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glibenclamide

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https://www.readbyqxmd.com/read/29792023/fern-9-11-ene-2%C3%AE-3%C3%AE-diol-action-on-insulin-secretion-in-hyperglycemic-conditions
#1
Allisson Jhonatan Gomes Castro, Luisa Helena Cazarolli, Gabrielle Da Luz, Delsi Altenhofen, Hemily Batista Da Silva, Francieli Kanumfre Carvalho, Moacir Geraldo Pizzolatti, Fátima Rmb Silva
The objective of this study was to investigate the effect and the mechanism of action of fernenediol as insulin secretagogue. Wistar rats were treated with 0.1; 1 and 10 mg/kg fernenediol and then induced hyperglycemia by oral glucose. The glycaemia, insulin, LDH, calcium and hepatic glycogen were analyzed. Considering the intestine and pancreas as targets for the triterpene action, the duodenum was used to verify the influence of fernenediol on intestinal glycosidases. Additionally, pancreatic islets were used for studies of 14 C-deoxyglucose uptake and influx of 45 Ca2+ in hyperglycemic medium with/without fernenediol in the presence/absence of an inhibitor/activator of KATP channels, glibenclamide, diazoxide, nifedipine, calcium chelator (BAPTA- AM) and H-89 and ST the inhibitors of the PKA and PKC enzymes...
May 24, 2018: Biochemistry
https://www.readbyqxmd.com/read/29789393/long-term-outcomes-in-patients-aged-%C3%A2-70-years-with-intravenous-glyburide-from-the-phase-ii-games-rp-study-of-large-hemispheric-infarction-an-exploratory-analysis
#2
Kevin N Sheth, Nils H Petersen, Ken Cheung, Jordan J Elm, Holly E Hinson, Bradley J Molyneaux, Lauren A Beslow, Gordon K Sze, J Marc Simard, W Taylor Kimberly
BACKGROUND AND PURPOSE: We aimed to determine whether subjects aged ≤70 years who were treated with intravenous glyburide (RP-1127; BIIB093; glibenclamide) would have better long-term outcomes than those who received placebo. METHODS: GAMES-RP (Glyburide Advantage in Malignant Edema and Stroke-Remedy Pharmaceuticals) was a prospective, double-blind, randomized, placebo-controlled phase 2 clinical trial. Eighty-six participants, aged 18 to 80 years, who presented to 18 centers with large hemispheric infarction (baseline diffusion-weighted imaging volumes, 82-300 cm3 ) randomized within 10 hours of symptom onset were enrolled...
May 22, 2018: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/29788881/novel-solid-lipid-nanocarrier-of-glibenclamide-a-factorial-design-approach-with-response-surface-methodology
#3
Sonia Pandey, Payal Patel, Arti Gupta
BACKGROUND: In the present investigation a factorial design approach attempt was applied to develop the solid lipid nanoparticles (SLN) of Glibenclamide (GLB) a poorly water-soluble drug (BCS -II) used in the treatment of type 2 diabetes. OBJECTIVES: Prime objectives of this experiment are to optimize the SLN formulation of Glibenclamide and improve the therapeutic effectiveness of the developed formulation. METHODS: Glibenclamide loaded SLNs (GLB-SLN) were fabricated by High speed homogenization technique...
May 21, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29777732/antinociceptive-effect-of-tadalafil-in-various-pain-models-involvement-of-opioid-receptors-and-nitric-oxide-cyclic-gmp-pathways
#4
Mohammad M Mehanna, Souraya Domiati, Hania Nakkash Chmaisse, Ahmed El Mallah
Nitric oxide has been proven to play an important role in nociception, accordingly, its promoters, phosphodiesterase inhibitors have been investigated as pain response modulators. Aiming to evaluate the central effect of tadalafil, a phosphodiesterase 5 inhibitor, and to determine its EC50, tail flick and hot plate tests were utilized. On the other hand, its nociceptive peripheral analgesic effect was assessed through acetic-acid induced writhing model. Formalin test was used to appraise both non-inflammatory and inflammatory pain responses...
May 16, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29777569/improving-metabolic-stability-with-deuterium-the-discovery-of-hwl-066-a-potent-and-long-acting-free-fatty-acid-receptor-1-agonists
#5
Chunxia Liu, Zheng Li, Wei Shi, Huilan Li, Nasi Wang, Yuxuan Dai, Chen Liao, Wenlong Huang, Hai Qian
The free fatty acid receptor 1 (FFA1) is a potential target due to its function in enhancing of glucose-stimulated insulin secretion. The FFA1 agonist GW9508 has great potential for the treatment of type 2 diabetes mellitus, but it has been suffering from high plasma clearance probably because the phenylpropanoic acid is vulnerable to β-oxidation. To identify orally available analog without influence on the unique pharmacological mechanism of GW9508, we tried to interdict the metabolically labile group by incorporating two deuterium atoms at the α-position of phenylpropionic acid affording compound 4 (HWL-066)...
May 18, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29772022/binding-of-sulphonylureas-to-plasma-proteins-a-katp-channel-perspective
#6
Peter Proks, Holger Kramer, Elizabeth Haythorne, Frances M Ashcroft
Sulphonylurea drugs stimulate insulin secretion from pancreatic β-cells primarily by inhibiting ATP sensitive potassium (KATP) channels in the β-cell membrane. The effective sulphonylurea concentration at its site of action is significantly attenuated by binding to serum albumin, which makes it difficult to compare in vitro and in vivo data. We therefore measured the ability of gliclazide and glibenclamide to inhibit KATP channels and stimulate insulin secretion in the presence of serum albumin. We used this data, together with estimates of free drug concentrations from binding studies, to predict the extent of sulphonylurea inhibition of KATP channels at therapeutic concentrations in vivo...
2018: PloS One
https://www.readbyqxmd.com/read/29770541/effect-of-short-term-treatment-with-sitagliptin-or-glibenclamide-on-daily-glucose-fluctuation-in-drug-na%C3%A3-ve-japanese-patients-with-type-2-diabetes-mellitus
#7
Ryo Suzuki, Jun-Ichi Eiki, Takashi Moritoyo, Kenichi Furihata, Akira Wakana, Yukari Ohta, Shigeru Tokita, Takashi Kadowaki
AIMS: To compare the effect of a dipeptidyl peptidase-4 inhibitor (DPP4-i) and a sulfonylurea (SU) on daily glucose fluctuation in drug-naïve Japanese patients with type 2 diabetes mellitus (T2DM). MATERIALS AND METHODS: Fifty-three drug-naïve Japanese patients with T2DM (HbA1c of 7.0% to 9.0% and fasting plasma glucose of 6.1 mmol/L or higher) were randomly assigned to either sitagliptin 50 mg q.d. or glibenclamide 2.5 mg per day (given in divided doses) in a 1:1 ratio...
May 17, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29769061/five-traditional-nigerian-polyherbal-remedies-protect-against-high-fructose-fed-streptozotocin-induced-type-2-diabetes-in-male-wistar-rats
#8
O E Kale, O B Akinpelu, A A Bakare, F O Yusuf, R Gomba, D C Araka, T O Ogundare, A C Okolie, O Adebawo, O Odutola
BACKGROUND: This present study sought to assess the modulatory effects of five Nigerian traditional polyherbal in high fructose-fed, streptozotocin-induced (HF-STZ) Type 2 diabetes (T2D) in rats. T2D was achieved via fructose feeding (20%W/V ) ad libitum for 2 weeks and streptozotocin (STZ, 40 mg/kg) (15th Day) intraperitoneally. METHODS: Seventy-two hours after STZ injection, fourty-eight diabetic rats were divided into eight of 6 rats/group: Diabetic normal untreated, glibenclamide (GBLI, 0...
May 16, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29769013/antidiabetic-effect-of-spearmint-in-streptozotocin-induced-diabetic-rats
#9
Omar Farid, A El Haidani, Mohamed Eddouks
In this work the effect of Mentha spicata (L.) (M. spicata) aerial part aqueous extract (A.P.A.E) at a dose of 20 mg/kg body weight on blood glucose levels has been demonstrated in normal and streptozotocin (STZ) diabetic rats. Additionally, a preliminary phytochemical screening for various bioactive constituents was realized and a dosage of polyphenols and flavonoid has been done. Moreover, the histopathological changes in liver and pancreas have been evaluated both in normal and STZ diabetic rats. The effect of M...
May 16, 2018: Endocrine, Metabolic & Immune Disorders Drug Targets
https://www.readbyqxmd.com/read/29762878/risk-of-hypoglycemia-after-concomitant-use-of-antidiabetic-antihypertensive-and-antihyperlipidemic-medications-a-database-study
#10
Masahiko Gosho
Hypoglycemia is the most important complication of antidiabetic medications. Most patients with diabetes mellitus take multiple medications. In this study, we explored clinical drug-drug interactions that result in hypoglycemia by analyzing the Japanese Adverse Drug Event Report (JADER) database. The primary outcome was the report of hypoglycemia. The Norén and Gosho methods, which quantitatively measure the discrepancy between the observed and expected number of adverse events under the combination of 2 drugs, were used as the criteria for detecting drug-drug interactions...
May 15, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29749986/-urtica-dioica-distillate-regenerates-pancreatic-beta-cells-in-streptozotocin-induced-diabetic-rats
#11
Ali Gohari, Ali Noorafshan, Masoumeh Akmali, Fahimeh Zamani-Garmsiri, Atefeh Seghatoleslam
Background: Urtica dioica is known as an anti-hyperglycemic plant. Urtica dioica distillate (UD) is a traditional Iranian drink, locally known as "aragh gazaneh". In spite of its widespread consumption in Iran, according to traditional Iranian medicine, there is no scientific report on the usefulness of UD for diabetic patients. This survey was designed to evaluate its protective effects for the recovery from diabetes by determining the serum insulin, blood glucose, volume of pancreatic islets, and the number and volume of β-cells in diabetic rats...
March 2018: Iranian Journal of Medical Sciences
https://www.readbyqxmd.com/read/29747754/mechanism-of-resveratrol-induced-relaxation-of-the-guinea-pig-fundus
#12
Ching-Chung Tsai, Shu-Leei Tey, Ming-Che Lee, Ching-Wen Liu, Yu-Tsun Su, Shih-Che Huang
BACKGROUND: Resveratrol is a polyphenolic compound that can be isolated from plants and also is a constituent of red wine. Resveratrol induces relaxation of vascular smooth muscle and may prevent cardiovascular diseases. PURPOSE: Impaired gastric accommodation plays an important role in functional dyspepsia and fundic relaxation and is a therapeutic target of functional dyspepsia. Although drugs for fundic relaxation have been developed, these types of drugs are still rare...
April 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29746136/relative-activity-factor-raf-based-scaling-of-uptake-clearance-mediated-by-organic-anion-transporting-polypeptide-oatp-1b1-and-oatp1b3-in-human-hepatocytes
#13
Saki Izumi, Yoshitane Nozaki, Hiroyuki Kusuhara, Koichiro Hotta, Toshiki Mochizuki, Takafumi Komori, Kazuya Maeda, Yuichi Sugiyama
In vitro-in vivo extrapolation based on uptake clearance determined in human hepatocytes has been used to predict in vivo hepatic clearance of organic anion transporting polypeptide (OATP) substrates. This study evaluated the relative activity factor (RAF) approach to extrapolate active uptake clearance in transporter-transfected cell systems (CLuptake ) to that in human hepatocyte suspensions (PSinf,act ). RAF values for OATP1B1 and OATP1B3 were determined in two batches of cryopreserved human hepatocytes using estrone-3-sulfate and cholecystokinin octapeptide as reference substrates, respectively...
May 10, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29736386/evaluation-of-antinociceptive-antihyperglycemic-and-membrane-stabilizing-activities-of-garcinia-lancifolia-roxb
#14
Antara Ghosh, Sujan Banik, Mohammad Nurul Amin, Jamiuddin Ahmed
This study was undertaken to examine the antinociceptive, antihyperglycemic, and membrane stabilizing activity with phytochemical screening of methanolic extract of Garcinia lanceifolia whole plant. The extracts were subjected to in-vivo antinociceptive, antihyperglycemic activity in laboratory animals and in-vitro membrane stabilizing activity. In peripheral antinociceptive activity, G. lanceifolia (400 and 200 mg/kg) exhibited significant (P < 0.001) inhibition of writhing with 59.15% and 49.30% respectively comparable to standard Diclofenac (54...
April 2018: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/29733860/estradiol-mediates-relaxation-of-porcine-lower-esophageal-sphincter
#15
Ching-Chung Tsai, Shu-Leei Tey, Li-Ching Chang, Yu-Tsun Su, Kai-Jen Lin, Shih-Che Huang
Most pregnant women have symptoms of gastroesophageal reflux disease (GERD) during pregnancy. Postmenopausal hormone replacement therapy is associated with GERD. The effects of estradiol on lower esophageal sphincter (LES) motility and GERD are not clearly known. The purpose of this study is to investigate the effects of estradiol on the motility of the porcine LES. Relaxations of clasp and sling strips of porcine LES caused by estradiol were measured using isometric transducers. We investigated the mechanism of estradiol-induced relaxation of the porcine LES using tetraethylammonium, apamine, iberiotoxin, glibenclamide, KT5720, KT5823, NG-nitro-l-arginine, tetrodotoxin, and ω-conotoxin GVIA...
May 5, 2018: Steroids
https://www.readbyqxmd.com/read/29733479/levosimendan-differentially-modulates-electrophysiological-activities-of-sinoatrial-nodes-pulmonary-veins-and-the-left-and-right-atria
#16
Yung-Kuo Lin, Yao-Chang Chen, Yi-Ann Chen, Jen-Hung Huang, Shih-Ann Chen, Yi-Jen Chen
INTRODUCTION: Calcium overload increases the risk of atrial fibrillation (AF). Levosimedan, a calcium sensitizer, increases myofilament contractility. Clinical reports suggested that levosimendan might increase AF occurrence, but the electrophysiological effects of levosimendan on AF substrates and triggers (pulmonary veins, PVs) are not clear. METHODS AND RESULTS: Conventional microelectrodes were used to record action potentials (APs) in isolated rabbit PVs, sinoatrial nodes (SANs), the left atrium (LA), and right atrium (RA) before and after application of different concentrations of levosimendan with or without milrinone (a phosphodiesterase (PDE) III inhibitor) and glibenclamide (an ATP-sensitive potassium channel (KATP ) inhibitor)...
May 7, 2018: Journal of Cardiovascular Electrophysiology
https://www.readbyqxmd.com/read/29723849/the-mechanism-of-action-of-zingerone-in-the-pacemaker-potentials-of-interstitial-cells-of-cajal-isolated-from-murine-small-intestine
#17
Jung Nam Kim, Hyun Jung Kim, Iksung Kim, Yun Tai Kim, Byung Joo Kim
BACKGROUND/AIMS: Zingerone, a major component found in ginger root, is clinically effective for the treatment of various diseases. Interstitial cells of Cajal (ICCs) are the pacemaker cells responsible for slow waves in the gastrointestinal (GI) tract. We investigated the effects of zingerone on the pacemaker potentials of ICCs to assess its mechanisms of action and its potential as a treatment for GI tract motility disorder. METHODS: We isolated ICCs from small intestines, and the whole-cell patch-clamp configuration was used to record the pacemaker potentials in cultured ICCs...
April 28, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29710541/muscarinic-receptors-nitric-oxide-formation-and-cyclooxygenase-pathway-involved-in-tracheal-smooth-muscle-relaxant-effect-of-hydro-ethanolic-extract-of-lavandula-angustifolia-flowers
#18
Farzaneh Naghdi, Zahra Gholamnezhad, Mohammad Hossein Boskabady, Morteza Bakhshesh
BACKGROUND: Lavandula angustifolia (L. angustifolia) Mill. (Common name Lavender) is used in traditional and folk medicines for the treatment of various diseases including respiratory disorders worldwide. The relaxant effect of the plant on the smooth muscle of some tissues was shown previously. The present study has investigated the role of different receptors and pathways in the relaxant effect of L. angustifolia on tracheal smooth muscle. METHODS: Cumulative concentrations of the hydro-ethanolic extract of L...
April 7, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29708459/betanin-exhibits-significant-potential-as-an-antihyperglycemic-and-attenuating-the-glycoprotein-components-in-streptozotocin-nicotinamide-induced-experimental-rats
#19
Indumathi Dhananjayan, Kathiroli Sujithra, Srinivasan Subramani, Veerasamy Vinothkumar
This study hypothesized to evaluate the effect of betanin, a chromoalkaloid on plasma and altered tissues glycoprotein components in streptozotocin - nicotinamide induced diabetic rats. Diabetes was induced by a single intraperitoneal (i.p.) injection of streptozotocin (45 mg/kg b.w.) dissolved in 0.1 M citrate buffer (pH 4.5) 15 min after the i.p. administration of nicotinamide (110 mg/kg b.w.). Experimental rats were administered betanin at the dose of 20 mg/kg b.w. and glibenclamide (600µg/kg b...
April 30, 2018: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/29686743/antinociceptive-activity-of-methanolic-extract-of-clinacanthus-nutans-leaves-possible-mechanisms-of-action-involved
#20
Zainul Amiruddin Zakaria, Mohammad Hafiz Abdul Rahim, Rushduddin Al Jufri Roosli, Mohd Hijaz Mohd Sani, Maizatul Hasyima Omar, Siti Farah Mohd Tohid, Fezah Othman, Siew Mooi Ching, Arifah Abdul Kadir
Methanolic extract of Clinacanthus nutans Lindau leaves (MECN) has been proven to possess antinociceptive activity that works via the opioid and NO-dependent/cGMP-independent pathways. In the present study, we aimed to further determine the possible mechanisms of antinociception of MECN using various nociceptive assays. The antinociceptive activity of MECN was (i) tested against capsaicin-, glutamate-, phorbol 12-myristate 13-acetate-, bradykinin-induced nociception model; (ii) prechallenged against selective antagonist of opioid receptor subtypes ( β -funaltrexamine, naltrindole, and nor-binaltorphimine); (iii) prechallenged against antagonist of nonopioid systems, namely, α 2 -noradrenergic (yohimbine), β -adrenergic (pindolol), adenosinergic (caffeine), dopaminergic (haloperidol), and cholinergic (atropine) receptors; (iv) prechallenged with inhibitors of various potassium channels (glibenclamide, apamin, charybdotoxin, and tetraethylammonium chloride)...
2018: Pain Research & Management: the Journal of the Canadian Pain Society
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