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glibenclamide

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https://www.readbyqxmd.com/read/27906419/sch-79797-a-selective-par1-antagonist-protects-against-ischemia-reperfusion-induced-arrhythmias-in-the-rat-hearts
#1
O Y Mohamed, A A Al-Masri, E A El Eter, R Lateef
OBJECTIVE: Thrombin is implicated in the genesis of arrhythmias and activation of thrombin receptors exacerbated ventricular arrhythmias following coronary artery ligation. The present study was designed to investigate the possible protective effect of the protease-activated receptor-1 antagonist, SCH79797 against ischemia and reperfusion arrhythmias in the rat heart. MATERIALS AND METHODS: Healthy male Wistar rats (250-350 g) were anesthetized with urethane. Coronary artery ligation was performed for 5 minutes followed by 10 minutes reperfusion...
November 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/27905383/-the-role-of-atp-dependent-potassium-channels-and-nitric-oxide-system-in-the-neuroprotective-effect-of-preconditioning
#2
O G Deryagin, S A Gavrilova, S V Buravkov, V V Andrianov, G G Yafarova, Kh L Gainutdinov, V B Koshelev
AIM: To study a role of ATP-dependent potassium channels (K+ATP) in the neuroprotective effect of ischemic (IP) and pharmacological (PP) preconditioning and evaluate the dynamics of blood nitric oxide (NO) metabolites in cerebral ischemia. MATERIAL AND METHODS: A model of ischemic stroke induced by the electrocoagulation of a middle cerebral artery (MCA) branch was used in male rats (n=86). Glibenclamide, a selective inhibitor of ATP-sensitive K+ channels, and diazoxide, a potassium channel activator, were used...
2016: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
https://www.readbyqxmd.com/read/27891351/evaluation-of-effect-of-nishamalaki-on-stz-and-hfhf-diet-induced-diabetic-neuropathy-in-wistar-rats
#3
Jayshree Shriram Dawane, Vijaya Anil Pandit, Madhura Shirish Kumar Bhosale, Pallawi Shashank Khatavkar
INTRODUCTION: Diabetic neuropathy is one of the most common complications affecting 50% of diabetic patients. Neuropathic pain is the most difficult types of pain to treat. There is no specific treatment for neuropathy. Nishamalaki (NA), combination of Curcuma longa and Emblica officinalis used to treat Diabetes Mellitus (DM). So, efforts were made to test whether NA is useful in prevention of diabetic neuropathy. AIM: To evaluate the effect of NA on diabetic neuropathy in type 2 diabetic wistar rats...
October 2016: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/27887948/s-allyl-cysteine-ameliorates-cognitive-deficits-in-streptozotocin-diabetic-rats-via-suppression-of-oxidative-stress-inflammation-and-acetylcholinesterase
#4
Tourandokht Baluchnejadmojarad, Zahra Kiasalari, Siamak Afshin-Majd, Zahra Ghasemi, Mehrdad Roghani
Diabetes mellitus (DM) is associated with learning, memory, and cognitive deficits. S-allyl cysteine (SAC) is the main organosulfur bioactive molecule in aged garlic extract with anti-diabetic, antioxidant, anti-inflammatory and nootropic property. This research was conducted to evaluate the efficacy of SAC on alleviation of learning and memory deficits in streptozotocin (STZ)-diabetic rats and to explore involvement of toll-like receptor 4 (TLR4), nuclear factor (erythroid-derived 2)-like 2 (Nrf2), nuclear factor-kappa B (NF-κB), and heme oxygenase 1 (HO-1) signaling cascade...
November 22, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27872020/niclosamide-ethanolamine-inhibits-artery-constriction
#5
Shan-Liang Li, Jie Yan, Yan-Qiu Zhang, Chang-Lin Zhen, Ming-Yu Liu, Jing Jin, Jin-Lai Gao, Xiao-Lin Xiao, Xin Shen, Yu Tai, Nan Hu, Xin-Zi Zhang, Zhi-Jie Sun, De-Li Dong
We previously demonstrated that the typical mitochondrial uncoupler carbonyl cyanide m-chlorophenylhydrazone (CCCP) inhibited artery constriction, but CCCP was used only as a pharmacological tool. Niclosamide is an anthelmintic drug approved by FDA. Niclosamide ethanolamine (NEN) is a salt form of niclosamide and has been demonstrated to uncouple mitochondrial oxidative phosphorylation. The aim of the present study was to elucidate the vasoactivity of NEN and the potential mechanisms. Isometric tension of rat mesenteric artery and thoracic aorta was recorded by using multi-wire myograph system...
November 18, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27871266/antioxidant-antidiarrheal-hypoglycemic-and-thrombolytic-activities-of-organic-and-aqueous-extracts-of-hopea-odorata-leaves-and-in-silico-pass-prediction-of-its-isolated-compounds
#6
Mohammad Shah Hafez Kabir, Mohammed Munawar Hossain, Md Imtiazul Kabir, Shabbir Ahmad, Nishan Chakrabarty, Md Atiar Rahman, Md Mominur Rahman
BACKGROUND: Hopea Odorata, locally known as Telsur (Bangladesh), has some traditional uses as folk medicine. This study aims to investigate the antioxidant, antidiarrheal, hypoglycemic and thrombolytic activities of H. odorata leaf extracts as new therapeutic prospects predicting the activity of some of the isolated compounds of this plant. METHODS: Leaves of Hopea odorata was extracted with pure methanol (MEHO), ethanol (EEHO) and water (AEHO). The extract was tested for antioxidant activity by using reducing power and H2O2 scavenging assay...
November 21, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27866687/glibenclamide-nanocrystals-in-a-biodegradable-chitosan-patch-for-transdermal-delivery-engineering-formulation-and-evaluation
#7
Hany S M Ali, Ahmed F Hanafy
Glibenclamide (GBD) nanocrystals (D50 = 429 nm) were engineered by applying combined precipitation and homogenization procedures. GBD crystallinity was maintained during the nanonization process as revealed by differential scanning calorimetry and X-ray analyses. Nanonized and micronized GBD were incorporated into chitosan solutions to fabricate transdermal delivery systems (TDDSs), nano- and micro-GBD, respectively. The fabricated TDDSs displayed satisfactory physicochemical characteristics without substantial aggregation of GBD nanocrystals during the casting and drying procedures...
November 17, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27851890/levosimendan-exerts-anticonvulsant-properties-against-ptz-induced-seizures-in-mice-through-activation-of-nnos-no-pathway-role-for-katp-channel
#8
Maziar Gooshe, Mohammad Tabaeizadeh, Ali Reza Aleyasin, Payam Mojahedi, Keyvan Ghasemi, Farbod Yousefi, Ali Vafaei, Hossein Amini Khoyi, Shayan Amiri, Ahmad Reza Dehpour
AIMS: Although approving new anticonvulsants was a major breakthrough in the field of epilepsy control, so far we have met limited success in almost one third of patients suffering from epilepsy and a definite and reliable method is yet to be found. Levosimendan demonstrated neuroprotective effects and reduced mortality in conditions in which seizure can be an etiology of death; however, the underlying neuroprotective mechanisms of levosimendan still eludes us. In the light of evidence suggesting levosimendan can be a KATP channel opener and nitrergic pathway activator, levosimendan may exert antiseizure effects through KATP channels and nitrergic pathway...
November 13, 2016: Life Sciences
https://www.readbyqxmd.com/read/27848204/securigenin-glycosides-as-hypoglycemic-principles-of-securigera-securidaca-seeds
#9
Zahra Tofighi, Fahimeh Moradi-Afrapoli, Samad Nejad Ebrahimi, Saied Goodarzi, Abbas Hadjiakhoondi, Markus Neuburger, Matthias Hamburger, Mohammad Abdollahi, Narguess Yassa
Seeds of Securigera securidaca (Fabaceae) are used in Iranian folk medicine as an antidiabetic treatment. In this study, the antihyperglycemic activity of chloroform and methanol fractions (CF and MF) from S. securidaca seed extract was investigated and their bioactive constituents were identified. The antidiabetic effects of fractions were assessed by streptozocin-induced diabetic Naval Medical Research Institute mice. The hypoglycemic activity of MF at 100 mg/kg and CF at 400 mg/kg was comparable with glibenclamide (3 mg/kg)...
November 15, 2016: Journal of Natural Medicines
https://www.readbyqxmd.com/read/27847209/in-vivo-study-for-anti-hyperglycemic-potential-of-aqueous-extract-of-basil-seeds-ocimum-basilicum-linn-and-its-influence-on-biochemical-parameters-serum-electrolytes-and-haematological-indices
#10
Sachin Chaudhary, Amit Semwal, Hitesh Kumar, Harish Chandra Verma, Amit Kumar
The study introduced anti-hyperglycemic influence of aqueous extract of Ocimum basilicum seeds (AEOBS) in Streptozotocin (STZ) induced diabetic rats and estimating its potential to ameliorate altered level of biochemical parameters, serum electrolytes level and haematological indices along with its effect on body weight of treated rats. The albino rats were selected to observe oral glucose tolerance test by oral intake of aq. glucose solution (4g/kg, body weight) in normal rats and estimation of blood glucose level after administration of AEOBS at 250mg/kg, 500mg/kg and standard drug glibenclamide at 0...
November 12, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27833799/ischemic-postconditioning-and-pinacidil-suppress-calcium-overload-in-anoxia-reoxygenation-cardiomyocytes-via-down-regulation-of-the-calcium-sensing-receptor
#11
Lin Zhang, Song Cao, Shengli Deng, Gang Yao, Tian Yu
Ischemic postconditioning (IPC) and ATP sensitive potassium channel (KATP) agonists (e.g. pinacidil and diazoxide) postconditioning are effective methods to defeat myocardial ischemia-reperfusion (I/R) injury, but their specific mechanisms of reducing I/R injury are not fully understood. We observed an intracellular free calcium ([Ca(2+)]i) overload in Anoxia/reoxygenation (A/R) cardiomyocytes, which can be reversed by KATP agonists diazoxide or pinacidil. The calcium-sensing receptor (CaSR) regulates intracellular calcium homeostasis...
2016: PeerJ
https://www.readbyqxmd.com/read/27829515/primary-degradation-of-antidiabetic-drugs
#12
Marta Markiewicz, Christian Jungnickel, Stefan Stolte, Anna Białk-Bielińska, Jolanta Kumirska, Wojciech Mrozik
Type 2 diabetes is a chronic disease affecting a large portion of the world population and is treated by orally administered drugs. Since these drugs are often taken in high doses and are excreted unchanged or partially metabolised many of them are nowadays detected in surface waters or wastewater treatment plants effluents. Unmetabolised antidiabetics or some of their transformation products retain their pharmacological activity, therefore their presence in the environment is highly undesired. One of the main routes of elimination from wastewaters or surface waters is biodegradation...
November 3, 2016: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/27826078/participation-of-potassium-channels-in-the-antinociceptive-effect-of-docosahexaenoic-acid-in-the-rat-formalin-test
#13
Arizai Yolia Landa-Juárez, Mario I Ortiz, Gilberto Castañeda-Hernández, Aracely Evangelina Chávez-Piña
Docosahexaenoic acid (DHA) is an omega-3 polyunsaturated fatty acid (PUFA) that has shown gastroprotective, cardioprotective, neuroprotective, anti-inflammatory and antinociceptive effects in different models. However, its action mechanism is still not well-defined. Reports indicate that some PUFAs regulate potassium (K(+)) channels in ventricular myocytes of rodents. As a result, the aim of this study was to evaluate the probable participation of K(+) channels in the antinociceptive effect of DHA. The rat paw 1% formalin test was used to assess nociception and antinociception...
November 6, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27820841/metformin-ameliorates-dysfunctional-traits-of-glibenclamide-and-glucose-induced-insulin-secretion-by-suppression-of-imposed-overactivity-of-the-islet-nitric-oxide-synthase-no-system
#14
Ingmar Lundquist, Israa Mohammed Al-Amily, Sandra Meidute Abaraviciene, Albert Salehi
Metformin lowers diabetic blood glucose primarily by reducing hepatic gluconeogenesis and increasing peripheral glucose uptake. However, possible effects by metformin on beta-cell function are incompletely understood. We speculated that metformin might positively influence insulin secretion through impacting the beta-cell nitric oxide synthase (NOS)-NO system, a negative modulator of glucose-stimulated insulin release. In short-time incubations with isolated murine islets either glibenclamide or high glucose augmented insulin release associated with increased NO production from both neural and inducible NOS...
2016: PloS One
https://www.readbyqxmd.com/read/27815172/nicorandil-inhibits-osteoclast-differentiation-in-vitro
#15
Futoshi Iwaki, Hitoshi Amano, Kiyoshi Ohura
Nicorandil is a hybrid angina therapeutic agent that has nitric oxide (NO) action and the ability to open ATP-sensitive K(+) channels (KATP channels). A transient increase in NO and intracellular Ca(2+) has been demonstrated to be highly involved in the differentiation and activation of osteoclasts. The objective of this study was to verify that the pharmacological effect of nicorandil suppresses the differentiation process of osteoclasts in vitro. Although little authentic NO production was detected in the culture medium in osteoclast formation assays, NO production increased only in the presence of nicorandil...
November 1, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27812367/the-methanolic-extract-from-murraya-koenigii-l-inhibits-glutamate-induced-pain-and-involves-atp-sensitive-k-channel-as-antinociceptive-mechanism
#16
Nushrat Sharmin Ani, Sudip Chakraborty, Md Moniruzzaman
Murraya koenigii L. is a perennial shrub, belonging to the family Rutaceae. Traditionally, the leaves of this plant are extensively used in treatment of a wide range of diseases and disorders including pain and inflammation. Although researchers have revealed the antinociceptive effects of this plant's leaves during past few years, the mechanisms underlying these effects are still unknown. Therefore, the present study evaluated some antinociceptive mechanisms of the methanolic extract of M. koenigii (MEMK) leaves along with its antinociceptive potential using several animal models...
2016: Advances in Pharmacological Sciences
https://www.readbyqxmd.com/read/27807801/role-of-glibenclamide-in-brain-injury-after-intracerebral-hemorrhage
#17
Bing Jiang, Lin Li, Qianwei Chen, Yihao Tao, Liming Yang, Bo Zhang, John H Zhang, Hua Feng, Zhi Chen, Jun Tang, Gang Zhu
Brain edema following intracerebral hemorrhage (ICH) causes severe secondary brain injury, and no efficient pharmacological preventions are available. The present study was designed to demonstrate the neuroprotective effects of glibenclamide on brain edema and key factors of the blood-brain barrier (BBB). The study was divided into two parts. First, we utilized an autoblood-induced rat model to investigate the expression of sulfonylurea receptor 1 (Sur1). Second, rats were randomized into sham, vehicle, and glibenclamide groups...
November 3, 2016: Translational Stroke Research
https://www.readbyqxmd.com/read/27785939/vasorelaxant-action-of-the-chloroform-fraction-of-orthosiphon-stamineusvia-no-cgmp-pathway-potassium-and-calcium-channels
#18
Mun Fei Yam, Chu Shan Tan, Mariam Ahmad, Ruan Shibao
Orthosiphon stamineus Benth. (Lamiaceae) is an important plant in traditional folk medicine that is used to treat hypertension and kidney stones. In humans, this plant has been tested as an addition regiment for antihypertensive treatment. Among the treatments for hypertension, O. stamineus had been to have diuretic and vasorelaxant effects in animal models. There is still very little information regarding the vasorelaxant effect of O. stamineus. Therefore, the present study was designed to investigate the vasorelaxant activity and mechanism of action of the fractions of O...
October 27, 2016: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/27785112/in-vitro-vasodilatory-activity-and-possible-mechanisms-of-the-crude-extracts-and-fractions-of-moringa-stenopetala-baker-f-cufod-leaves-in-isolated-thoracic-aorta-of-guinea-pigs
#19
Bekesho Geleta, Eyasu Makonnen, Asfaw Debella, Abiy Abebe, Netsanet Fekadu
Moringa stenopetala, a plant belonging to the family of Moringaceae, is traditionally used for the treatment of hypertension and diabetes in Ethiopia. This study evaluates the in vitro vasodilatory effect of the extract of M. stenopetala leaves and the possible mechanisms in precontracted isolated thoracic aorta of guinea pigs. A guinea pig was sacrificed by gentle cervical dislocation, and the thoracic aortic ring was removed, cut spirally, and mounted in an organ bath containing Krebs-Henseleit physiological solution maintained at 37°C, and then the solution was aerated with carbogen (95% O2 and 5% CO2)...
2016: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/27780710/the-effects-of-baicalein-on-gastric-mucosal-ulcerations-in-mice-protective-pathways-and-anti-secretory-mechanisms
#20
Ana Roseli S Ribeiro, José Diego do Nascimento Valença, Jeferson da Silva Santos, Thaise Boeing, Luisa Mota da Silva, Sérgio Faloni de Andrade, Ricardo L C Albuquerque-Júnior, Sara Maria Thomazzi
Many flavonoids have been shown to present good results for the treatment of gastric ulcers. Baicalein, a bioactive flavonoid derived from the Scutellaria baicalensis Georgi root, possesses several biological effects, such as anti-inflammatory and antioxidant. This study was conducted to assess the gastroprotective properties of baicalein. Anti-ulcerogenic assay was performed using the protocol of ulcer induced by ethanol/HCl in mice; then, the role of presynaptic α2-receptors, sulfhydryl (SH) compounds, nitric oxide (NO), prostaglandin (PG) and ATP-sensitive K(+) (KATP) channels in gastroprotection of baicalein was investigated...
October 22, 2016: Chemico-biological Interactions
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