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https://www.readbyqxmd.com/read/28103649/amlodipine-an-l-type-calcium-channel-blocker-protects-against-chlorpromazine-induced-neurobehavioural-deficits-in-mice
#1
Oluwafemi E Kale, Olufunsho Awodele, Temitope O Ogundare, Martins Ekor
The present study investigated the modulatory and chemopreventive benefit of amlodipine (AML), a dihydropyridine calcium channel antagonist, against neurobehavioural abnormalities (NAs) associated with chlorpromazine (CPZ) toxicity in mice. Adult mice were divided into five groups of 6 animals/group. Group 1 (control) was administered saline (10 ml/kg i.p.). Group 2 received CPZ (2 mg/kg i.p.). Groups 3 and 4 received bromocriptine (BMC, 2.5 mg/kg s.c.) and AML (1 mg/kg s.c.) respectively while group 5 received their combination...
January 19, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28103623/metabolic-inflexibility-with-obesity-and-the-effects-of-fenofibrate-on-skeletal-muscle-fatty-acid-oxidation
#2
Kristen E Boyle, Jacob E Friedman, Rachel C Janssen, Chantal Underkofler, Joseph A Houmard, Neda Rasouli
This study was designed to investigate mechanisms of lipid metabolic inflexibility in human obesity and the ability of fenofibrate (FENO) to increase skeletal muscle fatty acid oxidation (FAO) in primary human skeletal muscle cell cultures (HSkMC) exhibiting metabolic inflexibility. HSkMC from 10 lean and 10 obese, insulin resistant subjects were treated with excess fatty acid for 24 h (24hFA) to gauge lipid-related metabolic flexibility. Metabolically inflexible HSkMC from obese individuals were then treated with 24hFA in combination with FENO to determine effectiveness for increasing FAO...
January 2017: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
https://www.readbyqxmd.com/read/28103616/l-lysine-acts-as-a-serotonin-type-4-receptor-antagonist-to-counteract-in-vitro-and-in-vivo-the-stimulatory-effect-of-serotonergic-agents-on-aldosterone-secretion-in-man
#3
C Duparc, C André, J Ménard, B Godouet-Getti, J Wils, A F Cailleux, L Moreau-Grangé, E Louiset, H Lefebvre
In the normal human adrenal gland, serotonin (5-HT) stimulates aldosterone secretion through the 5-HT4 receptor (5-HT4R). However, the physiological role of the serotonergic control of adrenocortical function is not known. In the present study, we have investigated the ability of l-Lysine, which has been shown to act as a 5-HT4 receptor antagonist, to counteract in vitro and in vivo the stimulatory effect of 5-HT4R agonists on aldosterone production. l-Lysine was found to inhibit aldosterone production induced by 5-HT and the 5-HT4R agonists BIMU8 from cultured human adrenocortical cells...
January 19, 2017: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
https://www.readbyqxmd.com/read/28103486/combined-toxic-effects-and-mechanisms-of-microsystin-lr-and-copper-on-vallisneria-natans-lour-hara-seedlings
#4
Zhi Wang, Junqian Zhang, Enhua Li, Liang Zhang, Xuelei Wang, Lirong Song
Microcystin-LR (MCLR) and copper are commonly found in eutrophic water bodies because of eutrophic run-offs, cyanobacterial blooms, and copper algicide applications. However, the ecotoxicological risk of their combination remains unknown. This study investigated the effect of MCLR, Cu, and their mixture on the growth and physiological responses of Vallisneria natans. Results showed that the combined toxicity of them was concentration dependent. Synergistic effects were elicited at low concentrations of MCLR and Cu exposure (≤0...
January 3, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28103441/enantio-specific-allosteric-modulation-of-cannabinoid-1-receptor
#5
Robert B Laprairie, Pushkar M Kulkarni, Jeffrey R Deschamps, Melanie E M Kelly, David R Janero, Maria G Cascio, Lesley A Stevenson, Roger G Pertwee, Terry Kenakin, Eileen M Denovan-Wright, Ganesh A Thakur
The cannabinoid 1 receptor (CB1R) is one of the most widely expressed metabotropic G protein-coupled receptors in brain, and its participation in various (patho)physiological processes has made CB1R activation a viable therapeutic modality. Adverse psychotropic effects limit the clinical utility of CB1R orthosteric agonists and have promoted the search for CB1R positive allosteric modulators (PAMs) with the promise of improved drug-like pharmacology and enhanced safety over typical CB1R agonists. In this study, we describe the synthesis and in vitro and ex vivo pharmacology of the novel allosteric CB1R modulator GAT211 (racemic) and its resolved enantiomers, GAT228 (R) and GAT229 (S)...
January 19, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28103292/muscle-reactive-oxygen-species-ros-contribute-to-post-incisional-guarding-via-the-trpa1-receptor
#6
Daisuke Sugiyama, Sinyoung Kang, Timothy J Brennan
BACKGROUND: Deep tissues and their afferents have unique responses to various stimuli and respond to injury distinctively. However, the types of receptors and endogenous ligands that have a key role in pain after deep tissue incision are unknown. TRPA1 has been shown to mediate pain-related responses in inflammation- and nerve injury-induced pain models. We hypothesized that TRPA1 has an important role in pain behaviors after deep tissue incision. METHODS: The effect of various doses of intraperitoneal (i...
2017: PloS One
https://www.readbyqxmd.com/read/28103285/radioiodinated-exendin-4-is-superior-to-the-radiometal-labelled-glucagon-like-peptide-1-receptor-probes-overcoming-their-high-kidney-uptake
#7
Tilman Läppchen, Roswitha Tönnesmann, Jos Eersels, Philipp T Meyer, Helmut R Maecke, Svetlana N Rylova
GLP-1 receptors are ideal targets for preoperative imaging of benign insulinoma and for quantifying the beta cell mass. The existing clinical tracers targeting GLP-1R are all agonists with low specific activity and very high kidney uptake. In order to solve those issues we evaluated GLP-1R agonist Ex-4 and antagonist Ex(9-39) radioiodinated at Tyr40 side by side with [Nle14,Lys40(Ahx-DOTA-68Ga)NH2]Ex-4 (68Ga-Ex-4) used in the clinic. The Kd, Bmax, internalization and binding kinetics of [Nle14,125I-Tyr40-NH2]Ex-4 and [Nle14,125I-Tyr40-NH2]Ex(9-39) were studied in vitro using Ins-1E cells...
2017: PloS One
https://www.readbyqxmd.com/read/28103022/discovery-of-a-novel-series-of-orally-bioavailable-and-cns-penetrant-glucagon-like-peptide-1-receptor-glp-1r-non-competitive-antagonists-based-on-a-1-3-disubstituted-7-aryl-5-5-bis-trifluoromethyl-5-8-dihydropyrimido-4-5-d-pyrimidine-2-4-1h-3h-dione-core
#8
Kellie D Nance, Emily L Days, C David Weaver, Anastasia Coldren, Tiffany D Farmer, Hyekyung P Cho, Colleen M Niswender, Anna L Blobaum, Kevin D Niswender, Craig W Lindsley
A duplexed, functional multi-addition high throughput screen and subsequent optimization effort identified the first orally bioavailable and CNS penetrant glucagon-like peptide-1 receptor (GLP-1R) non-competitive antagonist. Antagonist 5d not only blocked Exendin-4-stimulated insulin release in islets, but also lowered insulin levels while increasing blood glucose in vivo.
January 19, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28102934/crosstalk-between-angiotensin-and-the-non-amyloidogenic-pathway-of-alzheimer-s-amyloid-precursor-protein
#9
Anna Maria Kanarek, Annika Wagner, Jim Küppers, Michael Gütschow, Rolf Postina, Elzbieta Kojro
The association between hypertension and an increased risk for Alzheimer's disease (AD) and dementia is well established. Many data suggest that modulation of the renin-angiotensin system may be meaningful for the prevention and therapy of neurodegenerative disorders, in particular AD. Proteolytic cleavage of the amyloid precursor protein (APP) by α-secretase precludes formation of neurotoxic Aβ peptides and is expected to counteract the development of AD. An established approach for the up-regulation of α-secretase cleavage is activation of G protein-coupled receptors (GPCRs)...
January 19, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28102879/the-conservative-and-pharmacological-management-of-chronic-subdural-haematoma
#10
Jehuda Soleman, Fabio Noccera, Luigi Mariani
Chronic subdural haematoma (cSDH), one of the most common neurosurgical entities, occurs typically in elderly patients. The incidence is expected to double by the year 2030, owing to the continuous aging of the population. Surgery is usually the treatment of choice, but conservative treatment may be a good alternative in some situations. We provide a systematic review of studies analysing the conservative treatment options and the natural history of cSDH. Of 231 articles screened, 35 were included in this systematic review...
January 19, 2017: Swiss Medical Weekly
https://www.readbyqxmd.com/read/28102773/the-optimal-duration-of-anticoagulant-therapy-after-unprovoked-venous-thromboembolism-still-a-challenging-issue
#11
Giovanna Elmi, Giuseppe Di Pasquale, Raffaele Pesavento
As about 50 % of patients with unprovoked venous thromboembolism (VTE) will develop new episodes after discontinuing therapy, indefinite treatment is suggested in patients with low or moderate bleeding risk. Baseline and post-baseline factors can help clinicians to identify patients at high risk of recurrence, who require extended treatment. Residual vein obstruction and D-dimer assay have been shown to be suitable methods for assessing the risk of VTE recurrences after a first unprovoked VTE. In treatment for VTE the use of direct oral anticoagulants (DOAC) is growing instead of the standard adjusted dose of vitamin K antagonists...
January 19, 2017: VASA. Zeitschrift Für Gefässkrankheiten
https://www.readbyqxmd.com/read/28102615/comparative-effectiveness-of-venous-thromboembolism-prophylaxis-options-for-the-patient-undergoing-total-hip-and-knee-replacement-a-network-meta-analysis
#12
A Kapoor, A Ellis, N Shaffer, J Gurwitz, A Chandramohan, J Saulino, A Ishak, T Okubanjo, F Michota, E Hylek, T A Trikalinos
: Essentials Despite trial data, guidelines have not endorsed direct oral Xa inhibitors above other options. We provide profiles of venous thromboembolism and hemorrhage risk for 12 options. Direct oral Xa inhibitors had a favorable profile compared with low-molecular-weight heparin. Other options did not have favorable profiles compared with low-molecular-weight heparin. SUMMARY: Background There are numerous trials and several meta-analyses comparing venous thromboembolism (VTE) prophylaxis options after total hip and knee replacement (THR and TKR)...
November 7, 2016: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28102399/microsphere-cytometry-to-interrogate-microenvironment-dependent-cell-signaling
#13
Henriette Christie Ertsås, Garry P Nolan, Mark A LaBarge, James B Lorens
Microenvironmental cues comprising surface-mediated and soluble factors control cellular signaling mechanisms underlying normal cellular responses that define homeostatic and diseased cell states. In order to measure cell signaling in single adherent cells, we developed a novel microsphere-based flow cytometry approach. Single normal or neoplastic cells were adhered to uniform microspheres that display mimetic-microenvironments comprising surface combinations of extracellular matrix (ECM) in the presence of soluble agonists/antagonists...
January 19, 2017: Integrative Biology: Quantitative Biosciences From Nano to Macro
https://www.readbyqxmd.com/read/28102361/effectiveness-and-tolerability-of-different-recommended-doses-of-ppis-and-h2ras-in-gerd-network-meta-analysis-and-grade-system
#14
Chao Zhang, Joey S W Kwong, Rui-Xia Yuan, Hao Chen, Chang Xu, Yi-Pin Wang, Gong-Li Yang, Jin-Zhu Yan, Le Peng, Xian-Tao Zeng, Hong Weng, Jie Luo, Yu-Ming Niu
Proton pump inhibitors (PPIs) and histamine-2-receptor antagonists (H2RAs) are used for gastro-esophageal reflux disease (GERD); however, the clinical evidence for treatment is poor. We evaluated the effectiveness and tolerability of different doses of PPIs, H2RAs and placebo in adults with GERD. Six online databases were searched through September 1, 2016. All related articles were included and combined with a Bayesian network meta-analysis from randomized controlled trials (RCTs). The GRADE systems were employed to assess the main outcome...
January 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28102330/new-insights-into-fetal-mammary-gland-morphogenesis-differential-effects-of-natural-and-environmental-estrogens
#15
Lucia Speroni, Maria Voutilainen, Marja L Mikkola, Skylar A Klager, Cheryl M Schaeberle, Carlos Sonnenschein, Ana M Soto
An increased breast cancer risk during adulthood has been linked to estrogen exposure during fetal life. However, the impossibility of removing estrogens from the feto-maternal unit has hindered the testing of estrogen's direct effect on mammary gland organogenesis. To overcome this limitation, we developed an ex vivo culture method of the mammary gland where the direct action of estrogens can be tested during embryonic days (E)14 to 19. Mouse mammary buds dissected at E14 and cultured for 5 days showed that estrogens directly altered fetal mammary gland development...
January 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28102288/acetylcholine-acts-through-m3-muscarinic-receptor-to-activate-the-egfr-signaling-and-promotes-gastric-cancer-cell-proliferation
#16
Huangfei Yu, Hongwei Xia, Qiulin Tang, Huanji Xu, Guoqing Wei, Ying Chen, Xinyu Dai, Qiyong Gong, Feng Bi
Acetylcholine (ACh), known as a neurotransmitter, regulates the functions of numerous fundamental central and peripheral nervous system. Recently, emerging evidences indicate that ACh also plays an important role in tumorigenesis. However, little is known about the role of ACh in gastric cancer. Here, we reported that ACh could be auto-synthesized and released from MKN45 and BGC823 gastric cancer cells. Exogenous ACh promoted cell proliferation in a does-dependent manner. The M3R antagonist 4-DAMP, but not M1R antagonist trihexyphenidyl and M2/4 R antagonist AFDX-116, could reverse the ACh-induced cell proliferation...
January 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28102080/n-oleoylglycine-induced-hyperphagia-was-associated-with-the-activation-of-agrp-neuron-by-cb1r
#17
Junguo Wu, Canjun Zhu, Liusong Yang, Zhonggang Wang, Lina Wang, Songbo Wang, Ping Gao, Yongliang Zhang, Qingyan Jiang, Gang Shu, Xiaotong Zhu
N-acyl amino acids (NAAAs) are conjugate products of fatty acids and amino acids, which are available in animal-derived food. We compared the effects of N-arachidonoyl glycine (NAGly), N-arachidonoyl serine (NASer), and N-Oleoylglycine (OLGly) on in vivo food intake and in vitro [Ca2+]i of AgRP neurons to identify the role of these compounds in energy homeostasis. The hypothalamic neuropeptide expression and anxiety behavior in response to OLGly were also tested. To further identify the underlying mechanism of OLGly on food intake, we first detected the expression level of potential OLGly receptors...
January 19, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28101900/bronchial-thermoplasty-in-severe-asthma-in-australia
#18
David Langton, Joy Sha, Alvin Ing, David Fielding, Erica Wood
BACKGROUND: Bronchial thermoplasty is an approved bronchoscopic intervention for the treatment of severe asthma. However, limited published experience exists outside of clinical trials regarding patient selection and outcomes achieved. Aims To evaluate the effectiveness and safety of bronchial thermoplasty in patients with severe asthma encountered in clinical practice. METHODS: This is a retrospective analysis of the first 'real world' data from Australia. The following outcomes were measured prior to, and 6 months following bronchial thermoplasty: Spirometry, Asthma Control Questionnaire-5 (ACQ-5) score, reliever and preventer medication use, and exacerbation history...
January 19, 2017: Internal Medicine Journal
https://www.readbyqxmd.com/read/28101847/off-target-anti-inflammatory-activity-of-the-p2x7-receptor-antagonist-az11645373
#19
Olga V Oskolkova, Viktoria Godschachner, Valery N Bochkov
We have found that a well-characterized P2X7 receptor antagonist AZ11645373 blocked production of pro-inflammatory chemokine IL-8 in endothelial cells treated with OxPAPC. The effect was not due to toxicity of AZ11645373 as documented by cellular metabolic activity assay. The mechanism of inhibition by AZ11645373 was apparently independent of the P2X7 receptor because this receptor was not involved in induction of IL-8 under our experimental conditions. In support of this notion, two P2X7 agonists ATP and BzATP did not upregulate IL-8...
January 19, 2017: Inflammation
https://www.readbyqxmd.com/read/28101568/puerarin-inhibits-m2-polarization-and-metastasis-of-tumor-associated-macrophages-from-nsclc-xenograft-model-via-inactivating-mek-erk-1-2-pathway
#20
Honggang Kang, Jing Zhang, Baozhong Wang, Meirong Liu, Jun Zhao, Mengxiang Yang, Yingxue Li
Non-small cell lung carcinoma (NSCLC) metastasis is responsible for most of cancer-related mortality. The tumor associated macrophages (TAMs) are known to be crucial cells in lung cancer and are usually divided into two antagonistic types, M1 and M2. Puerarin has a wide spectrum of pharmacological properties. The present study explores puerarin on macrophage polarization and metastasis of NSCLC. The results demonstrated that puerarin inhibited tumor growth and tumor volumes in NSCLC xenograft model, increased M1 markers [CD197+, inducible nitric oxide synthase (iNOS)+, CD40+)] and reduced M2 markers (CD206+, Arg-1+ and CD163+)...
February 2017: International Journal of Oncology
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