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Metabolism , propranolol

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https://www.readbyqxmd.com/read/29155297/divergent-profile-between-hypothalamic-and-plasmatic-aminopeptidase-activities-in-wky-and-shr-influence-of-beta-adrenergic-blockade
#1
Isabel Prieto, Ana B Segarra, Marc de Gasparo, Magdalena Martínez-Cañamero, Manuel Ramírez-Sánchez
AIMS: Wistar-Kyoto (WKY) and spontaneously hypertensive rats (SHR) differ in their renin-angiotensin system function and sympathetic tone. The metabolism of angiotensins and vasopressin depends on the action of certain aminopeptidases whose activity may be influenced by the autonomic nervous system. Their regulation may differ between WKY and SHR in hypothalamus and plasma according to the sympathetic tone. We analyzed aminopeptidases responsible for the hydrolysis of certain angiotensins, vasopressin, cholecystokinin or enkephalins in hypothalamus and plasma of WKY and SHR in untreated controls rats and under beta-adrenoceptor blockade...
November 16, 2017: Life Sciences
https://www.readbyqxmd.com/read/29110304/beta-blockers-for-preventing-aortic-dissection-in-marfan-syndrome
#2
REVIEW
Hyun-Kyoung Koo, Kendra Ak Lawrence, Vijaya M Musini
BACKGROUND: Marfan syndrome is a hereditary disorder affecting the connective tissue and is caused by a mutation of the fibrillin-1 (FBN1) gene. It affects multiple systems of the body, most notably the cardiovascular, ocular, skeletal, dural and pulmonary systems. Aortic root dilatation is the most frequent cardiovascular manifestation and its complications, including aortic regurgitation, dissection and rupture are the main cause of morbidity and mortality. OBJECTIVES: To assess the long-term efficacy and safety of beta-blocker therapy as compared to placebo, no treatment or surveillance only in people with Marfan syndrome...
November 7, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29107282/the-autonomic-nervous-system-and-cardiac-glp-1-receptors-control-heart-rate-in-mice
#3
Laurie L Baggio, John R Ussher, Brent A McLean, Xiemin Cao, M Golam Kabir, Erin E Mulvihill, Alexandra S Mighiu, Hangjun Zhang, Andreas Ludwig, Randy J Seeley, Scott P Heximer, Daniel J Drucker
OBJECTIVES: Glucagon-like peptide-1 (GLP-1) is secreted from enteroendocrine cells and exerts a broad number of metabolic actions through activation of a single GLP-1 receptor (GLP-1R). The cardiovascular actions of GLP-1 have garnered increasing attention as GLP-1R agonists are used to treat human subjects with diabetes and obesity that may be at increased risk for development of heart disease. Here we studied mechanisms linking GLP-1R activation to control of heart rate (HR) in mice...
November 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28948673/piperine-decreases-binding-of-drugs-to-human-plasma-and-increases-uptake-by-brain-microvascular-endothelial-cells
#4
Raghvendra K Dubey, Brigitte Leeners, Bruno Imthurn, Gabriele Susanne Merki-Feld, Marinella Rosselli
We previously reported that piperine, an active alkaloidal principal of black and long peppers, enhances drug bioavailability by inhibiting drug metabolism. Another mechanism influencing drug availability/uptake is its free fraction. Since piperine is highly lipophilic, we hypothesize that it could also interact with drugs through binding displacement and influence their bioavailability. Accordingly, using equilibrium dialysis, we investigated whether piperine alters the binding of model drug ligands, that is flunitrazepam, diazepam, warfarin, salicylic acid, propranolol, lidocaine, and disopyramide to human plasma (n = 4)...
September 26, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28917751/structural-characterization-of-electrochemically-and-in-vivo-generated-potential-metabolites-of-selected-cardiovascular-drugs-by-ec-uhplc-esi-ms-using-an-experimental-design-approach
#5
Małgorzata Szultka-Młyńska, Sylwia Bajkacz, Irena Baranowska, Bogusław Buszewski
In the last few years, a number of studies were conducted which aimed at understanding the mechanisms of cardiovascular drug, metabolism, and there is still the need to determine the metabolites of cardiac drugs for the purpose of metabolism control. In this study, we employ a direct combination of electrochemical oxidation and mass spectrometric (EC-MS) identification for monitoring the oxidation pathway of ten cardiovascular drugs (metoprolol, propranolol, propafenone, mexiletine, oxprenolol, pirbuterol, pindolol, cicloprolol, acebutolol and atenolol)...
January 1, 2018: Talanta
https://www.readbyqxmd.com/read/28874356/impact-of-%C3%AE-adrenergic-signaling-in-pgc-1%C3%AE-mediated-adaptations-in-mouse-skeletal-muscle
#6
Nina Brandt, Lene Nielsen, Bjørg Thiellesen Buch, Anders Gudiksen, Stine Ringholm, Ylva Hellsten, Jens Bangsbo, Henriette Pilegaard
PGC-1α has been suggested to regulate exercise training-induced metabolic adaptations and autophagy in skeletal muscle. The factors regulating PGC-1α are however not fully resolved. The aim was to investigate the impact of β-adrenergic signaling in PGC-1α mediated metabolic adaptations in skeletal muscle with exercise training. Muscle was obtained from muscle specific PGC-1α knockout (MKO) mice and LOX/LOX 1) 3h after a single exercise bout with or without prior injection of propranolol or 3h after a single injection of clenbuterol and 2) after 5 weeks of wheel running exercise training with or without propranolol treatment or after 5 weeks of clenbuterol treatment...
September 5, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28844874/cannabinoid-cb1-receptor-inverse-agonist-mj08-stimulates-glucose-production-via-hepatic-sympathetic-innervation-in-rats
#7
Wei Chen, Hongying Liu, Hua Guan, Nina Xue, Lili Wang
As a key insulin target tissue for maintaining systemic glucose homeostasis, the liver plays important roles in improving obesity-associated insulin intolerance via selective cannabinoid CB1 receptor antagonism/inverse agonism. However, it is unclear whether this receptor inverse agonism affects hepatic glucose metabolism. MJ08 is a novel cannabinoid CB1 receptor antagonist/inverse agonist that has superior inverse agonism over the well-known antagonist/inverse agonist, SR141716 (rimonabant). MJ08 remarkably elevates fasting blood glucose independent of inhibition of insulin release in mice...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28709412/study-protocol-safety-and-efficacy-of-propranolol-0-2-eye-drops-in-newborns-with-a-precocious-stage-of-retinopathy-of-prematurity-drop-rop-0-2-a-multicenter-open-label-single-arm-phase-ii-trial
#8
Luca Filippi, Giacomo Cavallaro, Elettra Berti, Letizia Padrini, Gabriella Araimo, Giulia Regiroli, Valentina Bozzetti, Chiara De Angelis, Paolo Tagliabue, Barbara Tomasini, Giuseppe Buonocore, Massimo Agosti, Angela Bossi, Gaetano Chirico, Salvatore Aversa, Roberta Pasqualetti, Pina Fortunato, Silvia Osnaghi, Barbara Cavallotti, Maurizio Vanni, Giulia Borsari, Simone Donati, Giuseppe Nascimbeni, Giancarlo la Marca, Giulia Forni, Silvano Milani, Ivan Cortinovis, Paola Bagnoli, Massimo Dal Monte, Anna Maria Calvani, Alessandra Pugi, Eduardo Villamor, Gianpaolo Donzelli, Fabio Mosca
BACKGROUND: Retinopathy of prematurity (ROP) still represents one of the leading causes of visual impairment in childhood. Systemic propranolol has proven to be effective in reducing ROP progression in preterm newborns, although safety was not sufficiently guaranteed. On the contrary, topical treatment with propranolol eye micro-drops at a concentration of 0.1% had an optimal safety profile in preterm newborns with ROP, but was not sufficiently effective in reducing the disease progression if administered at an advanced stage (during stage 2)...
July 14, 2017: BMC Pediatrics
https://www.readbyqxmd.com/read/28689816/a-novel-role-for-dopamine-signaling-in-the-pathogenesis-of-bone-loss-from-the-atypical-antipsychotic-drug-risperidone-in-female-mice
#9
Katherine J Motyl, Megan Beauchemin, Deborah Barlow, Phuong T Le, Kenichi Nagano, Annika Treyball, Anisha Contractor, Roland Baron, Clifford J Rosen, Karen L Houseknecht
Atypical antipsychotic (AA) drugs, including risperidone (RIS), are used to treat schizophrenia, bipolar disorder, and autism, and are prescribed off-label for other mental health issues. AA drugs are associated with severe metabolic side effects of obesity and type 2 diabetes. Cross-sectional and longitudinal data also show that risperidone causes bone loss and increases fracture risk in both men and women. There are several potential mechanisms of bone loss from RIS. One is hypogonadism due to hyperprolactinemia from dopamine receptor antagonism...
October 2017: Bone
https://www.readbyqxmd.com/read/28622605/flexible-nanofilms-coated-with-aligned-piezoelectric-microfibers-preserve-the-contractility-of-cardiomyocytes
#10
P José Gouveia, S Rosa, L Ricotti, B Abecasis, H V Almeida, L Monteiro, J Nunes, F Sofia Carvalho, M Serra, S Luchkin, A Leonidovitch Kholkin, P Marques Alves, P Jorge Oliveira, R Carvalho, A Menciassi, R Pires das Neves, L Silva Ferreira
The use of engineered cardiac tissue for high-throughput drug screening/toxicology assessment remains largely unexplored. Here we propose a scaffold that mimics aspects of cardiac extracellular matrix while preserving the contractility of cardiomyocytes. The scaffold is based on a poly(caprolactone) (PCL) nanofilm with magnetic properties (MNF, standing for magnetic nanofilm) coated with a layer of piezoelectric (PIEZO) microfibers of poly(vinylidene fluoride-trifluoroethylene) (MNF+PIEZO). The nanofilm creates a flexible support for cell contraction and the aligned PIEZO microfibers deposited on top of the nanofilm creates conditions for cell alignment and electrical stimulation of the seeded cells...
September 2017: Biomaterials
https://www.readbyqxmd.com/read/28580281/glucagon-like-peptide-2-promotes-gallbladder-refilling-via-a-tgr5-independent-glp-2r-dependent-pathway
#11
Bernardo Yusta, Dianne Matthews, Grace B Flock, John R Ussher, Brigitte Lavoie, Gary M Mawe, Daniel J Drucker
OBJECTIVE: Glucagon-like peptides (GLPs) are secreted from enteroendocrine cells in response to nutrients and bile acids and control metabolism via actions on structurally-related yet distinct G protein coupled receptors. GLP-1 regulates gut motility, appetite, islet function, and glucose homeostasis, whereas GLP-2 enhances intestinal nutrient absorption. GLP-1R agonists are used to treat diabetes and obesity, and a GLP-2R agonist is approved to treat short bowel syndrome. Unexpectedly, reports of gallbladder disease have been associated with the use of both GLP-1R and GLP-2R agonists and after bariatric surgery, although the mechanisms remain unknown...
June 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28554023/uptake-biotransformation-and-elimination-of-selected-pharmaceuticals-in-a-freshwater-invertebrate-measured-using-liquid-chromatography-tandem-mass-spectrometry
#12
Thomas H Miller, Nicolas R Bury, Stewart F Owen, Leon P Barron
Methods were developed to assess uptake and elimination kinetics in Gammarus pulex of nine pharmaceuticals (sulfamethazine, carbamazepine, diazepam, temazepam, trimethoprim, warfarin, metoprolol, nifedipine and propranolol) using targeted LC-MS/MS to determine bioconcentration factors (BCFs) using a 96 h toxicokinetic exposure and depuration period. The derived BCFs for these pharmaceuticals did not trigger any regulatory thresholds and ranged from 0 to 73 L kg(-1) (sulfamethazine showed no bioconcentration)...
September 2017: Chemosphere
https://www.readbyqxmd.com/read/28548953/from-rapalogs-to-anti-aging-formula
#13
Mikhail V Blagosklonny
Inhibitors of mTOR, including clinically available rapalogs such as rapamycin (Sirolimus) and Everolimus, are gerosuppressants, which suppress cellular senescence. Rapamycin slows aging and extends life span in a variety of species from worm to mammals. Rapalogs can prevent age-related diseases, including cancer, atherosclerosis, obesity, neurodegeneration and retinopathy and potentially rejuvenate stem cells, immunity and metabolism. Here, I further suggest how rapamycin can be combined with metformin, inhibitors of angiotensin II signaling (Losartan, Lisinopril), statins (simvastatin, atorvastatin), propranolol, aspirin and a PDE5 inhibitor...
May 30, 2017: Oncotarget
https://www.readbyqxmd.com/read/28502673/glucosamine-modulates-propranolol-pharmacokinetics-via-intestinal-permeability-in-rats
#14
Hanadi A Al Shaker, Nidal A Qinna, Mujtaba Badr, Mahmoud M H Al Omari, Nasir Idkaidek, Khalid Z Matalka, Adnan A Badwan
Propranolol (PROP) undergoes extensive first-pass metabolism by the liver resulting in a relatively low bioavailability (13-23%); thus, multiple oral doses are required to achieve therapeutic effect. Since some studies have reported that glucosamine (GlcN) can increase the bioavailability of some drugs, therefore, it is aimed to study whether GlcN can change the pharmacokinetic parameters of PROP, thus modulating its bioavailability. When PROP was orally co-administered with GlcN (200mg/kg) to rats, PROP area under curve (AUC) and maximum concentration (Cmax) were significantly decreased by 43% (p<0...
May 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28454738/rat-brain-cyp2d-enzymatic-metabolism-alters-acute-and-chronic-haloperidol-side-effects-by-different-mechanisms
#15
Sharon Miksys, Fariba Baghai Wadji, Edgor Cole Tolledo, Gary Remington, Jose N Nobrega, Rachel F Tyndale
Risk for side-effects after acute (e.g. parkinsonism) or chronic (e.g. tardive dyskinesia) treatment with antipsychotics, including haloperidol, varies substantially among people. CYP2D can metabolize many antipsychotics and variable brain CYP2D metabolism can influence local drug and metabolite levels sufficiently to alter behavioral responses. Here we investigated a role for brain CYP2D in acutely and chronically administered haloperidol levels and side-effects in a rat model. Rat brain, but not liver, CYP2D activity was irreversibly inhibited with intracerebral propranolol and/or induced by seven days of subcutaneous nicotine pre-treatment...
April 26, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28406442/liposomal-encapsulation-for-systemic-delivery-of-propranolol-via-transdermal-iontophoresis-improves-bone-microarchitecture-in-ovariectomized-rats
#16
Benjamin Teong, Shyh Ming Kuo, Wei-Hsin Tsai, Mei-Ling Ho, Chung-Hwan Chen, Han Hsiang Huang
The stimulatory effects of liposomal propranolol (PRP) on proliferation and differentiation of human osteoblastic cells suggested that the prepared liposomes-encapsulated PRP exerts anabolic effects on bone in vivo. Iontophoresis provides merits such as sustained release of drugs and circumvention of first pass metabolism. This study further investigated and evaluated the anti-osteoporotic effects of liposomal PRP in ovariectomized (OVX) rats via iontophoresis. Rats subjected to OVX were administered with pure or liposomal PRP via iontophoresis or subcutaneous injection twice a week for 12 weeks...
April 13, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28296053/vasoactive-effect-of-fibronectin-derived-epiviosamine-1-and-related-peptides-in-quiescent-and-stress-models
#17
Mary D Frame, Fubao Lin, Anthony M Dewar, Richard A F Clark
OBJECTIVE: Following thermal burn injury, plasma fibronectin degrades within the interstitium; one possible product is EVA-1, PSHISKYILRWRPK found within the FNIII1 . EVA-1 ameliorates thermal burn injury progression, and binds to and enhances PDGF-BB in promoting cell metabolism, growth and survival; shorter related peptides lose these abilities. Here we study the effect of EVA-1 and shorter peptides for their vasoactivity under quiescent and stress conditions. METHODS: Using the hamster cheek pouch intravital microscopy model, five EVA-1 related peptides were applied to small arterioles via micropipette (10(-16) -10(-4) mol L(-1) ) in quiescent tissue and after defined stress: nitric oxide or heat...
August 2017: Microcirculation: the Official Journal of the Microcirculatory Society, Inc
https://www.readbyqxmd.com/read/28237652/impact-of-epinephrine-contained-in-local-anesthetic-solution-on-serum-lactate-level-during-orthognathic-surgery
#18
Hidetaka Kuroda, Gaku Kawamura, Manabu Soya, Takayuki Kitamura, Tatsuya Ichinohe, Yoshitsugu Yamada
PURPOSE: There have been many discussions of a relation between endogenous and exogenous epinephrine and hyperlactatemia. This study aimed to identify the impact of epinephrine contained in a local anesthetic solution on serum lactate levels in patients who underwent orthognathic surgery. MATERIALS AND METHODS: This study was a retrospective record review of cases of maxillary and mandibular osteotomy at the Tokyo University Hospital (Tokyo, Japan) from January 2006 through December 2014...
August 2017: Journal of Oral and Maxillofacial Surgery
https://www.readbyqxmd.com/read/28236523/acute-but-not-chronic-exposure-to-arsenic-provokes-glucose-intolerance-in-rats-possible-roles-for-oxidative-stress-and-the-adrenergic-pathway
#19
Mohsen Rezaei, Mohammd Javad Khodayar, Enayatollah Seydi, Alboghobeish Soheila, Isa Kazemzadeh Parsi
OBJECTIVES: Health problems due to heavy metals have become a worldwide concern. Along with its carcinogenicity, arsenic exposure results in impairment of glucose metabolism and insulin secretion as well as altered gene expression and signal transduction. However, the exact mechanism behind the behaviour of arsenic on glucose homeostasis and insulin secretion has not yet been fully understood. METHODS: Fasting blood sugar and glucose tolerance tests were evaluated...
February 21, 2017: Canadian Journal of Diabetes
https://www.readbyqxmd.com/read/28126832/effect-of-%C3%AE-agonist-on-the-dexamethasone-induced-expression-of-aromatase-by-the-human-monocyte-cells
#20
Masatada Watanabe, Shuji Ohno, Hiroshi Wachi
Emerging evidence suggests that sex steroids are important for human skin health. In particular, estrogen improves skin thickness, elasticity and moisture of older women. The major source of circulating estrogen is the ovary; however, local estrogen synthesis and secretion have important roles in, for example, bone metabolism and breast cancer development. We hypothesized that infiltrated peripheral monocytes are one of the sources of estrogen in skin tissues. We also hypothesized that, during atopic dermatitis under stress, a decline in the hypothalamus-pituitary-adrenal axis (HPA) and facilitation of the (hypothalamus)-sympathetic-adrenomedullary system (SAM) attenuates estrogen secretion from monocytes...
February 2017: Endocrine Connections
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