keyword
MENU ▼
Read by QxMD icon Read
search

Agonist

keyword
https://www.readbyqxmd.com/read/28437860/chronic-inhibition-of-fatty-acid-amide-hydrolase-by-urb597-produces-differential-effects-on-cardiac-performance-in-normotensive-and-hypertensive-rats
#1
Anna Pedzinska-Betiuk, Jolanta Weresa, Marek Toczek, Marta Baranowska-Kuczko, Irena Kasacka, Ewa Harasim-Symbor, Barbara Malinowska
BACKGROUND AND PURPOSE: Fatty acid amide hydrolase (FAAH) inhibitors are postulated to possess anti-hypertensive potential, because their acute injection decreases blood pressure (BP) in spontaneously hypertensive rats (SHR) partially through normalization of cardiac contractile function. Here, we examined whether the potential hypotensive effect of chronic FAAH inhibition by URB597 in hypertensive rats correlates with changes in cardiac performance. EXPERIMENTAL APPROACH: Experiments were performed using perfused hearts and left atria isolated from 8-10 week old SHR, age-matched deoxycorticosterone acetate (DOCA-salt) rats and normotensive controls chronically treated with URB597 (1 mg kg(-1) ) or vehicle...
April 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28437792/phase-plate-cryo-em-structure-of-a-class-b-gpcr-g-protein-complex
#2
Yi-Lynn Liang, Maryam Khoshouei, Mazdak Radjainia, Yan Zhang, Alisa Glukhova, Jeffrey Tarrasch, David M Thal, Sebastian G B Furness, George Christopoulos, Thomas Coudrat, Radostin Danev, Wolfgang Baumeister, Laurence J Miller, Arthur Christopoulos, Brian K Kobilka, Denise Wootten, Georgios Skiniotis, Patrick M Sexton
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases, such as osteoporosis, diabetes and obesity. Here we report the structure of a full-length class B receptor, the calcitonin receptor, in complex with peptide ligand and heterotrimeric Gαsβγ protein determined by Volta phase-plate single-particle cryo-electron microscopy. The peptide agonist engages the receptor by binding to an extended hydrophobic pocket facilitated by the large outward movement of the extracellular ends of transmembrane helices 6 and 7...
April 24, 2017: Nature
https://www.readbyqxmd.com/read/28437630/modified-natural-cycle-for-embryo-transfer-using-frozen-thawed-blastocysts-a-satisfactory-option
#3
Quoc V Le, Sina Abhari, Omar M Abuzeid, Jennifer DeAnna, Mohamed A Satti, Tarek Abozaid, Iqbal Khan, Mostafa I Abuzeid
OBJECTIVE: To describe pregnancy outcomes of frozen-thawed blastocysts cycles using modified natural cycle frozen embryo transfers (NC-FET) and down-regulated hormonally controlled frozen embryo transfers (HC-FET) protocols. STUDY DESIGN: This retrospective cohort study included all patients undergoing either modified NC-FET or down-regulated HC-FET using frozen-thawed day 5 embryos. Cycles with donor blastocysts were excluded. Four hundred twenty eight patients underwent a total of 493 FET cycles...
April 6, 2017: European Journal of Obstetrics, Gynecology, and Reproductive Biology
https://www.readbyqxmd.com/read/28437434/comparisons-of-gnrh-antagonist-protocol-versus-gnrh-agonist-long-protocol-in-patients-with-normal-ovarian-reserve-a-systematic-review-and-meta-analysis
#4
Ruolin Wang, Shouren Lin, Yong Wang, Weiping Qian, Liang Zhou
OBJECTIVE: To evaluate the effectiveness and safety of gonadotropin-releasing hormone antagonist (GnRH-ant) protocol and gonadotropin-releasing hormone agonist (GnRH-a) long protocol in patients with normal ovarian reserve. METHODS: We searched the PubMed (1992-2016), Cochrane Library (1999-2016), Web of Science (1950-2016), Chinese Biomedical Database (CBM, 1979-2016), and China National Knowledge Infrastructure (CNKI, 1994-2016). Any randomized controlled trials (RCTs) that compared GnRH-ant protocol and GnRH-a long protocol in patients with normal ovarian reserve were included, and data were extracted independently by two reviewers...
2017: PloS One
https://www.readbyqxmd.com/read/28437302/pain-management-in-the-opioid-dependent-pregnant-woman
#5
Rebecca R Safley, Jamie Swietlikowski
Opioid dependence is an epidemic in the United States, and the percentage of pregnant women who are opioid dependent has increased dramatically in the last decade. Pain management, already a concern for intrapartum and postpartum care, is complicated in the context of opioid dependence. This clinical review surveys the literature on pain management in opioid-dependent pregnant women to summarize current consensus and evidence to guide clinical practice. Points of consensus for pain management in opioid-dependent pregnant women include continual opioid maintenance therapy throughout the pregnancy and the postpartum period; adequate management of acute pain; the contraindication of opioid agonist-antagonists for pain management; and the need for interdisciplinary teams using a multimodal approach to provide optimal care to opioid-dependent pregnant women...
April 2017: Journal of Perinatal & Neonatal Nursing
https://www.readbyqxmd.com/read/28437032/autonomic-receptor-mediated-regulation-of-production-and-release-of-nitric-oxide-in-normal-and-malignant-human-urothelial-cells
#6
Michael Winder, Renata Vesela, Patrik Aronsson, Bhavik Patel, Thomas Carlsson
In the urinary bladder, the main source of NO seems to be the urothelium and the underlying suburothelium. In this study, we aimed to characterize how receptors in the human urothelium regulate the production and release of NO. For this, we cultured two human urothelial cell lines - the normal immortalized cell line UROtsa and the malignant cell line T24. These were treated with an array of agonists and antagonists with affinity for adrenergic, muscarinic and purinergic receptors. The production of NO and expression of nitric oxide synthase (NOS) was studied by immunocytochemistry and western blotting...
April 24, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28437005/convergent-erk1-2-p38-and-jnk-mapk-signalling-mediate-catecholoestradiol-induced-proliferation-of-ovine-uterine-artery-endothelial-cells
#7
Rosalina Villalon Landeros, Sheikh O Jobe, Gabrielle Aranda-Pino, Gladys E Lopez, Jing Zheng, Ronald R Magness
Previously we demonstrated that the biologically active metabolites of 17β-oestradiol, 2-hydroxyoestradiol (2-OHE2 ) and 4-hydroxyoestradiol (4-OHE2 ), stimulate pregnancy-specific proliferation of uterine artery endothelial cells derived from pregnant (P-UAECs), but not non-pregnant ewes. However, unlike 17β-oestradiol, which induces proliferation via oestrogen receptor-β (ER-β), the catecholoestradiols mediate P-UAEC proliferation via β-adrenoceptors (β-AR) and independent of classic oestrogen receptors...
April 24, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28436934/biopolymers-codelivering-engineered-t-cells-and-sting-agonists-can-eliminate-heterogeneous-tumors
#8
Tyrel T Smith, Howell F Moffett, Sirkka B Stephan, Cary F Opel, Amy G Dumigan, Xiuyun Jiang, Venu G Pillarisetty, Smitha P S Pillai, K Dane Wittrup, Matthias T Stephan
Therapies using T cells that are programmed to express chimeric antigen receptors (CAR T cells) consistently produce positive results in patients with hematologic malignancies. However, CAR T cell treatments are less effective in solid tumors for several reasons. First, lymphocytes do not efficiently target CAR T cells; second, solid tumors create an immunosuppressive microenvironment that inactivates T cell responses; and third, solid cancers are typified by phenotypic diversity and thus include cells that do not express proteins targeted by the engineered receptors, enabling the formation of escape variants that elude CAR T cell targeting...
April 24, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28436723/asymptomatic-peripheral-artery-disease-can-limit-maximal-exercise-capacity-in-chronic-obstructive-pulmonary-disease-patients-regardless-of-airflow-obstruction-and-lung-hyperinflation
#9
Ernesto Crisafulli, Chiara Scelfo, Panagiota Tzani, Marina Aiello, Giuseppina Bertorelli, Alfredo Chetta
Background Silent/asymptomatic peripheral artery disease may occur in patients with chronic obstructive pulmonary disease, but it is poorly investigated. The primary aim of this study was to evaluate in chronic obstructive pulmonary disease patients the impact of asymptomatic/silent peripheral artery disease on maximal exercise capacity; the secondary aim was to search for predictors of peripheral artery disease. Methods We prospectively enrolled chronic obstructive pulmonary disease outpatients. Data on anthropometric characteristics, lung function, cardiopulmonary exercise test and ankle-brachial index were recorded...
January 1, 2017: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/28436486/muscle-wasting-and-cachexia-in-heart-failure-mechanisms-and-therapies
#10
REVIEW
Stephan von Haehling, Nicole Ebner, Marcelo R Dos Santos, Jochen Springer, Stefan D Anker
Body wasting is a serious complication that affects a large proportion of patients with heart failure. Muscle wasting, also known as sarcopenia, is the loss of muscle mass and strength, whereas cachexia describes loss of weight. After reaching guideline-recommended doses of heart failure therapies, the most promising approach to treating body wasting seems to be combined therapy that includes exercise, nutritional counselling, and drug treatment. Nutritional considerations include avoiding excessive salt and fluid intake, and replenishment of deficiencies in trace elements...
April 24, 2017: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/28436303/choline-supplementation-during-pregnancy-protects-against-gestational-lipopolysaccharide-induced-inflammatory-responses
#11
Min Zhang, Xinjia Han, Juejie Bao, Jinying Yang, Shao-Qing Shi, Robert E Garfield, Huishu Liu
OBJECTIVES: To estimate the effects and mechanisms of choline, an essential nutrient and a selective α7 nicotinic acetylcholine receptor (α7nAChR) agonist, on the prevention of symptoms and the effects on the cholinergic anti-inflammatory pathways (CAP) in a lipopolysaccharide (LPS)-induced inflammatory response in a rat model. METHODS: Inflammation was induced by LPS treatment (1.0 μg LPS/kg body weight) on gestational day (GD) 14. Nonpregnant and pregnant Sprague Dawley rats were placed on a normal choline diet (1...
January 1, 2017: Reproductive Sciences
https://www.readbyqxmd.com/read/28436258/thrombopoietin-and-platelet-aggregation-in-patients-with-stable-coronary-artery-disease
#12
Sanne Bøjet Larsen, Erik Lerkevang Grove, Søs Neergaard-Petersen, Morten Würtz, Anne-Mette Hvas, Steen Dalby Kristensen
Thrombopoietin (TPO) may facilitate platelet activation and aggregation. However, data on the impact of TPO on platelet aggregation in patients with stable coronary artery disease (CAD) are scarce. We aimed to investigate associations between TPO and platelet aggregation and activation in patients with stable coronary artery disease (CAD). We studied 900 stable CAD patients. Serum TPO was assessed by ELISA. Platelet aggregation was evaluated using the Multiplate Analyzer (agonists: arachidonic acid [AA] and collagen) and the VerifyNow Aspirin Assay...
April 24, 2017: Platelets
https://www.readbyqxmd.com/read/28436117/early-introduction-of-oral-paricalcitol-in-renal-transplant-recipients-an-open-label-randomized-study
#13
Hege Kampen Pihlstrøm, Franscesca Gatti, Clara Hammarström, Ivar Anders Eide, Monika Kasprzycka, Junbai Wang, Guttorm Haraldsen, My Hanna Sofia Svensson, Karsten Midtvedt, Geir Mjøen, Dag Olav Dahle, Anders Hartmann, Hallvard Holdaas
In stable renal transplant recipients with hyperparathyroidism, previous studies have indicated that vitamin D agonist treatment might have anti-proteinuric effects. Animal studies indicate possible anti-fibrotic and anti-inflammatory effects. Early introduction of paricalcitol in de-novo renal transplant recipients might reduce proteinuria and prevent progressive allograft fibrosis. We performed a single-centre, prospective, randomized, open-label trial investigating effects of paricalcitol 2μg/day added to standard care...
April 24, 2017: Transplant International: Official Journal of the European Society for Organ Transplantation
https://www.readbyqxmd.com/read/28435535/opioid-receptor-activity-and-analgesic-potency-of-dpdpe-peptide-analogues-containing-a-xylene-bridge
#14
Azzurra Stefanucci, Ettore Novellino, Sako Mirzaie, Giorgia Macedonio, Stefano Pieretti, Paola Minosi, Edina Szűcs, Anna I Erdei, Ferenc Zádor, Sándor Benyhe, Adriano Mollica
d-Pen(2),d-Pen(5) enkephalin (DPDPE) is one of the most selective synthetic peptide agonists targeting the δ-opioid receptor. Three cyclic analogues of DPDPE containing a xylene bridge in place of disulfide bond have been synthesized and fully characterized as opioid receptors agonists. The in vitro activity was investigated showing a good affinity of 7a-c for μ- and δ-receptors. In vivo biological assays revealed that 7b is the most potent analogue with the ability to maintain high level of analgesia from 15 to 60 min following intracerebroventricular (i...
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28435446/cardiovascular-risk-assessment-in-patients-with-diabetes
#15
REVIEW
Marcello Casaccia Bertoluci, Viviane Zorzanelli Rocha
Although patients with diabetes have 2 to 4 times increased risk of cardiovascular morbidity and mortality than individuals without diabetes, recent studies indicate that a significant part of patients are in a lower cardiovascular risk category. Men younger than 35 years, women younger than 45 years, patients with diabetes duration of less than 10 years without other risk factors have a much lower risk than patients who have traditional cardiovascular risk factors, and subclinical or established coronary artery disease (CAD)...
2017: Diabetology & Metabolic Syndrome
https://www.readbyqxmd.com/read/28435427/novel-4-thiazolidinone-derivatives-as-agonists-of-benzodiazepine-receptors-design-synthesis-and-pharmacological-evaluation
#16
Mehrdad Faizi, Reza Jahani, Seyed Abbas Ebadi, Sayyed Abbas Tabatabai, Elham Rezaee, Mehrnaz Lotfaliei, Mohsen Amini, Ali Almasirad
A new series of 4-chloro-N-(2-(substitutedphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide derivatives were designed, synthesized and biologically evaluated as anticonvulsant agents. The designed compounds have the main essential functional groups for binding to the benzodiazepine receptors and 4-thiazolidinone ring as an anticonvulsant pharmacophore. Some of the new synthesized compounds showed considerable anticonvulsant activity in electroshock and pentylenetetrazole-induced lethal convulsion tests. Compound 5i, 4-chloro-N-(2-(4-methoxyphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide, with the best activity was selected for evaluation of other benzodiazepine pharmacological effects...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28435305/glucagon-like-peptide-1-receptor-agonists-a-systematic-review-of-comparative-effectiveness-research
#17
REVIEW
Philip A Levin, Hiep Nguyen, Eric T Wittbrodt, Seoyoung C Kim
BACKGROUND: Glucagon-like peptide-1 receptor agonists (GLP-1RAs) act by increasing insulin secretion, decreasing glucagon secretion, slowing gastric emptying, and increasing satiety. OBJECTIVE: Published evidence directly comparing GLP-1RAs with other approved treatments for type 2 diabetes (T2D) was systematically reviewed. METHODS: A literature search was performed using MEDLINE and Embase databases to identify papers comparing GLP-1RAs with other classes of glucose-lowering therapy in patients with T2D...
2017: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
https://www.readbyqxmd.com/read/28435304/comparative-effectiveness-of-glycemic-control-in-patients-with-type-2-diabetes-treated-with-glp-1-receptor-agonists-a-network-meta-analysis-of-placebo-controlled-and-active-comparator-trials
#18
Michelle E Orme, Hiep Nguyen, Jackie Y Lu, Susan A Thomas
BACKGROUND: Clinical studies of patients with type 2 diabetes show that GLP-1 receptor agonists (GLP-1 RAs) improve glycemic control and promote weight loss. We conducted a Bayesian network meta-analysis (NMA) of placebo- and active-controlled randomized trials to assess the comparative effectiveness of liraglutide, albiglutide, dulaglutide, and exenatide twice daily and once weekly, with a focus on glycemic control. MATERIALS AND METHODS: We searched Medline, Embase, and the Cochrane Library (up to December 2014) for core registration programs for US-approved GLP-1 RAs...
2017: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
https://www.readbyqxmd.com/read/28435224/investigation-of-triamterene-as-an-inhibitor-of-the-tgr5-receptor-identification-in-cells-and-animals
#19
Yingxiao Li, Kai Chun Cheng, Chiang-Shan Niu, Shih-Hsiang Lo, Juei-Tang Cheng, Ho-Shan Niu
BACKGROUND: G-protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5) has been shown to participate in glucose homeostasis. In animal models, a TGR5 agonist increases incretin secretion to reduce hyperglycemia. Many agonists have been developed for clinical use. However, the effects of TGR5 blockade have not been studied extensively, with the exception of studies using TGR5 knockout mice. Therefore, we investigated the potential effect of triamterene on TGR5. METHODS: We transfected the TGR5 gene into cultured Chinese hamster ovary cells (CHO-K1 cells) to express TGR5...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28435125/the-blockage-of-ventromedial-hypothalamus-crf-type-2-receptors-impairs-escape-responses-in-the-elevated-t-maze
#20
Mariana S C F Silva, Thaissa M O Souza, Bruno A Pereira, Daniel A Ribeiro, Isabel C Céspedes, Jackson C Bittencourt, Milena B Viana
In a previous study, the administration of corticotrophin-releasing factor (CRF) into the dorsomedial hypothalamus (DMH), a region that modulates defensive reactions, was shown to facilitate elevated T-maze (ETM) avoidance responses, an anxiogenic-like effect. Intra-DMH administration of the CRF type 1 receptor (CRFR1) antagonist antalarmin induced anxiolytic-like effects and counteracted the anxiogenic effects of CRF. The present study further investigates the role played by CRF receptors of the medial hypothalamus in anxiety...
April 20, 2017: Behavioural Brain Research
keyword
keyword
19458
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"