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Dissertations / Theses on the topic 'Antagonistes AT₁'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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1

Sidibé, Aïchata. "Modulation allostérique de l'affinité du recepteur at¦1 de l'angiotensine II pour des ligands agonistes et antagonistes." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1997. http://www.collectionscanada.ca/obj/s4/f2/dsk3/ftp04/mq21829.pdf.

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2

Sidibé, Aïchata. "Modulation allostérique de l'affinité du récepteur AT[indice inférieur 1] de l'angiotensine II pour des ligands agonistes et antagonistes." Mémoire, Université de Sherbrooke, 1996. http://savoirs.usherbrooke.ca/handle/11143/3113.

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Dans cette étude, nous nous sommes intéressés aux propriétés de liaison d'antagonistes de l'Ang II sur le récepteur AT[indice inférieur 1] et aux effets découplants de GTP[gamma]S et du pentosan sulfate (PS), un polyanion, sur la liaison de ces antagonistes. Nos résultats démontrent que le PS inhibe la liaison de [indice supérieur 125]I-Ang II (d'environ 50%) de façon comparable au GTP[gamma]S, avec un IC[indice inférieur 50] de 5.4 x 10[indice supérieur -7]M. Des études d'inhibition compétitive de la liaison de [indice supérieur 125]I-Ang II par le [Sar[indice supérieur 1],D-Phe[indice supéri

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3

Meulon, Emmanuelle. "Conception et synthèse de ligands potentiels des récepteurs AT1 et AT2 de l'angiotensine II." Lille 1, 2000. https://pepite-depot.univ-lille.fr/RESTREINT/Th_Num/2000/50376-2000-156.pdf.

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Le système rénine - angiotensine est reconnu aujourd'hui comme l'un des principaux systèmes régulateurs des fonctions cardio-vasculaires et rénales de l'organisme. Par son action vasoconstrictrice puissante, l'angiotensine II joue un rôle fondamental dans la physiopathologie de l'hypertension artérielle. Antagoniser l'angiotensine II, au niveau de son site d'action, constitue le moyen le plus sélectif et le plus efficace de s'opposer à toutes les actions de l'angiotensine II quelles que soient les voies de synthèse de cette hormone. Dans un premier temps, notre travail a consisté à synthétiser

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4

El-Ajouz, Sam. "Molecular basis of antagonist action at the P2X1 receptor." Thesis, University of Leicester, 2011. http://hdl.handle.net/2381/10260.

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P2X receptors are ATP-gated cation channels. P2X1 receptors are widely expressed throughout the body and have a range of functional roles, e.g. contraction of mesenteric arteries and regulation of blood clotting. The recent crystallisation of the zebra fish P2X4 receptor has provided a major advance in understanding the molecular basis of receptor properties. However, how agonists or antagonists are co-ordinated and the extent of the proposed ligand binding site have not been addressed at a structural level. A mutagenesis based approach was used to propose a model of the ATP binding site and h

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5

Lehoux, Julie. "Une mutation répertoriée du récepteur AT[indice inférieur 1] humain réduit l'affinité du Losartan un antagoniste non-peptidique de l'Angiotensine II." Mémoire, Université de Sherbrooke, 2012. http://hdl.handle.net/11143/6334.

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L'hypertension est une maladie qui, avec le vieillissement de la population, touche de plus en plus de gens. L'hypertension artérielle est généralement bien contrôlée par l'administration d'antihypertenseurs tels que les antagonistes des récepteurs AT[indice inférieur 1] .Ceux-ci sont très utilisés en clinique, puisqu'ils sont généralement très efficaces et présentent moins d'effets secondaires que les autres classes. Mais il y a parfois des patients pour qui les antagonistes (comme le Cozaar ou le Diovan) des récepteurs AT[indice inférieur 1] se montrent inefficaces ou présentent une efficaci

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6

Damer, Susanne. "Pharmacological evaluation of NF279 as a P2 receptor antagonist structure activity relationship studies of analogues of the P2 receptor antagonists Suramin and NF023 at native P2 receptor subtypes and ecto-nucleotidases /." [S.l.] : [s.n.], 2002. http://deposit.ddb.de/cgi-bin/dokserv?idn=965187896.

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7

Wooden, Ekaphol. "Synthesis of Novel Biologically Active Peptide Analogues that are Agonists at Opioid Receptors and Antagonists at Cholecystokinin Receptors." Thesis, Tucson, Ariz. : University of Arizona, 2005. http://etd.library.arizona.edu/etd/GetFileServlet?file=file:///data1/pdf/etd/azu%5Fetd%5F1282%5F1%5Fm.pdf&type=application/pdf.

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8

Yan, Teng. "Pharmacological Evaluation of a Putative M5 Antagonist at M1, M3 and M5 Receptors." University of Toledo Health Science Campus / OhioLINK, 2015. http://rave.ohiolink.edu/etdc/view?acc_num=mco1404739223.

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9

Jones, Philip Leslie St John. "Structure-activity studies of novel compounds acting at metabotropic excitatory amino acid receptors in neonatal rat spinal motoneurons." Thesis, University of Bristol, 1994. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.385687.

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10

Polaske, Nathan Walter. "STRUCTURAL ANALYSIS AND SYNTHETIC PROGRESS TOWARDS SMALL MOLECULES AS MODULATORS OF ANGIOGENESIS AT THE CELLULAR AND TRANSCRIPTIONAL LEVELS." Diss., The University of Arizona, 2008. http://hdl.handle.net/10150/194357.

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Progress towards the design and the application of small molecules as inhibitors of angiogenesis is reported. First, the regulation of hypoxia inducible transcription with epipolythiodioxopiperazine (ETP) natural products is discussed, beginning with the exploration of the physical and chemical properties of ETP skeletal analogs, xylylene-linked bis-diketopiperazines (1,4-piperazine-2,5-diones, DKPs).The design, synthesis and solid-state structures of a new class of xylylene-linked bis(1,4-piperazine-2,5-diones) are reported in an effort to extend the molecular framework of piperazine-2,5-dio

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11

Agnes, Richard S. "New paradigm for drug design: Design and synthesis of novel biologically active peptides that are agonists at opioid receptors and antagonists at cholecystokinin receptors." Diss., The University of Arizona, 2003. http://hdl.handle.net/10150/280340.

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We now know from genomics that many disease states lead to changes in expressed proteins (adaptation/plasticity). Therefore, drug design and discovery based on normal states and single targets often is inadequate or even counter-indicated. Therefore, the "system changes" that have occurred must be considered in any treatment for the disease. Such "systems changes" are clearly evident in neuropathic pain where opioids can actually heighten pain. In these pain states there are increased levels of neurotransmitters such as cholecystokinin (CCK) in which both the peptides and their receptors are i

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12

Troppmann, Britta, Sabine Balfanz, Arnd Baumann, and Wolfgang Blenau. "Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5-HT1 receptor." Universität Potsdam, 2010. http://opus.kobv.de/ubp/texte_eingeschraenkt_verlag/2010/4434/.

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Background and purpose: 5-Hydroxytryptamine (5-HT) has been shown to control and modulate many physiological and behavioural functions in insects. In this study, we report the cloning and pharmacological properties of a 5-HT1 receptor of an insect model for neurobiology, physiology and pharmacology. Experimental approach: A cDNA encoding for the Periplaneta americana 5-HT1 receptor was amplified from brain cDNA. The receptor was stably expressed in HEK 293 cells, and the functional and pharmacological properties were determined in cAMP assays. Receptor distribution was investigated by RT-PC

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13

Hagenow, Stefanie [Verfasser], Holger [Gutachter] Stark, and Holger [Gutachter] Gohlke. "Histamine H3 receptor antagonists with multitargeting properties at GPCRs and enzymes / Stefanie Hagenow ; Gutachter: Holger Stark, Holger Gohlke." Düsseldorf : Universitäts- und Landesbibliothek der Heinrich-Heine-Universität Düsseldorf, 2019. http://d-nb.info/1178112543/34.

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14

Olson, Keith Mathew, and Keith Mathew Olson. "Atypical Opioid Interactions – Development of Selective Mu-Delta Heterodimer Antagonists, Clinical Opioids at Non-Mu Pain Targets and Endogenous Biased Signaling." Diss., The University of Arizona, 2017. http://hdl.handle.net/10150/626669.

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Most clinical opioids produce analgesia through the Mu Opioid Receptor (MOR) providing the only effective treatment for chronic pain patients. These studies explore three pre-clinical strategies to improve MOR analgesia and minimize side effects: 1) compounds that target G-protein Coupled Receptors (GPCRs) heterodimers, such as heterodimerization between the Delta Opioid Receptor (DOR) and MOR (MDOR); 2) multi-functional compounds that target multiple receptor systems for synergistic effects, such as a MOR agonist and a the serotonin reuptake transporter (SERT) inhibitor; or 3) biased agonists

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15

Harr, Jennifer C. "An electrophysiological study of the effects of resveratrol and catechin at GABAa receptors." Scholarly Commons, 2007. https://scholarlycommons.pacific.edu/uop_etds/649.

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Resveratrol and catechin have behavioral and neuroprotective effects that may be due to their interaction with neuronal ion channels. It was hypothesized that the grape compounds, resveratrol and catechin modulate GABAAA receptors. To address this hypothesis, the effects of resveratrol and catechin were investigated on human recombinant GABAA receptors expressed in HEK-293 cells using electrophysiological techniques.<.p> HEK-293 cells were cultured and transfected using eDNA encoding human GABAA receptors. GABA-evoked currents were recorded from HEK cells 24-48 hours following transfectio

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16

Mentro, Anne M. "Vitamin A status and inflammation during the first week of life in extremely premature infants at risk for bronchopulmonary dysplasia." Connect to this title online, 2004. http://rave.ohiolink.edu/etdc/view?acc%5Fnum=osu1092500146.

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Thesis (Ph. D.)--Ohio State University, 2004.<br>Title from first page of PDF file. Document formatted into pages; contains xiv, 133 p.; also includes graphics (some col.) Includes bibliographical references (p. 107-133). Available online via OhioLINK's ETD Center

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17

Green, Belinda K. W. "Thrombolytic therapy and beta-adrenergic blockade in acute myocardial infarction : a prospective evaluation at Groote Schuur Hospital 1988-1990." Master's thesis, University of Cape Town, 1991. http://hdl.handle.net/11427/27126.

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The advent of intravenous thrombolytic agents has revolutiontzed the management of patients with acute myocardial infarction and has dramatically altered the morbidity and mortality associated with this condition. The aims of this study in patients presenting with acute myocardial infarction and treated with thrombolytic agents are: 1. To evaluate the efficacy of thrombolytic agents used at Groote Schuur Hospital in terms of (a) patency of the infarct related artery; ( b) short and long-term mortality. 2. To assess the feasibility and safety of combining intravenous beta-adrenergic blockade wi

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18

Merges, Dominik [Verfasser], Eike Lena [Gutachter] Neuschulz, and Meike [Gutachter] Piepenbring. "Mutualistic and antagonistic effects of plant-animal and plant-fungal interactions on plant recruitment at the tree line / Dominik Merges ; Gutachter: Eike Lena Neuschulz, Meike Piepenbring." Frankfurt am Main : Universitätsbibliothek Johann Christian Senckenberg, 2020. http://d-nb.info/120699844X/34.

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19

Abbott, Mary-Alice. "Structural and Signaling Proteins at the Synapse: Dystroglycan & Insulin Receptor Tyrosine Kinase Substrate p58/53: a Dissertation." eScholarship@UMMS, 1999. https://escholarship.umassmed.edu/gsbs_diss/124.

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The synapse is the primary locus of cell-cell communication in the nervous system. The elaboration of a functional synapse requires both a specialized structure and an efficient communication system. For my thesis work, I studied proteins implicated in each of these functions: the structural molecules dystroglycan and dystrophin, and the signaling elements Insulin Receptor Substrate p58/53 and insulin receptor. The α/β-dystroglycan complex, believed to be the heart of cellmatrix adhesion in muscle and other tissues, provides a link between dystrophin, a cytoskeletal protein at the base of the

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20

Damayanti, Sophi [Verfasser]. "Novel agonists and potent antagonists at P2Y11 purinergic receptors: synthesis and biological testing = Neue Agonisten und potente Antagonisten an P2Y11-Purinergic-Rezeptoren: Synthese und biologische Untersuchung / vorgelegt von Sophi Damayanti." 2008. http://d-nb.info/991824679/34.

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21

Duguay, David. "Rôles et mécanismes moléculaires de l'apoptose cardiovasculaire en réponse à des antihypertenseurs." Thèse, 2007. http://hdl.handle.net/1866/15519.

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22

Damer, Susanne [Verfasser]. "Pharmacological evaluation of NF279 as a P2 receptor antagonist : structure activity relationship studies of analogues of the P2 receptor antagonists Suramin and NF023 at native P2 receptor subtypes and ecto-nucleotidases / von Susanne Damer." 2002. http://d-nb.info/965187896/34.

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23

Hongwiset, Darunee [Verfasser]. "Development of potent and selective antagonists at P2Y1_tn1 receptors: symmetrical and asymmetrical derivatives of NF340 / vorgelegt von Darunee Hongwiset." 2008. http://d-nb.info/991240456/34.

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24

Linder, Matthias [Verfasser]. "Radioligand binding studies : structure affinity relationships of antagonists at muscarinic, serotonergic and histaminergic receptor subtypes = Radioligandbindungsstudien / by Matthias Linder." 2008. http://d-nb.info/988089963/34.

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