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Showing 1-30 of 119 results for "t0891" within Papers
Rajesh H Bahekar et al.
Bioorganic & medicinal chemistry, 15(21), 6782-6795 (2007-08-29)
In the present investigation, two series of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines (2a-l) and thieno[2,3-b]pyridines (3a-l) were designed as analogs of BL 11282 (1). The in vitro glucose dependent insulinotropic activity of all the test compounds was evaluated using RIN5F cell based assay and
Simona Bo et al.
European journal of endocrinology, 169(1), 117-126 (2013-05-11)
Available data about mortality of type 2 diabetic patients treated with different sulphonylureas are scarce and contradictory. We evaluated the associations between all-cause and cause-specific mortality and treatments with different sulphonylureas in a retrospective cohort of type 2 diabetic patients
Francisco J Prado-Prado et al.
Bioorganic & medicinal chemistry, 18(6), 2225-2231 (2010-02-27)
There are many of pathogen parasite species with different susceptibility profile to antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one parasite species. Consequently, predicting the probability with which a drug is active against
Jingwen Gao et al.
Journal of ethnopharmacology, 145(2), 566-572 (2012-12-05)
Cooked rhubarb and wine processed rhubarb are the processed rhubarbs of raw rhizomes from Rheum palmatum L., Rheum tanguticum Maxim. ex Balf. or Rheum officinale Baill. They are clinically used in traditional Chinese medicine to compose anti-diabetic formulas and remove
Aurelie Vivares et al.
Xenobiotica; the fate of foreign compounds in biological systems, 45(1), 29-44 (2014-07-30)
1. The quantitative prediction of the pharmacokinetic parameters of a drug from data obtained using human in vitro systems remains a significant challenge i.e. prediction of metabolic clearance in humans and estimation of the relative contribution of enzymes involved in
T Marras-Marquez et al.
International journal of pharmaceutics, 479(2), 265-276 (2014-12-30)
Pectin-based resistant, interactive and versatile hydrogel vehicles for oral administration have been prepared. These systems are thought to be versatile enough to allow the inclusion of substances (such as the surfactants tested: Pluronic, Tween, Na Lauryl sulphate) that may contribute
Izumi Yamasaki et al.
Biomedical research (Tokyo, Japan), 33(4), 235-242 (2012-09-15)
Kale (Brassica oleracea L. var acephala DC) is a leafy green vegetable belonging to the cabbage family (Brassicaceae) that contains a large amount of health-promoting phytochemicals. There are any reports about the effects of kale ingestion on the chemoprevention function
Nigel Greene et al.
Chemical research in toxicology, 23(7), 1215-1222 (2010-06-18)
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential
Yu-Jin Guo et al.
Die Pharmazie, 69(4), 306-310 (2014-05-06)
Myricetin is one of the main ingredients of Chinese bayberry, which is used as a traditional medicine. The purpose of this study was to find out whether myricetin influences the rat cytochrome P450 (CYP) enzymes (CYP1A2, CYP2C9 and CYP3A4) by
Jeffrey C Davis et al.
Cell reports, 31(6), 107623-107623 (2020-05-14)
Stem cell-derived β (SC-β) cells could provide unlimited human β cells toward a curative diabetes treatment. Differentiation of SC-β cells yields transplantable islets that secrete insulin in response to glucose challenges. Following transplantation into mice, SC-β cell function is comparable
Mi Ran Choi et al.
Biopharmaceutics & drug disposition, 35(5), 264-274 (2014-03-05)
Under hyperlipidemic conditions, there are likely to be alterations in the pharmacokinetics of CYP2C11 substrates following decreased expression of CYP2C11, which is homologous to human CYP2C9. The pharmacokinetics of tolbutamide (TB) and its metabolite 4-hydroxy tolbutamide (4-OHTB) were evaluated as
Renli Teng et al.
International journal of clinical pharmacology and therapeutics, 51(4), 305-312 (2013-02-06)
To assess the effect of ticagrelor on the pharmacokinetics of tolbutamide (a CYP2C9 substrate), and the effect of tolbutamide on ticagrelor pharmacokinetics. In this randomized, double-blind, two-period, crossover study, 23 healthy volunteers received either placebo or ticagrelor 180 mg twice
Ru Feng et al.
Phytomedicine : international journal of phytotherapy and phytopharmacology, 19(12), 1125-1133 (2012-07-24)
Halenia elliptica D. Don is a Tibetan herb and medicinal preparations containing Halenia elliptica have been commonly used for the treatment of hepatitis B virus infection in China. The metabolism of 1-hydroxy-2,3,5-trimethoxy-xanthone (HM-1) to its metabolites is mediated through cytochrome
Xi Huang et al.
PloS one, 9(11), e113819-e113819 (2014-11-27)
Meranzin hydrate (MH), an absorbed bioactive compound from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS), was first isolated in our laboratory and was found to possess anti-depression activity. However, the role of cytochrome P450s (CYPs) in the metabolism of MH
Dong-Lou Liang et al.
Die Pharmazie, 69(4), 301-305 (2014-05-06)
The purpose of this study was to find out whether icaritin influences the effect on rat cytochrome P450 (CYP) enzymes (CYP1A2, CYP2C9, CYP2E1 and CYP3A4) using cocktail probe drugs in vivo. A cocktail solution at a dose of 5 mL/kg
Anne-Charlotte Dubbelman et al.
Journal of chromatography. A, 1374, 122-133 (2014-12-02)
The present study investigated the practical use of modern ultra-high performance liquid chromatography (UHPLC) separation techniques for drug metabolite profiling, aiming to develop a widely applicable, high-throughput, easy-to-use chromatographic method, with a high chromatographic resolution to accommodate simultaneous qualitative and
Sang Yoon Lee et al.
Toxicology letters, 229(1), 33-40 (2014-06-10)
Although cytochrome P450 inhibition is the major drug-drug interaction (DDI) mechanism in clinical pharmacotherapy, DDI of a number of well-established drugs have not been investigated. Rifampicin, isoniazid, pyrazinamide and ethambutol combination therapy inhibits clearance of theophylline in patients with tuberculosis.
Xuelin Zhou et al.
Phytomedicine : international journal of phytotherapy and phytopharmacology, 20(3-4), 367-374 (2012-10-30)
Previous studies have shown that major tanshinones isolated from Danshen (Salvia miltiorrhiza) inhibited human and rat CYP450 enzymes-mediated metabolism of model probe substrates, with potential in causing herb-drug interactions. Miltirone, another abietane type-diterpene quinone isolated from Danshen, has been reported
Yuan Zhang et al.
Die Pharmazie, 70(1), 47-54 (2015-05-16)
Polygonum multiflorum is a traditional Chinese medicinal herb used in clinical medicine to nourish the liver and kidney. However, in recent years, there have been increased reports of clinical adverse reactions associated with Polygonum multiflorum preparations, especially due to liver
Ju-Hee Ryu et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 983-984, 62-67 (2015-01-27)
A suitable liquid chromatography tandem mass spectrometry (LC-MS/MS) method is required to determine pelubiprofen and its active metabolite, trans-alcohol (M-D), in human plasma for pharmacokinetic studies of pelubiprofen preparations. After one-step liquid-liquid extraction (LLE) using methyl tert-butyl ether (MTBE), pelubiprofen
Rafael Gozalbes et al.
Bioorganic & medicinal chemistry, 18(19), 7078-7084 (2010-09-03)
Solubility plays a very important role in the selection of compounds for drug screening. In this context, a QSAR model was developed for predicting water solubility of drug-like compounds. First, a set of relevant parameters for establishing a drug-like chemical
A Guerra et al.
European journal of medicinal chemistry, 45(3), 930-940 (2009-12-22)
A neural model based on a numerical molecular representation using CODES program to predict oral absorption of any structure is described. This model predicts both high and low-absorbed compounds with a global accuracy level of 74%. CODES/ANN methodology shows promising
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this
Philip Reinoß et al.
Current biology : CB, 30(23), 4579-4593 (2020-09-26)
Locomotion requires energy, yet animals need to increase locomotion in order to find and consume food in energy-deprived states. While such energy homeostatic coordination suggests brain origin, whether the central melanocortin 4 receptor (Mc4r) system directly modulates locomotion through motor
David Buttar et al.
Bioorganic & medicinal chemistry, 18(21), 7486-7496 (2010-09-28)
The displacement of probes that bind selectively to subdomains IIA or IIIA on human serum albumin (HSA) by competing compounds has been followed using fluorescence spectroscopy, and has therefore been used to assign a primary binding site for these compounds
Xuejia Zhai et al.
Die Pharmazie, 68(1), 19-26 (2013-03-01)
Cytochrome P450 enzymes are responsible for the oxidative metabolism of most pharmaceutical compounds. A "cocktail" approach which employs simultaneous administration of a mixture of substrates of CYP enzymes was often used to assess the metabolic activity of multiple P450 forms
Shaojun Yang et al.
The Journal of pharmacology and experimental therapeutics, 352(3), 529-540 (2015-01-01)
Sepiapterin reductase (SPR) catalyzes the reduction of sepiapterin to dihydrobiopterin (BH2), the precursor for tetrahydrobiopterin (BH4), a cofactor critical for nitric oxide biosynthesis and alkylglycerol and aromatic amino acid metabolism. SPR also mediates chemical redox cycling, catalyzing one-electron reduction of
Valentina L Kouznetsova et al.
Bioorganic & medicinal chemistry, 19(11), 3320-3340 (2011-05-17)
Organic anion transporter 1 (Oat1), first identified as NKT, is a multispecific transporter responsible for the handling of drugs and toxins in the kidney and choroid plexus, but its normal physiological role appears to be in small molecule metabolite regulation.
Zhiping Lin et al.
Die Pharmazie, 69(7), 537-541 (2014-07-31)
To investigate the influence of scutellarin on the activities of CYP1A2, CYP2C11, CYP2D1, and CYP3A1/2 in rats in vivo. Scutellarin and saline were intravenously administered to male Wistar rats via the caudal vein for 7 days consecutively. On the 8th
Meiling Ye et al.
Nanoscale research letters, 9(1), 642-642 (2014-12-19)
Nano-sized particles are known to interfere with drug-metabolizing cytochrome P450 (CYP) enzymes, which can be anticipated to be a potential source of unintended adverse reactions, but the mechanisms underlying the inhibition are still not well understood. Herein we report a
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