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Alpha 1b antagonist

Ingunn Holen, Diane V Lefley, Sheila E Francis, Sarah Rennicks, Steven Bradbury, Robert E Coleman, Penelope Ottewell
BACKGROUND: We have recently identified interleukin 1B (IL-1B) as a potential biomarker for predicting breast cancer patients at increased risk for developing bone metastasis. In mouse models, IL-1B and its receptor (IL-1R1) are upregulated in breast cancer cells that metastasise to bone compared with cells that do not. We have now investigated the functional role of IL-1 by blocking IL-1R signalling with the clinically licensed antagonist, anakinra. METHODOLOGY: 6-week old female BALB/c mice received a subcutaneous or intra-venous injection of MDA-MB-231-IV or MCF7 cells...
September 27, 2016: Oncotarget
Rashmi Priya, Kenneth Wee, Srikanth Budnar, Guillermo A Gomez, Alpha S Yap, Magdalene Michael
Non-muscle myosin II (NMII) motor proteins are responsible for generating contractile forces inside eukaryotic cells. There is also a growing interest in the capacity for these motor proteins to influence cell signaling through scaffolding, especially in the context of RhoA GTPase signaling. We previously showed that NMIIA accumulation and stability within specific regions of the cell cortex, such as the zonula adherens (ZA), allows the formation of a stable RhoA signaling zone. Now we demonstrate a key role for Coronin 1B in maintaining this junctional pool of NMIIA, as depletion of Coronin 1B significantly compromised myosin accumulation and stability at junctions...
September 20, 2016: Cell Cycle
R Croft Thomas, Patrick M Cowley, Abhishek Singh, Bat-Erdene Myagmar, Philip M Swigart, Anthony J Baker, Paul C Simpson
The alpha-1A-adrenergic receptor (AR) subtype is associated with cardioprotective signaling in the mouse and human heart. The rabbit is useful for cardiac disease modeling, but data on the alpha-1A in the rabbit heart are limited. Our objective was to test for expression and function of the alpha-1A in rabbit heart. By quantitative real-time reverse transcription PCR (qPCR) on mRNA from ventricular myocardium of adult male New Zealand White rabbits, the alpha-1B was 99% of total alpha-1-AR mRNA, with <1% alpha-1A and alpha-1D, whereas alpha-1A mRNA was over 50% of total in brain and liver...
2016: PloS One
Junjun Huang, Fei He, Minyi Huang, Xiawen Liu, Yan Xiong, Yajian Huang, Liu Zhu, Ya Yang, Xingjie Xu, Mu Yuan
Eleven novel naftopidil-related compounds that contain amide and indole groups were designed and synthesized. The biological effects of these compounds on three α1-adrenoceptor subtypes and cancerous human prostate cell lines (PC-3, DU-145, and LNCaP) were determined. Compounds 2, 3, 5, 11, and 12 exhibited an α1-adrenoceptor antagonistic activity, whereas compounds 9, 10, and 12 displayed moderate antiproliferative activities. Compound 3 exhibited a significant α(1D/1A) blocking activity in isolated rat tissues (97...
2015: European Journal of Medicinal Chemistry
E L Ivanova
The aim of this study was to assess the presence or absence of association between the degree of changes in microbiota and gene polymorphism of cytokines IL-1Ra, IL-1b, TNFa, IL-4, IL-10 in patients with IBS. Materials and methods. The sample consisted of 81 patients, the diagnosis was verified according to the Rome criteria III. Polymorphism genotyping of IL-1Ra, IL-1b, IL-4, TNFα was carried out by PCR. Statistical processing: chi-square test, Fisher's exact test, odds ratio. The relationship between the heterozygous genotype G/A -308 TNFa and clinically relevant microbiological disorders in patients with irritable bowel syndrome was established...
2014: Experimental & Clinical Gastroenterology
G Tripathi, D Rangaswamy, M Borkar, N Prasad, R K Sharma, S N Sankhwar, S Agrawal
We evaluated whether polymorphisms in interleukin (IL-1) gene cluster (IL-1 alpha [IL-1A], IL-1 beta [IL-1B], and IL-1 receptor antagonist [IL-1RN]) are associated with end stage renal disease (ESRD). A total of 258 ESRD patients and 569 ethnicity matched controls were examined for IL-1 gene cluster. These were genotyped for five single-nucleotide gene polymorphisms in the IL-1A, IL-1B and IL-1RN genes and a variable number of tandem repeats (VNTR) in the IL-1RN. The IL-1B - 3953 and IL-1RN + 8006 polymorphism frequencies were significantly different between the two groups...
January 2015: Indian Journal of Nephrology
M W Pawlik, S Kwiecien, R Pajdo, A Ptak-Belowska, B Brzozowski, G Krzysiek-Maczka, M Strzalka, S J Konturek, T Brzozowski
Gastroesophageal reflux disease (GERD) is a global disease rapidly increasing among world population. The pathogenesis of reflux esophagitis which is considered as the early stage of GERD is complex, resulting from an imbalance between aggressive factors damaging the esophagus and a number of the natural defense mechanisms. The esophageal mucosa is in a state of continuous exposure to potentially damaging endogenous and exogenous factors. Important aggressive components of gastric refluxate include acid and pepsin and also pancreatic enzymes and bile...
December 2014: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
Tanju Keten, Yilmaz Aslan, Melih Balci, Altug Tuncel, Ovunc Bilgin, Cem Dilmen, Umit Ozdemir, Sedat Yahsi, Ozer Guzel, Ali Atan
OBJECTIVE: To compare the efficacy of 4 mg and 8 mg doxazosin XL treatments in patients with benign prostatic hyperplasia-related lower urinary tract symptoms and determine the efficiency of 8 mg in those patients with inadequate response to 4 mg. METHODS: A total of 162 patients were included in this study. Of the patients, 108 were randomized to receive 4 mg doxazosin XL (group 1), and 54 were randomized to receive 8 mg (group 2) treatments. After 1 month of treatment, 31 patients in group 1 whose quality of life (QoL) score was unchanged or had deteriorated were switched to 8 mg doxazosin XL treatment (group 1b)...
January 2015: Urology
Ursula Storch, Stephanie Blodow, Thomas Gudermann, Michael Mederos Y Schnitzler
OBJECTIVE: Myogenic vasoconstriction is mediated by vascular smooth muscle cells of resistance arteries sensing mechanical stretch. Angiotensin II AT1 receptors and in particular AT1BRs in murine vascular smooth muscle cells have been characterized as mechanosensors that cannot fully account for myogenic vasoconstriction observed. Therefore, we aimed at uncovering novel vascular mechanosensors by expression profiling and functional characterization of candidate proteins. APPROACH AND RESULTS: Analyzing myogenic tone of isolated murine mesenteric arteries of AT1A and AT1B receptor double gene-deficient (AT1A/1B (-/-)) mice ex vivo, we observed a decreased myogenic tone at high intraluminal pressures and an unexpected hyper-reactivity at low intraluminal pressures because of upregulation of cysteinyl leukotriene 1 receptors (CysLT1Rs)...
January 2015: Arteriosclerosis, Thrombosis, and Vascular Biology
Junli Chen, Adrian P Campbell, Kaniz F Urmi, Laurence P G Wakelin, William A Denny, Renate Griffith, Angela M Finch
A series of ring-substituted ethyl- and heptyl-linked 4-aminoquinoline dimers were synthesized and evaluated for their affinities at the 3 human α(1)-adrenoceptor (α(1)-AR) subtypes and the human serotonin 5-HT(1A)-receptor (5-HT(1A)-R). We find that the structure-specificity profiles are different for the two series at the α(1)-AR subtypes, which suggests that homobivalent 4-aminoquinolines can be developed with α(1)-AR subtype selectivity. The 8-methyl (8-Me) ethyl-linked analogue has the highest affinity for the α(1A)-AR, 7 nM, and the greatest capacity for discriminating between α(1A)-AR and α(1B)-AR (6-fold), α(1D)-AR (68-fold), and the 5-HT(1A)-R (168-fold)...
November 1, 2014: Bioorganic & Medicinal Chemistry
J J Huang, Y J Huang, L Zhu, M Yuan, L Huang
Alpha1-AR antagonists are currently first-line therapy for lower urinary tract symptoms associated with benign prostatic hyperplasia (LUTS/BPH). In this study, we report the synthesis of a new series of arylpiperazine derivatives containing acetophenone (3-17) which possess alpha1-adrenoreceptor blocking activity. The in vitro alpha1-adrenoreceptor blocking activity of each derivative was first screened using rabbit thoracic aortic rings by measuring the relaxation response (%) activated by (-)-noradrenaline (3 microM)...
August 2014: Die Pharmazie
Ma Trinidad Villamil-Hernández, Oscar Alcántara-Vázquez, Araceli Sánchez-López, Erika J Gutiérrez-Lara, David Centurión
The sympathetic nervous system that innervates the peripheral circulation is regulated by several mechanisms/receptors. It has been reported that prejunctional 5-HT1A, 5-HT1B, 5-HT1D, D2-like receptors and α2-adrenoceptors mediate the inhibition of the vasopressor sympathetic outflow in pithed rats. In addition, ergotamine, an antimigraine drug, displays affinity at the above receptors and may explain some of its adverse/therapeutic effects. Thus, the aims of this study were to investigate in pithed rats: (i) whether ergotamine produces inhibition of the vasopressor sympathetic outflow; and (ii) the major receptors involved in this effect...
October 5, 2014: European Journal of Pharmacology
Boris Monge-Roffarello, Sebastien M Labbe, Marie-Claude Roy, Marie-Laurence Lemay, Estelle Coneggo, Pierre Samson, Damien Lanfray, Denis Richard
The present study was designed to investigate the involvement of the cannabinoid receptor 1 (CB1) in the stimulating effects of the melanocortin-4 receptor (MC4R) agonism on whole-body and brown adipose tissue (BAT) thermogenesis. In a first series of experiments, whole-body and BAT thermogenesis were investigated in rats infused in the third ventricle of the brain with the MC4R agonist melanotan II (MTII) and the CB1 agonist δ9-tetrahydrocannabinol (δ(9)-THC) or the CB1 antagonist AM251. Whole-body thermogenesis was measured by indirect calorimetry and BAT thermogenesis assessed from interscapular BAT (iBAT) temperature...
September 2014: Endocrinology
A S Sarsenbaeva, E L Ivanova, A L Burmistrova, I V Drozdov
UNLABELLED: The aim of this study was to evaluate the presence or absence of a relationship between the variants of the course of IBS and their association with genetic polymorphisms of genes and intergenic interaction of cytokines. MATERIALS AND METHODS: The sample consisted of 81 patients, the diagnosis was verified according to the criteria of the Rome III, were isolated psychopathological, morphological complications, extra-intestinal symptoms. Polymorphism genotyping IL-1Ra, IL-b, IL-4, TNFa performed by PCR...
2013: Experimental & Clinical Gastroenterology
Takehiro Nakamura, Tetsuya Ikeda, Ryuichiro Takeda, Kaori Igawa, Rumi Naono-Nakayama, Sumio Sakoda, Toshikazu Nishimori, Yasushi Ishida
Milnacipran, a reuptake inhibitor of noradrenaline (NA) and serotonin (5-HT), elicits an antiallodynic effect in rats with neuropathic pain; however, the role of NA and 5-HT receptors in the induction of the antiallodynic effect of milnacipran remains unclear. Thus, we examined the effects of prazosin as an α1 adrenoceptor antagonist, yohimbine as an α2 adrenoceptor antagonist, metergoline as a 5-HT1, 5-HT2 and 5-HT7 receptor antagonist, cyanopindolol as a 5-HT1A/1B receptor antagonist, ketanserin as a 5-HT2 receptor antagonist, and ondansetoron as a 5-HT3 receptor antagonist on the antiallodynic effect of milnacipran in neuropathic rats with chronic constriction injury (CCI)...
September 5, 2014: European Journal of Pharmacology
E A Shpakova, K V Derkach, A O Shpakov
The ligand-recognizing part of G protein-coupled receptors consists of their extracellular loops and N-terminal domain. Identification of these sites is essential for receptor mapping and for the development and testing of new hormone system regulators. The peptides corresponding by their structure to extracellular loop 2 of serotonin 1B/1D receptor (peptide 1), extracellular loop 3 of melanocortin 3 receptor (peptide 2), and N-terminal domain of melanocortin 4 (peptide 3) were synthesized by the solid-phase method...
March 2014: Bulletin of Experimental Biology and Medicine
Zhou-Yang Jiao, Jing Wu, Chao Liu, Bing Wen, Wen-Zeng Zhao, Xin-Ling Du
The main purpose of this study was to investigate whether type 3 muscarinic acetylcholine receptor (M3R) dysfunction induced vascular hyperpermeability. Transwell system analysis showed that M3R inhibition by selective antagonist 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP) and small interfering RNA both increased endothelial permeability. Using coimmunoprecipitation and Western blot assay, we found that M3R inhibition increased VE-cadherin and β-catenin tyrosine phosphorylation without affecting their expression...
October 2014: BMB Reports
Bernardo G Gasperin, Rogério Ferreira, Monique T Rovani, Vilceu Bordignon, Raj Duggavathi, José Buratini, João F C Oliveira, Paulo B D Gonçalves
Bone morphogenetic proteins are known to be involved in determining ovulation rate in mammals. The mechanisms through which these proteins determine follicle fate are incompletely understood. In the present study, we used cattle as a model to evaluate the regulation of BMP15 and GDF9 receptors in granulosa cells during dominant follicle (DF) selection. Before follicular deviation (day 2 of the follicular wave), BMPR2 mRNA abundance tended to be higher in the second largest follicles (F2; P<0.1) compared to the future dominant follicle (F1)...
January 30, 2014: Animal Reproduction Science
Brian C Jensen, Timothy D OʼConnell, Paul C Simpson
Alpha-1-adrenergic receptors (ARs) are G protein-coupled receptors activated by catecholamines. The alpha-1A and alpha-1B subtypes are expressed in mouse and human myocardium, whereas the alpha-1D protein is found only in coronary arteries. There are far fewer alpha-1-ARs than beta-ARs in the nonfailing heart, but their abundance is maintained or increased in the setting of heart failure, which is characterized by pronounced chronic elevation of catecholamines and beta-AR dysfunction. Decades of evidence from gain and loss-of-function studies in isolated cardiac myocytes and numerous animal models demonstrate important adaptive functions for cardiac alpha-1-ARs to include physiological hypertrophy, positive inotropy, ischemic preconditioning, and protection from cell death...
April 2014: Journal of Cardiovascular Pharmacology
Felix Nau, Bangning Yu, David Martin, Charles D Nichols
Tumor necrosis factor alpha (TNF-α) plays a key role in inflammation, and its production and signaling contribute to many inflammatory related diseases. Recently, we discovered that selective activation of serotonin 5-HT2A receptors with the agonist (R)-DOI produces a super-potent blockade of proinflammatory markers in primary rat aortic smooth muscle cells. Here, we demonstrate that systemic administration of (R)-DOI can block the systemic effects of TNF-α in whole animal, with potent anti-inflammatory effects in the aortic arch and small intestine...
2013: PloS One
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