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Poonam Shukla et al.
Bioorganic & medicinal chemistry letters, 17(3), 799-802 (2006-11-11)
A series of chalcone based aryloxypropanolamines were synthesized and evaluated for their antihyperglycemic activity in SLM and STZ rat models. Most of the compounds exhibited moderate to good activity ranging from 6.5% to 31.1% in SLM and 8.3% to 22.6%
Nagaraj Kerur et al.
Investigative ophthalmology & visual science, 54(12), 7395-7401 (2013-10-12)
Accumulation of Alu RNA transcripts due to DICER1 deficiency in the retinal pigmented epithelium (RPE) promotes geographic atrophy. Recently we showed that Alu RNA activated the NLRP3 inflammasome, leading to RPE cell death via interleukin-18 (IL-18)-mediated MyD88 signaling. However, the
Gaetano Santulli et al.
The Journal of clinical investigation, 125(5), 1968-1978 (2015-04-07)
The type 2 ryanodine receptor (RyR2) is a Ca2+ release channel on the endoplasmic reticulum (ER) of several types of cells, including cardiomyocytes and pancreatic β cells. In cardiomyocytes, RyR2-dependent Ca2+ release is critical for excitation-contraction coupling; however, a functional
Glyburide-induced cholestatic hepatitis and liver failure. Case-report and review of the literature.
J P van Basten et al.
The Netherlands journal of medicine, 40(5-6), 305-307 (1992-06-01)
As sulphonylurea derivatives are used ubiquitously, the possibility that they may cause liver disease deserves attention. In contrast to the known pattern of reversible parenchymal liver disease due to sulphonylurea derivatives, we describe a fatal case of glyburide-induced cholestatic hepatitis
Montserrat Balsells et al.
BMJ (Clinical research ed.), 350, h102-h102 (2015-01-23)
To summarize short term outcomes in randomized controlled trials comparing glibenclamide or metformin versus insulin or versus each other in women with gestational diabetes requiring drug treatment. Systematic review and meta-analysis. Randomized controlled trials that fulfilled all the following: (1)
Vincenzo Calderone et al.
Bioorganic & medicinal chemistry, 17(15), 5426-5432 (2009-07-15)
Endothelial dysfunction and consequent reduction of biosynthesis of endogenous nitric oxide (NO) play an important pathogenetic role in the cardiovascular complications associated with type II diabetes. In this work, the hybrid drugs 3a and 3b, nitrooxymethylbenzoate-derivatives of 1 (which is
Ihab T Abdel-Raheem et al.
Basic & clinical pharmacology & toxicology, 113(3), 158-166 (2013-04-30)
Doxorubicin is a chemotherapeutic drug used to treat solid and haematopoietic tumours. Its use is limited by a major side effect of cardiotoxicity. It was reported that doxorubicin-induced cardiotoxicity is mediated through oxidative stress coupled with impaired NO bioavailability and
Nir Melamed et al.
Women's health (London, England), 5(6), 649-658 (2009-10-30)
Until the last decade, oral hypoglycemic agents have not been recommended in pregnancy owing to fear of their potential adverse fetal effects, including teratogenicity and neonatal hypoglycemia. However, the evidence in support of these recommendations is weak and is principally
Brice-Loïc Renard et al.
European journal of medicinal chemistry, 46(5), 1935-1941 (2011-03-15)
In the study of previously reported modulators of CFTR chloride channels that are cyclic methylglyoxal (MG) diadducts (CMGD) to aromatic α-aminoazaheterocycles, we optimized a new expeditious one pot route for preparing in water novel aromatic polycyclic azaheterocycles and described 5-pyrimidinols
Ruchira M Jha et al.
Journal of neurotrauma, 38(5), 628-645 (2020-11-19)
Glibenclamide (GLY) is the sixth drug tested by the Operation Brain Trauma Therapy (OBTT) consortium based on substantial pre-clinical evidence of benefit in traumatic brain injury (TBI). Adult Sprague-Dawley rats underwent fluid percussion injury (FPI; n = 45), controlled cortical impact (CCI;
Shuwen Jiang et al.
Drug metabolism and pharmacokinetics, 30(3), 240-246 (2015-04-22)
Accumulating evidences have shown that diabetes is often accompanied with depression, thus it is possible that oral antidiabetic agent glyburide and antidepressive agent paroxetine are co-administered in diabetic patients. The aim of this study was to assess interactions between glyburide
Charles E Norton et al.
American journal of physiology. Lung cellular and molecular physiology, 315(2), L212-L226 (2018-03-16)
The sensory neurotransmitter calcitonin gene-related peptide (CGRP) is associated with vasodilation of systemic arteries through activation of ATP-sensitive K+ (KATP) channels in smooth muscle cells (SMCs); however, its effects on endothelial cell (EC) membrane potential ( Vm) are unresolved. In
Carlos A Aguilar-Salinas et al.
Metabolism: clinical and experimental, 62(5), 638-641 (2013-01-01)
To test the hypothesis that persons with the R230C allele of ABCA1 show a decreased glycemic response to glyburide. This polymorphism is exclusively found in Ameri-indian populations and is associated with type 2 diabetes. This is a single blind controlled
Shay Eliahu et al.
Journal of medicinal chemistry, 53(6), 2472-2481 (2010-02-24)
Dinucleoside polyphosphates exert their physiological effects via P2 receptors (P2Rs). They are attractive drug candidates, as they offer better stability and specificity compared to nucleotides, the most common P2 receptor ligands. The activation of pancreatic P2Y receptors by nucleotides increases
Faiyaz Shakeel et al.
Pharmaceutical development and technology, 19(7), 799-805 (2013-08-24)
The present study was undertaken to evaluate the impact of various combinations of nonionic surfactants on self-nanoemulsifying performance of two grades of Lauroglycol (Lauroglycol-90 and Lauroglycol-FCC) in glibenclamide (GBN) nanoemulsion. Formulations (L1-L30) were prepared by spontaneous emulsification method. Prepared formulations
Rajanbabu Venugopal et al.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, 36(5), 2012-2024 (2015-07-24)
Neuregulin (NRG)-1-human epidermal receptor (HER)-2 signaling pathway is a key regulator of IL-1β-mediated pulmonary inflammation and epithelial permeability. The inflammasome is a newly discovered molecular platform required for caspase-1 activation and maturation of IL-1β. However, the role of the inflammasome
Z Wojnarowska et al.
Physical review. E, Statistical, nonlinear, and soft matter physics, 86(6 Pt 2), 067104-067104 (2013-02-02)
Rheological measurements have been applied to study the tautomerization of the pharmaceutically active compound glibenclamide. The rate constant and activation energy of the imidic-acid-amide transformation have been successfully determined by monitoring the evolution of shear viscosity. The kinetic parameters from
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
Diana L Shuster et al.
Biochemical pharmacology, 92(4), 690-700 (2014-12-03)
Glyburide is commonly prescribed for the treatment of gestational diabetes mellitus; however, fetal exposure to glyburide is not well understood and may have short- and long-term consequences for the health of the child. Glyburide can cross the placenta; fetal concentrations
Wenbo Zhang et al.
PloS one, 9(9), e107639-e107639 (2014-09-13)
Myocardial contractile dysfunction in sepsis is associated with the increased morbidity and mortality. Although the underlying mechanisms of the cardiac depression have not been fully elucidated, an exaggerated inflammatory response is believed to be responsible. Nucleotide-binding oligomerization domain-like receptor containing
Atma P Dwivedi et al.
Bioorganic & medicinal chemistry letters, 18(7), 2301-2305 (2008-03-21)
A series of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines were synthesized and evaluated for their antihyperglycemic activity. Compounds 3g and 6d exhibited lowering of postprandial plasma glucose by 30.7%, 23.3% in SLM and 25.6%, 25.4% in STZ models respectively which is significant
[Diagnosis and treatment of type 2 diabetes from the perspective of guidelines].
M Kellerer
Deutsche medizinische Wochenschrift (1946), 139(21), 1114-1115 (2014-05-16)
Carlo Marchetti et al.
Journal of cardiovascular pharmacology, 66(1), 1-8 (2015-04-29)
Sterile inflammation resulting from myocardial injury activates the NLRP3 inflammasome and amplifies the inflammatory response mediating further damage. We used 2 experimental models of ischemic injury (acute myocardial infarction [AMI] with and without reperfusion) and a model of nonischemic injury
Séverin Slove et al.
Hypertension (Dallas, Tex. : 1979), 62(4), 794-801 (2013-08-07)
Hypertension is a cardiovascular disorder that appears in more than half of the patients with Williams-Beuren syndrome, hemizygous for the elastin gene among 26 to 28 other genes. It was shown that the antihypertensive drug minoxidil, an ATP-dependent potassium channel
McGuinness OP; discussion 51S-53S et al.
The American journal of medicine, 89(2A), 26S-37S (1990-08-20)
Glyburide, along with the other second-generation oral hypoglycemic agent glipizide, has been used as adjunctive therapy for the treatment of non-insulin-dependent diabetes mellitus. After glyburide therapy, basal glycemia and glucose response to a meal are greatly improved. The mechanism for
A Ahmadi et al.
Drug research, 63(12), 614-619 (2013-07-06)
In this study, new glibenclamide analogues (5a-d) with substituted pharmacological triethoxysilyl propan, allyl and ethoxyphenyl groups for cyclohexyl moiety have been synthesized by condensing sulfonamide (4) with related isocyanate or isothiocyanate's compounds. The newly synthesized drugs were evaluated for their
Nandita Sinha et al.
European journal of medicinal chemistry, 46(2), 618-630 (2010-12-28)
A QSAR based predictive model of hERG activity in terms of 'global descriptors' has been developed and evaluated. The QSAR was developed by training 77 compounds covering a wide range of activities and was validated based on an external 'test
Gustav Ahlin et al.
Journal of medicinal chemistry, 51(19), 5932-5942 (2008-09-16)
The liver-specific organic cation transport protein (OCT1; SLC22A1) transports several cationic drugs including the antidiabetic drug metformin and the anticancer agents oxaliplatin and imatinib. In this study, we explored the chemical space of registered oral drugs with the aim of
Sol Cristians et al.
Journal of natural products, 72(3), 408-413 (2009-01-15)
The CH(2)Cl(2)-MeOH (1:1) extract of the leaves of Hintonia standleyana and H. latiflora caused significant decrease in blood glucose levels in both normal and streptozotozin (STZ)-induced diabetic rats when compared with vehicle-treated groups (p < 0.05). These extracts were not
Yi-Ling Hsieh et al.
Journal of pharmaceutical sciences, 103(9), 2724-2735 (2014-02-08)
The aim of this study was to investigate the pH-induced precipitation behavior of four ionizable compounds (papaverine, dipyridamole, glyburide, and warfarin) in the absence and presence of polymers. Polymers selected included nonionic, anionic, and cationic polymers. Precipitates were analyzed immediately
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