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glibenclamide

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https://www.readbyqxmd.com/read/28213290/zd0947-a-sulphonylurea-receptor-modulator-detects-functional-sulphonylurea-receptor-subunits-in-murine-vascular-smooth-muscle-atp-sensitive-k-channels
#1
Tadashi Yamamoto, Kohei Takahara, Keiichiro Uchida, Noriyoshi Teramoto
In order to identify functional sulphonylurea receptor (SUR.x) subunits of native ATP-sensitive K(+) channels (KATP channels) in mouse portal vein, the effects of ZD0947, a SUR.x modulator, were investigated on spontaneous portal vein contractions, macroscopic membrane currents and unitary currents recorded (using patch-clamp techniques) in freshly dispersed mouse portal vein myocytes. Spontaneous contractions in mouse portal vein were reversibly reduced by ZD0947 in a concentration-dependent manner (Ki = 293nM)...
February 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28207836/tmg-123-a-novel-glucokinase-activator-exerts-durable-effects-on-hyperglycemia-without-increasing-triglyceride-in-diabetic-animal-models
#2
Yoshinori Tsumura, Yu Tsushima, Azusa Tamura, Makiko Hasebe, Masanobu Kanou, Hirotsugu Kato, Tsunefumi Kobayashi
Glucokinase (GK) plays a critical role for maintaining glucose homeostasis with regulating glucose uptake in liver and insulin secretion in pancreas. GK activators have been reported to decrease blood glucose levels in patients with type 2 diabetes mellitus. However, clinical development of GK activators has failed due to the loss of glucose-lowering effects and increased plasma triglyceride levels after chronic treatment. Here, we generated a novel GK activator, TMG-123, examined its in vitro and in vivo pharmacological characteristics, and evaluated its risks of aforementioned clinical issues...
2017: PloS One
https://www.readbyqxmd.com/read/28192880/ameliorating-effect-of-betanin-a-natural-chromoalkaloid-by-modulating-hepatic-carbohydrate-metabolic-enzyme-activities-and-glycogen-content-in-streptozotocin-nicotinamide-induced-experimental-rats
#3
Indumathi Dhananjayan, Sujithra Kathiroli, Srinivasan Subramani, Vinothkumar Veerasamy
Betanin, a chromoalkaloid of beetroot, has shown significant biological effects of antioxidants, anti-inflammatory and anticarcinogenic activities. So, we attempted to determine whether betanin (a natural pigment) would be protective against hyperglycemia in streptozotocin (STZ) - nicotinamide (NA) induced diabetic rats. Rats were injected with STZ (40mg/kgb.w.) 15 mins after the administration of NA (110mg/kgb.w.) by intraperitonially (i.p.) 30days for the induction of experimental diabetes mellitus. After 72h diabetic rats were treated with betanin orally at a doses of 10, 20 and 40mg/kg b...
February 7, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28188508/potentially-inappropriate-prescribing-and-associated-factors-in-elderly-patients-at-hospital-discharge-in-brazil-a-cross-sectional-study
#4
Ana Luiza Pereira Moreira Mori, Renata Cunha Carvalho, Patricia Melo Aguiar, Maria Goretti Farias de Lima, Magali da Silva Pacheco Nobre Rossi, José Fernando Salvador Carrillo, Egídio Lima Dórea, Sílvia Storpirtis
Background The Screening Tool of Older Persons' Prescriptions/Screening Tool to Alert doctors to Right Treatment (STOPP/START) criteria is used to identify instances of potentially inappropriate prescribing in a patient's medication regimen. Objective To determine the prevalence and predictors of potentially inappropriate medications (PIMs) and potential prescribing omissions (PPOs) among elderly patients at hospital discharge. Setting A university hospital medical clinic in Brazil. Method Discharge prescriptions were examined using the STOPP/START criteria...
February 10, 2017: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/28185976/effects-of-oral-glibenclamide-on-brain-contusion-volume-and-functional-outcome-of-patients-with-moderate-and-severe-traumatic-brain-injury-a-randomized-double-blind-placebo-controlled-clinical-trial
#5
Hosseinali Khalili, Nima Derakhshan, Amin Niakan, Fariborz Ghaffarpasand, Mohammad Salehi, Hamed Eshraghian, Alireza Shakibafard, Bita Zahabi
OBJECTIVE: The aim of the current study was to investigate the effects of oral glibenclamide on brain contusion volume and functional outcome of patients with moderate and severe traumatic brain injury (TBI). METHODS: This was randomized clinical trial being conducted during a 16-month period from May 2015 and August 2016 in a level I trauma center in Southern Iran. We included 66 patients with moderate (GCS: 9-13) to severe (GCS: 5-8) TBI who had brain contusions of less than 30cc volume...
February 6, 2017: World Neurosurgery
https://www.readbyqxmd.com/read/28184360/evaluation-of-the-effect-of-glibenclamide-in-patients-with-diffuse-axonal-injury-due-to-moderate-to-severe-head-trauma
#6
Peyman Zafardoost, Amir Abbas Ghasemi, Firooz Salehpour, Chia Piroti, Ehsan Ziaeii
BACKGROUND: Traumatic brain injury (TBI) is a major health problem worldwide. Secondary injuries after TBI, including diffuse axonal injury (DAI) often occur, and proper treatments are needed in this regard. It has been shown that glibenclamide could reduce secondary brain damage after experimental TBI and improve outcomes. OBJECTIVES: We aim to evaluate the role of glibenclamide on the short-term outcome of patients with DAI due to moderate to severe TBI. PATIENTS AND METHODS: In this controlled randomized clinical trial, 40 patients with moderate to severe TBI were assigned to glibenclamide (n = 20) and control (n = 20) groups...
November 2016: Trauma Monthly
https://www.readbyqxmd.com/read/28177665/possible-involvement-of-atp-sensitive-potassium-channels-in-the-antidepressant-like-effects-of-gabapentin-in-mice-forced-swimming-test
#7
Sattar Ostadhadi, Reyhaneh Akbarian, Abbas Norouzi-Javidan, Vahid Nikoui, Samira Zolfaghari, Mohsen Chamanara, Ahmad-Reza Dehpour
Gabapentin as an anticonvulsant drug also has beneficial effects in treatment of depression. Previously we showed that acute administration of gabapentin produced an antidepressant-like effect in the mouse forced swimming test (FST) by a mechanism involves the inhibition of the nitric oxide (NO). Considering the involvement of NO in adenosine triphosphate (ATP)-sensitive potassium channels (KATP), in the present study we investigated the involvement of KATP channels in antidepressant-like effect of gabapentin...
January 29, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28176198/constituents-of-leaves-from-bauhinia-curvula-benth-exert-gastroprotective-activity-in-rodents-role-of-quercitrin-and-kaempferol
#8
Ana Paula Beber, Priscila de Souza, Thaise Boeing, Lincon Bordignon Somensi, Luísa Nathália Bolda Mariano, Benhur Judah Cury, Ligia Moura Burci, Cristiane Bezerra da Silva, Euclésio Simionatto, Sérgio Faloni de Andrade, Luísa Mota da Silva
The Bauhinia genus is known as "Pata-de-Vaca" and a wide variety of these species are used in Brazilian folk medicine due to their gastroprotective properties. This study aimed to investigate the antiulcer efficacy of the hydroalcoholic extract from B. curvula (HEBC) leaves, as well as its semi-purified fraction (SPFr) and the contribution of their phytochemicals constituents for this effect. For that, ethanol 60%/HCl 0.3 M- and indomethacin-induced gastric ulcer were performed in rodents. Gastric ulcerated tissues were processed for histological, histochemical and biochemical analysis...
February 7, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28167291/elucidation-of-the-possible-mechanism-of-analgesic-actions-of-butanol-leaf-fraction-of-olax-subscorpioidea-oliv
#9
Saidi Odoma, Abdulkadir Umar Zezi, Nuhu Mohammed Danjuma, Abubakar Ahmed, Muhammed Garba Magaji
ETHNOPHARMACOLOGICAL RELEVANCE: Preparations of Olax subscorpioidea have been used traditionally for the management of pains, inflammatory diseases, yellow fever, cancer and rheumatism. Previously, the analgesic activity of its leaf extract have been reported. Furthermore, an analgesic assay guided fractionation showed that the butanol soluble fraction is the most active. However, the mechanism of this activity remains to be elucidated. This present study investigated the possible pharmacological mechanisms involved in the analgesic activity of the butanol leaf fraction of Olax subscorpioidea (BFOS) using the acetic acid induced writhing test in mice...
February 3, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28166749/antidiabetic-effects-of-brucea-javanica-seeds-in-type-2-diabetic-rats
#10
Abdulwali Ablat, Mohammed Farouq Halabi, Jamaludin Mohamad, Muhammad Hafiz Husna Hasnan, Hazrina Hazni, Ser-Huy Teh, Jamil A Shilpi, Zulqarnain Mohamed, Khalijah Awang
BACKGROUND: Brucea javanica (B. javanica) seeds, also known as "Melada pahit" in Indo-Malay region are traditionally used to treat diabetes. The objective of this study was to determine antidiabetic, antioxidant and anti-inflammatory effects of B. javanica seeds on nicotinamide (NA)-streptozotocin (STZ) induced type 2 diabetic (T2D) rats and to analyze its chemical composition that correlate with their pharmacological activities. METHODS: A hydroethanolic extract of B...
February 6, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28163539/inhibition-by-tadalafil-of-contractility-of-isolated-nonpregnant-human-myometrium
#11
Sumalya Sen, Anitha Thomas, Saibal Das, Jayanta Kumar Dey, Abraham Peedicayil, Vinotha Thomas, Jacob Peedicayil
OBJECTIVE: To investigate the inhibitory effect of tadalafil on the contractility of isolated nonpregnant human myometrium. MATERIALS AND METHODS: The ability of tadalafil (25, 40, and 63 μM) to inhibit 55 mM KCl-induced contractility of isolated nonpregnant human myometrium was studied. The ability of the ATP-sensitive potassium channel blocker glibenclamide (10 μM) and the calcium-sensitive potassium channel (BKCa) blocker iberiotoxin (100 nM) to reverse the inhibitory effect of 40 μM tadalafil on 55 mM KCl-induced myometrial contractility was also studied...
October 2016: Journal of Pharmacology & Pharmacotherapeutics
https://www.readbyqxmd.com/read/28162170/-effects-of-different-sulfonylureas-on-the-warm-up-phenomenon-in-diabetes-patients-with-coronary-artery-disease
#12
M Zheng, L Z Li, Z A Jiang, L H Li, Y G Feng, X H Fu
Objective: To explore the different effects of chronic treatment with glibenclamide and gliclazide on the warm-up phenomenon in diabetes patients with coronary artery disease. Methods: A total of seventy-one patients with chronic stable angina and diabetes who were positive for exercise test and was proven that the stenosis degree was 70%-90% in at least one major branch through coronary angiogram were included into the study.They were divided into three groups, diet control group (DMD), glibenclamide group (DMG1) and gliclazide group (DMG2), according to the treatment of diabetes...
January 17, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/28161991/stabilizing-ability-of-surfactant-on-physicochemical-properties-of-drug-nanoparticles-generated-from-solid-dispersions
#13
Thanu Thongnopkoon, Satit Puttipipatkhachorn
This study was aimed to examine the nanoparticle formation from redispersion of binary and ternary solid dispersions. Binary systems composed of various ratios of glibenclamide (GBM) and polyvinylpyrrolidone K30 (PVP-K30), whereas a constant amount at 2.5%w/w of a surfactant, sodium lauryl sulfate (SLS) or Gelucire44/14 (GLC), was added to create ternary systems. GBM nanoparticles were collected after the systems were dispersed in water for 15 minutes. The obtained nanoparticles were characterized for size distribution, crystallinity, thermal behavior, molecular structure, and dissolution properties...
February 6, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28161542/vasorelaxation-effect-of-glycyrrhizae-uralensis-through-the-endothelium-dependent-pathway
#14
Chu Shan Tan, Yung Sing Ch'ng, Yean Chun Loh, Mohd Zaini Asmawi, Mariam Ahmad, Mun Fei Yam
ETHNOPHARMACOLOGICAL RELEVANCE: Glycyrrhiza uralensis (G. uralensis) is one of the herbs used in traditional Chinese medicine (TCM) and serves as an envoy medicinal. Since G. uralensis plays a major role in the anti-hypertensive TCM formulae, we believe that G. uralensis might possess vasorelaxation activity. AIM OF THE STUDY: This study is designed to investigate the vasorelaxation effect of G. uralensis from various extracts and to study its pharmacology effect...
February 1, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28129400/appropriate-insulin-level-in-selecting-fortified-diet-fed-streptozotocin-treated-rat-model-of-type-2-diabetes-for-anti-diabetic-studies
#15
Stanley Irobekhian Reuben Okoduwa, Ismaila A Umar, Dorcas B James, Hajiya M Inuwa
BACKGROUND: Pathophysiological investigation of disease in a suitable animal model is a classical approach towards development of a credible therapeutic strategy. This study examined appropriate insulin level in selecting animal model for type 2 diabetes (T2D) studies. METHOD: Albino Wistar rats (150-200g) were divided into two groups fed with commercially available normal-diet-feed (NDF) and water or fortified diet feed (FDF) (10g NDF per gram of margarine) with 20% fructose solution as drinking water...
2017: PloS One
https://www.readbyqxmd.com/read/28120427/oral-anti-diabetic-pharmacological-therapies-for-the-treatment-of-women-with-gestational-diabetes
#16
REVIEW
Julie Brown, Ruth Martis, Brenda Hughes, Janet Rowan, Caroline A Crowther
BACKGROUND: Gestational diabetes mellitus (GDM) is a major public health issue with rates increasing globally. Gestational diabetes, glucose intolerance first recognised during pregnancy, usually resolves after birth and is associated with short- and long-term complications for the mother and her infant. Treatment options can include oral anti-diabetic pharmacological therapies. OBJECTIVES: To evaluate the effects of oral anti-diabetic pharmacological therapies for treating women with GDM...
January 25, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28119170/existence-of-atp-sensitive-potassium-currents-on-human-periodontal-ligament-cells
#17
Phuong Thi Huyen Tran, Young Hee Lee, Janardhan Prasad Bhattarai, Soo Joung Park, Ho-Keun Yi, Seong Kyu Han
OBJECTIVE: Potassium channels of the ATP-sensitive family (KATP channel) are inhibited by increase in intracellular ATP. Electrophysiological studies have demonstrated that the kinetics and pharmacological properties of KATP channels vary among different tissues, suggesting structurally and functionally distinct types. There are studies showing human periodontal ligament (PDL) cells respond to mechanical stress by increasing ATP release, which participates in bone resorption or bone homeostasis...
January 17, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/28119150/vascular-katp-channels-mitigate-severe-muscle-o2-delivery-utilization-mismatch-during-contractions-in-chronic-heart-failure-rats
#18
Clark T Holdsworth, Scott K Ferguson, Trenton D Colburn, Alexander J Fees, Jesse C Craig, Daniel M Hirai, David C Poole, Timothy I Musch
The vascular ATP-sensitive K(+) (KATP) channel is a mediator of skeletal muscle microvascular oxygenation (PO2mv) during contractions in health. We tested the hypothesis that KATP channel function is preserved in chronic heart failure (CHF) and therefore its inhibition would reduce PO2mv and exacerbate the time taken to reach the PO2mv steady-state during contractions of the spinotrapezius muscle. Moreover, we hypothesized that subsequent KATP channel activation would oppose the effects of this inhibition. Muscle PO2mv (phosphorescence quenching) was measured during 180s of 1-Hz twitch contractions (∼6V) under control, glibenclamide (GLI, KATP channel antagonist; 5mg/kg) and pinacidil (PIN, KATP channel agonist; 5mg/kg) conditions in 16 male Sprague-Dawley rats with CHF induced via myocardial infarction (coronary artery ligation, left ventricular end-diastolic pressure: 18±1mmHg)...
January 22, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28117739/affinin-spilanthol-isolated-from-heliopsis-longipes-induces-vasodilation-via-activation-of-gasotransmitters-and-prostacyclin-signaling-pathways
#19
Jesús Eduardo Castro-Ruiz, Alejandra Rojas-Molina, Francisco J Luna-Vázquez, Fausto Rivero-Cruz, Teresa García-Gasca, César Ibarra-Alvarado
Heliopsis longipes roots have been widely used in Mexican traditional medicine to relieve pain, mainly, toothaches. Previous studies have shown that affinin, the major alkamide of these roots, induces potent antinociceptive and anti-inflammatory activities. However, the effect of H. longipes root extracts and affinin on the cardiovascular system have not been investigated so far. In the present study, we demonstrated that the dichloromethane and ethanolic extracts of H. longipes roots, and affinin, isolated from these roots, produce a concentration-dependent vasodilation of rat aorta...
January 22, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28114735/effects-of-type-2-diabetes-mellitus-in-patients-on-treatment-with-glibenclamide-and-metformin-on-carvedilol-enantiomers-metabolism
#20
Glauco H B Nardotto, Eduardo B Coelho, Carlos E Paiva, Vera L Lanchote
Carvedilol is available in clinical practice as a racemate in which (S)-(-)-carvedilol is a β- and α1 -adrenergic antagonist and (R)-(+)-carvedilol is only an α1 -adrenergic antagonist. Carvedilol is mainly metabolized by glucuronidation, by CYP2D6 to hydroxyphenylcarvedilol (OHC), and by CYP2C9 to O-desmethylcarvedilol (DMC). This study evaluated the pharmacokinetics of carvedilol enantiomers and their metabolites OHC and DMC in healthy volunteers (n = 13) and in type 2 diabetes mellitus patients with good glycemic control (n = 13)...
January 23, 2017: Journal of Clinical Pharmacology
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