Journal: Pharmaceuticals

Article Title: Pharmacological Profiling of K ATP Channel Modulators: An Outlook for New Treatment Opportunities for Migraine

doi: 10.3390/ph16020225

Figure Lengend Snippet: Selectivity profiling of reference K ATP inhibitors.

Article Snippet: Diazoxide, levcromakalim, nateglinide, P1075, PNU-37883A, repaglinide, Y-26763, and ZM226600 were purchased from Tocris (Bristol, UK).

Techniques:

Journal: British Journal of Clinical Pharmacology

Article Title: Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism

doi: 10.1111/j.1365-2125.2010.03772.x

Figure Lengend Snippet: Proposed biotransformation pathways for repaglinide with enzymes responsible for each pathway. The bold texts represent the major enzyme involved in the reaction

Article Snippet: Repaglinide, d 5 -repaglinide and gemfibrozil 1-O-glucuronide were purchased from Toronto Research Chemicals (North York, Ontario, Canada).

Techniques:

Journal: British Journal of Clinical Pharmacology

Article Title: Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism

doi: 10.1111/j.1365-2125.2010.03772.x

Figure Lengend Snippet: M2 formation in the presence of CYP3A4, 2C8, HLM, HLS, and mixtures of cytosol and CYP3A4/2C8. Data represent the average of duplicate measurements. A) radiochromatograms of [3H]-repaglinide (0.49 µm) incubated with HLM (0.5 mg ml−1) in the presence of NADPH. B) radiochromatogram of [3H]-repaglinide (0.49 µm) incubated with HLS (2 mg ml−1) in the presence of NADPH. C) relative activities of M2 formation in different enzymatic systems in the absence or presence of cyanide. D) Inhibition of M2 formation in HLS by ketoconazole and montlukast (1 µm each). Control (); montelukast (1 µm) (); ketoconazole (1 µm) (□)

Article Snippet: Repaglinide, d 5 -repaglinide and gemfibrozil 1-O-glucuronide were purchased from Toronto Research Chemicals (North York, Ontario, Canada).

Techniques: Incubation, Inhibition

Journal: British Journal of Clinical Pharmacology

Article Title: Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism

doi: 10.1111/j.1365-2125.2010.03772.x

Figure Lengend Snippet: Radiochromatogram of [3H]-repaglinide (0.49 µm) incubated with 1 million cells ml−1 fresh human primary hepatocytes in suspension for 2 h (A) and the MS2 spectra of RG (B)

Article Snippet: Repaglinide, d 5 -repaglinide and gemfibrozil 1-O-glucuronide were purchased from Toronto Research Chemicals (North York, Ontario, Canada).

Techniques: Incubation

Journal: British Journal of Clinical Pharmacology

Article Title: Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism

doi: 10.1111/j.1365-2125.2010.03772.x

Figure Lengend Snippet: The inhibitory effects of gemfibrozil and itraconazole on the depletion of repaglinide (0.1 µ m initial concentration) formation of M2, M4 and repaglinide glucuronide (RG) in fresh hepatocyte incubations (1 million cells ml −1 )

Article Snippet: Repaglinide, d 5 -repaglinide and gemfibrozil 1-O-glucuronide were purchased from Toronto Research Chemicals (North York, Ontario, Canada).

Techniques: Concentration Assay, Inhibition

Journal: British Journal of Clinical Pharmacology

Article Title: Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism

doi: 10.1111/j.1365-2125.2010.03772.x

Figure Lengend Snippet: Repaglinide glucuronidation activities of different recombinant human UGT enzymes. Repaglinide (0.2 µm) was incubated with 0.25 mg ml−1 UGT for 45 min. Data represent the average of duplicate incubations. The units on the Y-axis are LC/MS peak area ratios of RG vs. internal standard

Article Snippet: Repaglinide, d 5 -repaglinide and gemfibrozil 1-O-glucuronide were purchased from Toronto Research Chemicals (North York, Ontario, Canada).

Techniques: Recombinant, Incubation, Liquid Chromatography with Mass Spectroscopy

Journal: British Journal of Clinical Pharmacology

Article Title: Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism

doi: 10.1111/j.1365-2125.2010.03772.x

Figure Lengend Snippet: A) Repaglinide glucuronidation activities in a panel of individual HLM from 15 donors categorized into three groups based on UGT1A1 allele status. P values shown are from two-tailed unpaired t-test. B) Scatter plot of RG activity vs.β-estradiol-3-O-glucuronidation activity in a panel of HLM. E3G: β-estradiol-3-O-glucuronide. E3G activity was determined previously in the same set of HLM by Zhang et al. [31]. The units on the Y-axis are LC/MS peak area ratios of RG vs. internal standard. *1* (○); *1*28 (); *28* (▵)

Article Snippet: Repaglinide, d 5 -repaglinide and gemfibrozil 1-O-glucuronide were purchased from Toronto Research Chemicals (North York, Ontario, Canada).

Techniques: Two Tailed Test, Activity Assay, Liquid Chromatography with Mass Spectroscopy

Journal: British Journal of Clinical Pharmacology

Article Title: Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism

doi: 10.1111/j.1365-2125.2010.03772.x

Figure Lengend Snippet: A) The inhibition of repaglinide (0.2 µm) glucuronidation in HLM (0.5 mg ml−1) by various concentrations of gemfibrozil. B) the inhibition of repaglinide glucuronidation in selected recombinant UGTs by gemfibrozil (100 µm). Data represent the average of duplicate incubations

Article Snippet: Repaglinide, d 5 -repaglinide and gemfibrozil 1-O-glucuronide were purchased from Toronto Research Chemicals (North York, Ontario, Canada).

Techniques: Inhibition, Recombinant

Journal: British Journal of Clinical Pharmacology

Article Title: Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism

doi: 10.1111/j.1365-2125.2010.03772.x

Figure Lengend Snippet: The inhibition of repaglinide (0.2 µm) glucuronidation in HLM (0.5 mg ml−1) and UGT1A1 (0.25 mg ml−1) at various concentrations of gemfibrozil 1-O-glucuronide with or without 25 min pre-incubation. Data represent mean and standard deviations of triplicate incubations. A) HLM with pre-incubation, B) HLM without pre-incubation, C) UGT1A1 with pre-incubation and D) UGT1A1 without pre-incubation

Article Snippet: Repaglinide, d 5 -repaglinide and gemfibrozil 1-O-glucuronide were purchased from Toronto Research Chemicals (North York, Ontario, Canada).

Techniques: Inhibition, Incubation