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显示 31-60 共 148 条结果 关于 "G2539" 范围 论文
Ryan Mathias et al.
American journal of physiology. Gastrointestinal and liver physiology, 304(6), G623-G634 (2013-01-01)
Mesenteric lymphatic vessels actively transport lymph, immune cells, fat, and other macromolecules from the intestine via a rhythmical contraction-relaxation process called lymphatic pumping. We have previously demonstrated that mesenteric lymphatic pumping was compromised in the guinea pig model of 2,4,6-trinitrobenzenesulfonic
Sherrie L Aspinall et al.
The American journal of geriatric pharmacotherapy, 9(1), 58-68 (2011-04-05)
The objectives of this study were to describe changes in glyburide prescribing in cohorts that were and were not targeted by a risk reduction project, assess factors associated with glyburide discontinuation, and evaluate changes in glycated hemoglobin (ie, HbA(1c)) levels
Ramya V Shingalapur et al.
European journal of medicinal chemistry, 45(5), 1753-1759 (2010-02-04)
In seeking broad spectrum pharmacological activities of benzimidazole derivatives, a group of 4-thiazolidinones 5(a-j) and 1,3,4-oxadiazoles 6(a-j) containing 2-mercapto benzimidazole moiety were synthesized and screened for in vivo anticonvulsant activity by Maximal Electroshock (MES) model and antidiabetic activity using Oral
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
Manthena V S Varma et al.
Journal of medicinal chemistry, 52(15), 4844-4852 (2009-05-19)
Kidney plays an important role in the elimination of drugs, especially with low or negligible hepatic clearance. An analysis of the interrelation of physicochemical properties and the human renal clearance for a data set of 391 drugs or compounds tested
Ya-Jean Wang et al.
Toxicology letters, 223(2), 139-145 (2013-09-10)
Methamphetamine (MA), a highly abused amphetamine-like psychostimulant, has surged in popularity worldwide in the last decade. Repeated MA exposure has been shown to affect the alternative splice variant expression of large conductance Ca(2+)-activated K(+) (BK) channels. It remains unclear whether
The second generation oral sulfonylureas: glyburide and glipizide.
T Kuhn
American pharmacy, NS28(10), 55-61 (1988-10-01)
Editorial: sulfonylureas differ in effects on ischemic preconditioning--is it time to retire glyburide?
Matthew C Riddle
The Journal of clinical endocrinology and metabolism, 88(2), 528-530 (2003-02-08)
Atul Kumar et al.
Bioorganic & medicinal chemistry, 17(14), 5285-5292 (2009-06-09)
We have designed 1,3-disubstituted-5-membered heteroaromatic ring system as a common core motif from known anti-hyperglycemic agents. Designed compounds were synthesized and screened for in vivo anti-hyperglycemic activity in sucrose loaded model (SLM), sucrose-challenged streptozotocin-induced diabetic rat model (STZ-S) as well
Mariana Torres-Piedra et al.
European journal of medicinal chemistry, 45(6), 2606-2612 (2010-03-30)
The aim of the current study was to investigate the oral antidiabetic activity of six structurally related flavonoids: flavone (1), 3-hydroxyflavone (2), 6-hydroxyflavone (3), 7-hydroxyflavone (4), chrysin (5) and quercetin (6). Normoglycemic and STZ-nicotinamide diabetic rats were treated with these
Hiroe Honda et al.
Journal of leukocyte biology, 96(6), 1087-1100 (2014-09-12)
Inflammasome activation initiates the development of many inflammatory diseases, including obesity and type 2 diabetes. Therefore, agents that target discrete activation steps could represent very important drugs. We reported previously that ILG, a chalcone from Glycyrrhiza uralensis, inhibits LPS-induced NF-κB
R C Palheta et al.
Life sciences, 92(10), 569-575 (2013-01-29)
We previously reported that mechanical atrial stretch (AS) by balloon distention increased gastric tonus in anesthetized rats. The present study evaluated the effect of AS on the gastric emptying of a liquid test meal in awake rats and its underlying
A E Boyd et al.
The American journal of medicine, 89(2A), 3S-10S (1990-08-20)
A high-affinity sulfonylurea receptor has been identified on the plasma membrane of the beta cell. The potent second-generation sulfonylureas, glyburide and glipizide, saturate the receptor in the low nM concentration range, whereas first-generation drugs bind to and saturate the receptor
Mariel Núñez et al.
BMC pharmacology & toxicology, 14, 6-6 (2013-01-15)
Glibenclamide (Gli) binds to the sulphonylurea receptor (SUR) that is a regulatory subunit of ATP-sensitive potassium channels (KATP channels). Binding of Gli to SUR produces the closure of KATP channels and the inhibition of their activity. This drug is widely
Charles J Glueck et al.
Expert opinion on pharmacotherapy, 3(11), 1557-1568 (2002-11-20)
Gestational diabetes (GD) develops because pregnancy increases requirements for insulin secretion while increasing insulin resistance. Women with GD often have impaired pancreatic beta-cell compensation for insulin resistance. The nature of GD is currently contentious, with debate about its existence, diagnosis
Gary N Fox et al.
Cutis, 76(1), 41-45 (2005-09-08)
Lichenoid reactions to sulfonylurea drugs have been reported, albeit infrequently. To our knowledge, this is the first case of a generalized lichenoid dermatitis likely induced by the third-generation sulfonylurea hypoglycemic drug glyburide.
J F Caro
The American journal of medicine, 89(2A), 17S-25S (1990-08-20)
Increased hepatic glucose production is responsible for fasting hyperglycemia in type II diabetes. Insulin resistance is the key in this process because of the inability of insulin to suppress hepatic glucose production, thereby allowing an unopposed glucagon effect. Glyburide, one
Vijay Ramani et al.
Journal of leukocyte biology, 98(6), 1037-1048 (2015-08-09)
Inflammation is induced because of interplay among multiple signaling pathways and molecules during infectious and noninfectious tissue injuries. Crosstalk between Toll-like receptor-4 signaling and the neuronal apoptosis inhibitor protein, major histocompatibility class 2 transcription activator, incompatibility locus protein from Podospora
Ayesha Rashid et al.
Pakistan journal of pharmaceutical sciences, 27(1), 153-159 (2014-01-01)
The study was aimed to evaluate various pharmacokinetic parameters of a commercially available fixed dose combination of oral antidiabetics (Metformin/Glibenclamide 500/5mg tablets) in plasma sample of normal healthy adult male volunteers by applying an accurate, selective, and reproducible HPLC-UV analytical
Mark C Wenlock et al.
Bioorganic & medicinal chemistry letters, 21(12), 3550-3556 (2011-05-24)
In drug discovery projects the ability to show a relationship between a compound's molecular structure and its pharmacokinetic, in vivo efficacy, or toxicity profile is paramount for the design of better analogues. To aid this understanding the measurement of distribution
Sammy W M Shiu et al.
Clinical science (London, England : 1979), 126(2), 175-181 (2013-08-03)
LDL (low-density lipoprotein) is subjected to pro-atherogenic modifications in the circulation. A novel uraemia-independent mechanism of carbamylation of lipoproteins mediated by MPO (myeloperoxidase) has recently been reported. We have investigated whether carbamylation of LDL was increased in patients with Type
Marilia Trindade de Santana et al.
Pharmaceutical biology, 51(9), 1144-1149 (2013-06-26)
Citronellal is a monoterpene present in the oil of many species, including Cymbopogon winterianus Jowitt (Poaceae). The present study investigated the effect of citronellal on inflammatory nociception induced by different stimuli and examined the involvement of the NO-cGMP-ATP-sensitive K⁺ channel
Shilpa Raut et al.
Journal of pharmaceutical and biomedical analysis, 109, 121-127 (2015-03-15)
We are reporting a new methodology of using Raman spectroscopy for studying the drug surfactant interactions in self-emulsifying drug delivery systems (SEDDS). The physicochemical properties of surfactants could affect the performance of drugs from lipid delivery systems. Thus the purpose
Maryam Sharifi-Sanjani et al.
American journal of physiology. Heart and circulatory physiology, 304(10), H1294-H1301 (2013-03-26)
Myocardial metabolites such as adenosine mediate reactive hyperemia, in part, by activating ATP-dependent K(+) (K(ATP)) channels in coronary smooth muscle. In this study, we investigated the role of adenosine A(2A) and A(2B) receptors and their signaling mechanisms in reactive hyperemia.
Zhiwei Cai et al.
American journal of physiology. Cell physiology, 305(8), C817-C828 (2013-06-21)
The chemical structures of the thyroid hormones triiodothyronine (T3) and thyroxine (T4) resemble those of small-molecules that inhibit the cystic fibrosis transmembrane conductance regulator (CFTR) Cl(-) channel. We therefore tested the acute effects of T3, T4 and reverse T3 (rT3)
Eva Bernhart et al.
Biochemical pharmacology, 96(2), 119-130 (2015-05-24)
Glioblastoma is the most common malignant brain tumor, which, despite combined radio- and chemotherapy, recurs and is invariably fatal for affected patients. Members of the sphingolipid (SL) family are potent effectors of glioma cell proliferation. In particular sphingosine-1-phosphate (S1P) and
G Koren
Reproductive toxicology (Elmsford, N.Y.), 15(3), 227-229 (2001-06-08)
Oral hypoglycemics have been avoided in pregnancy due to their potential to cause fetal hyperinsulinemia/hypoglycemia. A recent human study has shown glyburide to minimally cross the placenta, allowing a safe new treatment for gestational diabetes. The mechanisms for the minimal
Ge Li et al.
mBio, 11(6) (2020-12-10)
Successful treatment of HIV-infected patients with combinational antiretroviral therapies (cART) can now prolong patients' lives to nearly normal life spans. However, the new challenge faced by many of those HIV-infected patients is chronic neuroinflammation and neurotoxicity that often leads to
Sarah E Tulk et al.
Journal of cellular biochemistry, 116(5), 711-720 (2015-02-03)
Vitamin D3 has emerged as an important regulator of the immune system. With metabolic enzymes for vitamin D3 activation and vitamin D receptors (VDR) now identified in a variety of immune cells, the active vitamin D3 metabolite 1,25(OH)2D3, is thought
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
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