. [Journal Article]
    Front Endocrinol (Lausanne). 2022; 13:1011238.Lu J, Shi TT, … Yang JK
  • Mutations in KCNH6 has been proved to cause hypoinsulinemia and diabetes in human and mice. Cisapride is a stomach-intestinal motility drug used to treat gastrointestinal dysfunction. Cisapride has been reported to be a potential inhibitor of the KCNH family, but it remained unclear whether cisapride inhibited KCNH6. Here, we discovered the role of cisapride on glucose metabolism, focusing on the…
  • Evaluation of Safety and Clinically Relevant Drug-Drug Interactions with Tucatinib in Healthy Volunteers. [Journal Article]
    Clin Pharmacokinet. 2022 Oct; 61(10):1417-1426.Topletz-Erickson A, Lee A, … Endres CJ
  • CONCLUSIONS: The potential DDIs identified here may be mitigated by avoiding concomitant use of tucatinib with strong CYP3A inducers, moderate CYP2C8 inducers, CYP3A substrates with a narrow therapeutic window (modifying substrate dose where concomitant use is unavoidable), and strong CYP2C8 inhibitors (decreasing tucatinib dose where concomitant use is unavoidable), or by reducing the dose of P-glycoprotein substrates with a narrow therapeutic window.
  • Inhibition of imrecoxib on mRNA and protein expression of CYP2C11 enzyme in rats. [Journal Article]
    Biomed Chromatogr. 2022 Oct; 36(10):e5439.Wu X, An Q, … Zhang Z
  • To evaluate the effect of imrecoxib on CYP2C11 enzyme activity, mRNA, and protein expression, a UPLC method was established. Tolbutamide was selected as the CYP2C11 enzyme-specific probe drug and incubated with imrecoxib in rat liver microsomes. The yield of 4-hydroxytolbutamide was measured using UPLC to investigate the effect of imrecoxib on CYP2C11 enzyme activity. Imrecoxib (10 mg/kg) was adm…
  • Crystal structure of 4-bromo-N-(propyl-carbamo-yl)benzene-sulfonamide. [Journal Article]
    Acta Crystallogr E Crystallogr Commun. 2022 May 01; 78(Pt 5):485-489.Bookwala M, Patel S, … Wildfong PLD
  • The title compound, C10H13BrN2O3S, 1, contains a sulfonyl urea moiety, which possesses potential therapeutic functions (e.g., anti-diabetic and herbicidal). The geometry of 1 is similar to its closely related analogues, chlorpropamide and tolbutamide. This compound crystallizes in the monoclinic space group C2/c, having one mol-ecule in its asymmetric unit. The crystal structure of 1, recorded at…
  • Glucose inhibits glucagon secretion by decreasing [Ca2+]c and by reducing the efficacy of Ca2+ on exocytosis via somatostatin-dependent and independent mechanisms. [Journal Article]
    Mol Metab. 2022 07; 61:101495.Singh B, Khattab F, Gilon P
  • CONCLUSIONS: We propose a model according to which glucose controls α-cell [Ca2+]c and glucagon secretion through multiple mechanisms. Increasing the glucose concentration modestly decreases [Ca2+]c in α-cells independently of their KATP channels and partly via SST. The involvement of SST increases with the glucose concentration, and one major effect of SST is to keep α-cell [Ca2+]c at low levels by counteracting the effect of an entrainment of α-cells by β-cells when β-cells become stimulated by glucose. All these [Ca2+]c changes induce parallel changes in glucagon release. Glucose also decreases the efficacy of Ca2+ on exocytosis by an attenuating pathway that is opposite to the well-established amplifying pathway controlling insulin release in β-cells.
  • Solids Turn into Liquids-Liquid Eutectic Systems of Pharmaceutics to Improve Drug Solubility. [Journal Article]
    Pharmaceuticals (Basel). 2022 Feb 23; 15(3)Sarraguça MC, Ribeiro PRS, … Seabra CL
  • The low solubility of active pharmaceutical ingredients (APIs) is a problem in pharmaceutical development. Several methodologies can be used to improve API solubility, including the use of eutectic systems in which one of the constituents is the API. This class of compounds is commonly called Therapeutic Deep Eutectic Systems (THEDES). THEDES has been gaining attention due to their properties suc…
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