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glibenclamide

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https://www.readbyqxmd.com/read/29150777/glibenclamide-and-therapeutic-hypothermia-have-comparable-effect-on-attenuating-global-cerebral-edema-following-experimental-cardiac-arrest
#1
Shin Nakayama, Noriko Taguchi, Yumi Isaka, Takako Nakamura, Makoto Tanaka
BACKGROUND: Cerebral edema is one of the major causes of mortality following cardiac arrest (CA) and cardiopulmonary resuscitation (CPR). A subunit of the sulfonylurea receptor 1-transient receptor potential M4 (Sur1-TRPM4) channel has been implicated in the pathogenesis of ischemia-evoked cerebral edema. In this study, we examined whether glibenclamide (GBC), a Sur1-TRPM4 channel inhibitor, attenuates cerebral edema following CA/CPR and further examined the efficacy of GBC combined with therapeutic hypothermia...
November 17, 2017: Neurocritical Care
https://www.readbyqxmd.com/read/29148978/antidiabetic-and-in-vitro-antioxidant-effects-of-hydromethanol-extract-of-paullinia-pinnata-root-bark-in-alloxan-induced-diabetic-rat
#2
Onoja Samuel Okwudili, Nwachukwu Glory Chimaobi, Ezeja Maxwell Ikechukwu, Omeh Yusuf Ndukaku
Background The study evaluated phytochemical composition, antidiabetic, oral glucose tolerance test and in vitro antioxidant activities of hydromethanol extract of Paullinia pinnata root bark. Methods Cold maceration method was used in extract preparation and scavenging of 2,2-diphenyl-1-picrylhydrazyl radicals was used to evaluate antioxidant properties of the extract. Diabetes was induced with alloxan at the dose of 160 mg/kg. The antidiabetic activity of the extract was tested at doses of 50, 100 and 200 mg/kg, and glibenclamide was used as reference drug...
November 17, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/29134983/anti-hyperglycaemic-effects-of-rutin-on-blood-glucose-oxidative-stress-biomarkers-and-lipid-peroxidation-in-alloxan-induced-hyperglycaemic-wistar-rats
#3
Y Tanko, A I Salisu, K A Mohammed, S A Musa, A Jimoh, R Yusuf
The present study investigated the anti-hyperglycaemic effect of rutin on blood glucose, oxidative stressbiomarkers and lipid peroxidation in alloxan induced hyperglycaemic wistar rats. Diabetes was induced in rats by anintraperitoneal (i.p) injection of alloxan monohydrate 150 mg/kg body weight. Twenty five wistar rats were divided asfollows; Group1 served as diabetic control received distilled water 2 mg/kg, Group served as positive control received 2mg/kg glibenclamide, 3, 4 and 5 received rutin at 50, 100 and 200 mg/kg body weight for 28 days respectively...
June 30, 2017: Nigerian Journal of Physiological Sciences: Official Publication of the Physiological Society of Nigeria
https://www.readbyqxmd.com/read/29130561/mechanism-of-action-of-camphoryl-benzene-sulfonamide-derivative-on-glucose-uptake-in-adipose-tissue
#4
Marisa Jádna Silva Frederico, Allisson Jhonatan Gomes Castro, Veronica Aiceles de Medeiros Pinto, Cristiane da Fonte Ramos, Fabíola Branco Filippin Monteiro, Alessandra Mascarello, Ricardo José Nunes, Fátima Regina Mena Barreto Silva
The aim of the present study was to investigate the mechanism of action of a sulfonamide derivative on glucose uptake in adipose tissue, as well as to characterize the effects of this compound on intestinal disaccharidases and advanced glycation end-products (AGEs) formation. Camphoryl-benzene sulfonamide (CS) was able to stimulate glucose uptake in isolated adipocytes, adipose tissue and in soleus muscle. The stimulatory effect of the compound (10 μM) on glucose uptake on adipose tissue was blocked by diazoxide, wortmannin, U73122, colchicine, and N-ethylmaleimide...
November 11, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29128812/pharmacological-evidence-for-the-involvement-of-adenosine-triphosphate-sensitive-potassium-channels-in-chloroquine-induced-itch-in-mice
#5
Sattar Ostadhadi, Arash Foroutan, Nazgol-Sadat Haddadi, Abbas Norouzi-Javidan, Majid Momeny, Ghazaleh Zarrinrad, Seyed Hamid Ghaffari, Ahmad-Reza Dehpour
BACKGROUND: Chloroquine (CQ) evokes itch in human and scratching behavior in rodents through a histamine-independent pathway. Chloroquine directly excites peripheral sensory neurons which convey itch signals to the central nervous system. It has been revealed that ATP-sensitive potassium channels (KATP channels) are important in regulating neuronal excitability. Thus, we aimed to investigate the involvement of KATP channels in CQ-induced itch which may also reveal a linkage between metabolic state of cells and itch...
June 3, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29123442/functional-effects-of-alagebrium-alt-711-isolated-rat-carotid-artery
#6
Cigdem Toprak, Basar Sirmagul, Semra Yigitaslan
Objective: In our study, the effects of glycosylated protein cross-link breaker, alagebrium was investigated on isolated rat carotid artery using myography. Alagebrium showed vasodilator effect on carotid artery rings; particularly, this effect was significantly increased in endothelium-intact rings. Materials and Methods: To clarify the vasodilator mechanism of alagebrium, different antagonists such as N(G)-Nitro-L-arginine methyl ester (L-NAME), glibenclamide, indomethacin, metoprolol, propranolol, tetraethylammonium, and calcium channel activator BAYK-8644 were used to reverse this effect...
October 2017: Eurasian Journal of Medicine
https://www.readbyqxmd.com/read/29119680/nicorandil-regulates-the-macrophage-skewing-and-ameliorates-myofibroblasts-by-inhibition-of-rhoa-rho-kinase-signalling-in-infarcted-rats
#7
Tsung-Ming Lee, Shinn-Zong Lin, Nen-Chung Chang
We have demonstrated that ATP-sensitive potassium (KATP ) channel agonists attenuated fibrosis; however, the mechanism remained unclear. Since RhoA has been identified as a mediator of cardiac fibrosis, we sought to determine whether the anti-fibrotic effects of KATP channel agonists were mediated via regulating macrophage phenotype and fibroblast differentiation by a RhoA/RhoA-kinase-dependent pathway. Wistar male rats after induction of myocardial infarction were randomized to either vehicle, nicorandil, an antagonist of KATP channel glibenclamide, an antagonist of ROCK fasudil, or a combination of nicorandil and glibenclamide or fasudil and glibenclamide starting 24 hrs after infarction...
November 9, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29080465/antihyperglycemic-effect-of-hesperetin-a-citrus-flavonoid-extenuates-hyperglycemia-and-exploring-the-potential-role-in-antioxidant-and-antihyperlipidemic-in-streptozotocin-induced-diabetic-rats
#8
Revathy Jayaraman, Srinivasan Subramani, Shahul Hameed Sheik Abdullah, Muruganathan Udaiyar
Diabetes is the major health problem in modern civilization which occurs due to inadequate metabolism of carbohydrate and lipid could cause tremendous changes in the metabolic activities of liver. In this study, we investigated the antihyperglycemic, antioxidant and antihyperlipidemic effects of hesperetin, a citrus flavonoid against streptozotocin (STZ)-induced experimental rats. To stimulate diabetes mellitus, rats were injected with STZ intraperitoneally at a single dose of 45mg/kg. STZ induced rats showed marked increase in the level of plasma glucose and significant reduction in the level of plasma insulin...
October 31, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29080222/free-fatty-acid-receptor-1-agonist-mr1704-lowers-blood-glucose-levels-in-rats-unresponsive-to-the-sulfonylurea-glibenclamide
#9
Naoto Tsuda, Atsuko Kawaji, Mitsuhiro Takagi, Chika Higashi, Masaki Nakamura, Yoshitaka Hosaka, Junichi Sakaki
Preclinical Research & Development MR1704 is a selective G protein-coupled receptor 40/free fatty acid receptor 1 agonist, which exhibited favorable pharmacokinetic profiles and glucose-lowering effects in animal models. We studied the effects of MR1704 in a sulfonylurea-desensitized Sprague-Dawley rat model and evaluated the risk of pancreatic β-cell exhaustion compared to that of glibenclamide in Zucker fatty rats. Rats fed ad libitum a diet containing 0.03% glibenclamide exhibited lower non-fasting blood glucose levels compared to those in rats fed a control diet during the first 6 days...
October 27, 2017: Drug Development Research
https://www.readbyqxmd.com/read/29076435/andrographolide-reorganise-hyperglycaemia-and-distorted-antioxidant-profile-in-streptozotocin-induced-diabetic-rats
#10
Ramavat Ravindhar Naik, Praveen Kumar Munipally, Turlapati Nagaraju
Diabetes mellitus (DM) is a constant and illimitable metabolic disorder that can happen even at a young age due to the virtual absence of naturally acting insulin, which uptakes and accumulates glucose; thereby reduce the use of glucose. In the present study, we evaluated the neuroprotective efficacy of andrographolide on streptozotocin (STZ) induced diabetic Sprague dawley rats. Diabetes was induced by intraperitonial injection of STZ (45 mg/kg B.W) in Sprague dawley rats. Andrographolide (2.5 mg/kg B.W) was administered orally to diabetic rats and Glibenclamide (25mg/kg B...
October 26, 2017: Cardiovascular & Hematological Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29069819/comparison-of-twelve-single-drug-regimens-for-the-treatment-of-type-2-diabetes-mellitus
#11
Shao-Lian Wang, Wen-Bin Dong, Xiao-Lin Dong, Wen-Min Zhu, Fang-Fang Wang, Fang Han, Xin Yan
We performed a network meta-analysis to compare the efficacy of 12 single-drug regimens (Glibenclamide, Glimepiride, Pioglitazone, Rosiglitazone, Repaglinide, Metformin, Sitaglitin, Exenatide, Liraglutide, Acarbose, Benfluorex, and Glipizide) in the treatment of type 2 diabetes mellitus (T2DM). Fifteen relevant randomized controlled trials (RCTs) were included; direct and indirect evidence from these studies was combined, and weighted mean difference (WMD) and surface under the cumulative ranking curves (SUCRAs) were examined to evaluate the monotherapies...
September 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/29066416/a-novel-danshensu-tetramethylpyrazine-derivative-induces-vasorelaxation-on-rat-aorta-and-exerts-cardioprotection-in-dogs
#12
Benhong Xu, Huixing Deng, Xiaojing Zhang, Jingxiong Luo, Gaoxiao Zhang, Zaijun Zhang, Yuqiang Wang, Luchen Shan
ADTM, a previously reported novel Danshensu (DSS)/tetramethylpyrazine (TMP) derivative with cardioprotective and antiplatelet aggregative effects, is a promising therapeutic candidate for ischemic heart diseases. In the present study, ADTM increased coronary blood flow and protected myocardium against ischemic injury in dogs. In addition, the relaxing effect of ADTM on rat thoracic aorta and its underlying mechanisms were examined. ADTM relaxed KCl- and phenylephrine-precontracted arotic rings in a concentration-dependent manner...
October 21, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29062801/effects-of-ethanolic-extract-of-jasminum-grandiflorum-linn-flowers-on-wound-healing-in-diabetic-wistar-albino-rats
#13
Hiren Hirapara, Vishal Ghori, Ashish Anovadiya, Seema Baxi, Chandrabhanu Tripathi
OBJECTIVE: To evaluate wound healing activity of ethanolic extract of Jasminum grandiflorum Linn. (J. grandiflorum) flowers in diabetic rats. MATERIALS AND METHODS: Streptozotocin-induced diabetic Wistar albino rats were divided into six groups (n=6).Three groups - diabetic control, positive control (that received Glibenclamide) and treatment (that received J. grandiflorum Linn. Flower extract) were operated for excision wounds (EW). These groups were evaluated for wound contraction and re-epithelization...
September 2017: Avicenna Journal of Phytomedicine
https://www.readbyqxmd.com/read/29056256/glibenclamide-inhibits-nlrp3-inflammasome-mediated-il-1%C3%AE-secretion-in-human-trophoblasts
#14
Kazuhiro Tamura, Gen Ishikawa, Mikihiro Yoshie, Wakana Ohneda, Akihito Nakai, Toshiyuki Takeshita, Eiichi Tachikawa
Infection-associated pregnancy complications cause premature delivery. Caspase-1 is involved in the maturation of interleukin (IL)-1β, which is activated by the NLRP3 inflammasome. To characterize the significance of the NLRP3 inflammasome pathway in the placenta, the effects of activators and inhibitors on NLRP3-related molecules were examined using isolated primary trophoblasts. Caspase-1 and IL-1β mRNA expression was markedly increased in response to lipopolysaccharide (LPS), a toll-like receptor (TLR)4 ligand...
October 6, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29042208/antiallodynic-activity-of-leflunomide-is-partially-inhibited-by-naltrexone-and-glibenclamide-and-associated-with-reduced-production-of-tnf-%C3%AE-and-cxcl-1
#15
Ana Mercy S Brito, Adriana M Godin, Paulo Sérgio A Augusto, Raquel R Menezes, Ivo S F Melo, Marcela G M B Dutra, Sarah O A M Costa, Franciele A Goulart, Felipe F Rodrigues, Marcela Ísis Morais, Renes R Machado, Márcio M Coelho
Leflunomide, an immunosuppressive drug approved for the treatment of patients with rheumatoid arthritis, exhibits many mechanisms which may affect the nociceptive processing. Therefore, the present study aimed to evaluate the effect induced by leflunomide on the mechanical allodynia in models of inflammatory and neuropathic pain in mice and investigate mechanisms mediating such effects. Per os (p.o.) administration of leflunomide (25, 50 or 100mg/kg) inhibited the inflammatory edema and mechanical allodynia induced by intraplantar carrageenan...
October 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29035201/anti-diabetic-drug-binding-site-in-a-mammalian-katp-channel-revealed-by-cryo-em
#16
Gregory M Martin, Balamurugan Kandasamy, Frank DiMaio, Craig Yoshioka, Show-Ling Shyng
Sulfonylureas are anti-diabetic medications that act by inhibiting pancreatic KATP channels composed of SUR1 and Kir6.2. The mechanism by which these drugs interact with and inhibit the channel has been extensively investigated, yet it remains unclear where the drug binding pocket resides. Here, we present a cryo-EM structure of a hamster SUR1/rat Kir6.2 channel bound to a high-affinity sulfonylurea drug glibenclamide and ATP at 3.63 Å resolution, which reveals unprecedented details of the ATP and glibenclamide binding sites...
October 24, 2017: ELife
https://www.readbyqxmd.com/read/29028586/ameliorative-effect-of-borneol-a-natural-bicyclic-monoterpene-against-hyperglycemia-hyperlipidemia-and-oxidative-stress-in-streptozotocin-induced-diabetic-wistar-rats
#17
Kodikonda Madhuri, Prakash Ramachandra Naik
Diabetes mellitus is a major public health problem worldwide. Oxidative stress plays a pivotal role in the pathogenesis of diabetes as it is one of the inevitable outcomes of the cellular process. The present study aims to investigate the putative antihyperglycemic, antihyperlipidemic and antioxidant efficacy of a monoterpene borneol, in comparison with glibenclamide, a standard drug for therapy of diabetes. Diabetes was induced by a single intraperitoneal injection of 40mg/kg body weight. The results of the present study showed a significant increase in the biochemical indices viz...
October 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29025046/decreased-insulin-secretion-in-pregnant-rats-fed-a-low-protein-diet
#18
Haijun Gao, Eric Ho, Meena Balakrishnan, Vijay Yechoor, Chandra Yallampalli
Low protein (LP) diet during pregnancy leads to reduced plasma insulin levels in rodents, but the underlying mechanisms remain unclear. Glucose is the primary insulin secretagogue, and enhanced glucose-stimulated insulin secretion (GSIS) in beta cells contributes to compensation for insulin resistance and maintenance of glucose homeostasis during pregnancy. In this study, we hypothesized that plasma insulin levels in pregnant rats fed LP diet are reduced due to disrupted GSIS of pancreatic islets. We first confirmed reduced plasma insulin levels, then investigated in vivo insulin secretion by glucose tolerance test and ex vivo GSIS of pancreatic islets in the presence of glucose at different doses, and KCl, glibenclamide, and L-arginine...
October 1, 2017: Biology of Reproduction
https://www.readbyqxmd.com/read/29024691/mechanisms-involved-in-the-increased-sensitivity-of-the-rabbit-basilar-artery-to-atrial-natriuretic-peptide-in-diabetes
#19
Mikahela A López-Morales, José M Centeno, Teresa Jover-Mengual, Vannina G Marrachelli, María C Burguete, María Castelló-Ruiz, Alicia Aliena-Valero, Enrique Alborch, Germán Torregrosa, Juan B Salom, Francisco J Miranda
Atrial natriuretic peptide (ANP) is a vasodilator with significant regional differences and controversial effects in the cerebral circulation, a vascular bed particularly prone to diabetes-induced complications. The present study has investigated how alloxan-induced diabetes modifies the mechanisms involved in the response of the rabbit basilar artery to ANP. ANP (10(-12)-10(-7)M) relaxed precontracted basilar arteries, with higher potency in diabetic than in control rabbits. In arteries from both groups of animals, endothelium removal reduced ANP-induced relaxations...
October 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28987074/combination-of-rheum-ribes-and-metformin-against-diabetes-thermal-hyperalgesia-and-tactile-allodynia-in-a-mice-model
#20
Karim Raafat, Abdalla El-Lakany
Context • The prevalence of diabetes mellitus (DM) is increasing. Because of its progressive nature, therapeutic shifts and combinations are often required to reduce the risk of glucose toxicity and avoid serious side effects. To treat DM and its related complications, a combination therapy may offer a promising remedy to counteract those issues. Objectives • The study was established to evaluate the phytochemical content of a standardized aqueous extract of Rheum ribes (RR) and to determine the antidiabetic, antihyperalgesic, and antimechanical allodynic effects of 50 mg/kg of RR alone, 25 mg/kg of metformin (MTF) alone, and a combination of the 2 substances (MTF+RR) in mice with alloxan-induced diabetes...
October 2, 2017: Alternative Therapies in Health and Medicine
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