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Dissertations / Theses on the topic 'Adenosine receptors antagonists'

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Published: 9 March 2023

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1

Paoletta, Silvia. "Designing adenosine receptors antagonists using an in silico approach." Doctoral thesis, Università degli studi di Padova, 2012. http://hdl.handle.net/11577/3422906.

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The neuromodulator adenosine affects a wide variety of physiopathological processes through activation of four receptors, classified as A1, A2A, A2B, and A3 subtypes. Adenosine receptors (ARs) belong to family A of G protein-coupled receptors (GPCRs) and are ubiquitously expressed in the human body. Activation or blockade of ARs is responsible for a wide range of effects in numerous organ systems; and therefore the regulation of ARs can have many potential therapeutic applications. The main objective of this project has been the investigation of the in silico molecular pharmacology of adenosi

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2

Beauglehole, Anthony Robert, and anthony@adenrx com. "N3-substituted xanthines as irreversible adenosine receptor antagonists." Deakin University. School of Biological and Chemical Sciences, 2000. http://tux.lib.deakin.edu.au./adt-VDU/public/adt-VDU20080612.084330.

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8-Cyclopentyl-3-(3-(4-fluorosulfonylbenzoyl)oxy)propyl-propylxanthine (44, FSCPX) has been reported to exhibit potent and selective irreversible antagonism of the A1 adenosine receptor when using in vitro biological preparations. However, FSCPX (44) suffers from cleavage of the ester linkage separating the reactive 4-(fluorosulfonyl)phenyl moiety from the xanthine pharmacophore when used in in vivo biological preparations or preparations containing significant enzyme activity, presumably by esterases. Cleavage

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3

SAPONARO, Giulia. "Design and Synthesis of New A2A and A3 Adenosine Receptors Antagonists." Doctoral thesis, Università degli studi di Ferrara, 2009. http://hdl.handle.net/11392/2388703.

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The aim of this work was the design and synthesis of new A2A and A3 adenosine receptors antagonists. Two different studies have been performed. The first one based on structural modifications of the pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pirimidine nucleus, reported in literature. In order to identify a new series of A2A or A3 AR antagonists and with the aim to better investigate the role of the nitrogen at the 7- position on the interaction with ARs, it was performed a synthetic strategy for the preparation of the pyrrolo[3,4-e][1,2,4]triazolo[1,5-c]pyrimidine nucleus which can be considered

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4

Do, Khoa Quang. "Design, Synthesis and Binding Studies of Trisubstitutedpyrazolo[3,4-d]pyrimidines." Thesis, Griffith University, 2006. http://hdl.handle.net/10072/367533.

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Pyrazolo[3,4-d]pyrimidines were known as adenosine antagonists at the rat A1 and A2A adenosine receptors based on our previous studies. In this study, 245 pyrazolo[3,4-d]pyrimidines derivatives with various benzyl substitutents at N-1 and various hydrophobic side chains at C-4 and C-6 were synthesized and screened at the human A1, A2A and A3 adenosine receptors. 14 out of 245 compounds were resynthesized and purified to determine the Ki values of these compounds at the human A1 adenosine receptor. Chapter 1 of the thesis is a literature review of adenosine research. It describes the physiology

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5

Morizzo, Erika. "G Protein-Coupled Receptors as Potential Drug Target: From Receptor Topology to Rational Drug Design, an in-silico Approach." Doctoral thesis, Università degli studi di Padova, 2009. http://hdl.handle.net/11577/3426081.

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G protein-coupled receptors (GPCRs) constitute a very large family of heptahelical, integral membrane proteins that mediate a wide variety of physiological processes, ranging from the transmission of the light and odorant signals to the mediation of neurotransmission and hormonal actions. GPCRs are dysfunctional or deregulated in several human diseases and are estimated to be the target of more than 40% of drugs used in clinical medicine today. The crystal structures of rhodopsin and the recent published crystal structures of beta-adrenergic receptors and human A2A Adrenergic Receptor pr

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6

Van, der Walt Mietha Magdalena. "Syntheses of sulfanylphthalimide and xanthine analogues and their evaluation as inhibitors of monoamine oxidase and as antagonists of adenosine receptors / Mietha Magdalena van der Walt." Thesis, North-West University, 2013. http://hdl.handle.net/10394/9537.

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Currently L-DOPA is the drug most commonly used for the treatment of Parkinson’s disease (PD). However, the long-term use of L-DOPA is associated with the development of motor fluctuations and dyskinesias. Treatment mainly addresses the dopaminergic features of the disease and leaves its progressive course unaffected. An optimal treatment would be a combination of both motor and non-motor symptom relief with neuroprotective properties. Two drug targets have attracted the attention for PD treatment, namely monoamine oxidase B (MAOB) and adenosine A2A receptors. MAO-B inhibitors enhance the elev

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7

Robinson, Sarel Johannes. "Syntheses of chalcones and 2-aminopyrimidines and their evaluation as monoamine oxidase inhibitors and as adenosine receptor antagonists / Sarel Johannes Robinson." Thesis, North-West University, 2013. http://hdl.handle.net/10394/9534.

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Background and rationale - Parkinson’s disease is a neurodegenerative disorder characterised by reduced levels of dopamine in the brain. The cause of Parkinson's disease is still unknown; however several theories pertaining to the etiology exist. Current treatment mainly aims at dopamine replacement, with agents such as levodopa and dopamine agonists that provide patients with symptomatic relief. This relief is unfortunately only temporary as the progression of the disease is not halted. Furthermore, these therapies are associated with a range of side effects and novel approaches to the treat

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8

BARALDI, Stefania. "Design and Synthesis of New A2B Adenosine Receptor Antagonists." Doctoral thesis, Università degli studi di Ferrara, 2009. http://hdl.handle.net/11392/2388704.

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Starting from chemical structure of N-benzo-[1,3]dioxol-5-yl-2-[5-(2,6dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-1-methyl-1H-pyrazol3-yloxy]-acetamide, MRE2029F20* various structural modifications were realized to afford a new series of A2B antagonists. The bioisosteric replacement of the anilide moiety with benzimidazole or quinazoline rings, the effect of the substitution of pyrazole with isoxazole moiety were investigated. Amide bond has been also replaced with the 5phenyl-1,2,4-oxadiazole nucleus on the basis of other adenosine pharmacophores reported previously. In this con

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9

McKeveney, Declan, and n/a. "The Solid-Phase Combinatorial Synthesis of 2,6,9- Trisubstituted Purines as Potential Adenosine A3 Receptor Antagonists." Griffith University. School of Science, 2005. http://www4.gu.edu.au:8080/adt-root/public/adt-QGU20050830.120105.

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Purines as a class of compounds have been implicated in many biological systems, including as adenosine receptor antagonists. A method of synthesising 2,6,9-trisubstituted purines would be useful to produce small libraries of compounds for probing adenosine receptor selectivity. A library of trisubstituted purines has been achieved using a solid-phase methodology. The electronic properties of the substrate were found to result in difficulties with the loading of substrate onto the resin. Theoretical calculations provided the basis for mono-substitution in order to activate the substrate. This

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10

McKeveney, Declan. "The Solid-Phase Combinatorial Synthesis of 2,6,9- Trisubstituted Purines as Potential Adenosine A3 Receptor Antagonists." Thesis, Griffith University, 2005. http://hdl.handle.net/10072/367926.

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Purines as a class of compounds have been implicated in many biological systems, including as adenosine receptor antagonists. A method of synthesising 2,6,9-trisubstituted purines would be useful to produce small libraries of compounds for probing adenosine receptor selectivity. A library of trisubstituted purines has been achieved using a solid-phase methodology. The electronic properties of the substrate were found to result in difficulties with the loading of substrate onto the resin. Theoretical calculations provided the basis for mono-substitution in order to activate the substrate. This

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11

Morato, Manuela Sofia Rodrigues. "Hipertensão causada por um antagonista dos receptores da adenosina : Papel da angiotensina II." Doctoral thesis, Universidade do Porto. Reitoria, 2004. http://hdl.handle.net/10216/9602.

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12

Morato, Manuela Sofia Rodrigues. "Hipertensão causada por um antagonista dos receptores da adenosina : Papel da angiotensina II." Tese, Universidade do Porto. Reitoria, 2004. http://hdl.handle.net/10216/9602.

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13

Aguiar, Lissiana Magna Vasconcelos. "Antagonismo do receptor da adenosina A2a: Nova perspectiva para o tratamento da doenÃa de Parkinson." Universidade Federal do CearÃ, 2009. http://www.teses.ufc.br/tde_busca/arquivo.php?codArquivo=3047.

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Conselho Nacional de Desenvolvimento CientÃfico e TecnolÃgico<br>A doenÃa de Parkinson (DP) Ã uma desordem neurodegenerativa, caracterizada pela destruiÃÃo dos neurÃnios nigroestriatais dopaminÃrgicos. O tratamento atual para esta doenÃa estÃ restrito ao alÃvio sintomÃtico, porque atÃ o presente momento nÃo existem agentes capazes de inibir a degeneraÃÃo neuronal. Existem evidÃncias experimentais de que antagonistas de receptores A2A da adenosina poderiam ser Ãteis no tratamento de DP. Com a finalidade de investigar essa possibilidade, o presente trabalho demonstrou os efeitos da cafeÃna e do

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14

Aguiar, Lissiana Magna Vasconcelos. "Antagonismo do receptor da adenosina A2a : nova perspectiva para o tratamento da doença de Parkinson." reponame:Repositório Institucional da UFC, 2009. http://www.repositorio.ufc.br/handle/riufc/2744.

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AGUIAR, Lissiana Magna Vasconcelos. Antagonismo do receptor da adenosina A2a : nova perspectiva para o tratamento da doença de Parkinson. 2009. 215 f. Tese (Doutorado em Farmacologia) - Universidade Federal do Ceará. Faculdade de Medicina, Fortaleza, 2009.<br>Submitted by denise santos (denise.santos@ufc.br) on 2012-06-14T12:05:44Z No. of bitstreams: 1 2009_tese_lmvaguiar.pdf: 4247715 bytes, checksum: 824a44fc5b2266d47deaa9a03cb884de (MD5)<br>Approved for entry into archive by Eliene Nascimento(elienegvn@hotmail.com) on 2012-06-14T12:52:54Z (GMT) No. of bitstreams: 1 2009_tese_lmvaguiar.pdf: 4

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15

Carmo, Marta Regina Santos do. "Efeito neuroprotetor do antagonismo do receptor P2X7 no Parkinsonismo experimental induzido por 6-OHDA." reponame:Repositório Institucional da UFC, 2015. http://www.repositorio.ufc.br/handle/riufc/11458.

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CARMO, Marta Regina Santos do. Efeito neuroprotetor do antagonismo do receptor P2X7 no Parkinsonismo experimental induzido por 6-OHDA. 2015. 110 f. Tese (Doutorado em Farmacologia) - Faculdade de Medicina, Universidade Federal do Ceará, Fortaleza, 2015.<br>Submitted by denise santos (denise.santos@ufc.br) on 2015-04-17T13:13:51Z No. of bitstreams: 1 2015_tese_mrscarmo.pdf: 2518438 bytes, checksum: 237c71b94e431515b74c222c224d8c8e (MD5)<br>Approved for entry into archive by denise santos(denise.santos@ufc.br) on 2015-04-17T13:14:18Z (GMT) No. of bitstreams: 1 2015_tese_mrscarmo.pdf: 2518438 byt

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16

By, Youlet. "Modulation des récepteurs de l'adénosine par anticorps monoclonaux et ligands synthétiques. : application en physiopathologie humaine." Thesis, Aix-Marseille 2, 2010. http://www.theses.fr/2010AIX20688/document.

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L’adénosine est un nucléoside ubiquitaire qui exerce un contrôle puissant sur les systèmes nerveux,immunitaire et cardiovasculaire par l’intermédiaire de quatre récepteurs membranaires : A1R, A2AR, A2BR etA3R. L’étude des récepteurs de l’adénosine est nécessaire à la compréhension de physio‐pathologieshumaines non encore élucidées. Pour étudier l’expression des A2AR, nous avons, dans une première étude,produit un anticorps monoclonal, appelé Adonis, d’isotype IgM, . Adonis reconnait un épitope linéaire desept acides aminés sur la partie C‐terminale de la seconde boucle extra‐cellulaire de l’A

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17

Affini, Anna [Verfasser]. "Histamine H3 receptor antagonists in combination with monoamine oxidase B and adenosine A1/A2A receptor ligands as multi-target approach for the treatment of Parkinson´s disease / Anna Affini." Düsseldorf : Universitäts- und Landesbibliothek der Heinrich-Heine-Universität Düsseldorf, 2019. http://d-nb.info/1190350807/34.

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18

Harmse, Rozanne. "Syntheses of 8-(phenoxymethyl)caffeine analogues and their evaluation as inhibitors of monoamine oxidase and as antagonists of the adenosine A2A receptor / Rozanne Harmse." Thesis, North-West University, 2013. http://hdl.handle.net/10394/9663.

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Background and rationale: Parkinson’s disease (PD) is a progressive, degenerative disorder of the central nervous system and is characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta. The loss of functional dopamine in the striatum is thought to be responsible for the typical symptoms of PD. Cardinal features of PD include bradykinesia, muscular rigidity, resting tremor and impairment of postural balance. This study focuses on the inhibition of monoamine oxidase B (MAO-B) and antagonism of A2A receptors as therapeutic strategies for PD. Monoamine oxidase (MAO)

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19

Pretorius, Judey. "The synthesis and evaluation of caffeine analogues as inhibitors of monoamine oxidase B and antagonists of the adenosine A₂A receptor / by Judey Pretorius." Thesis, North-West University, 2008. http://hdl.handle.net/10394/4127.

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The adenosine A2A receptor has emerged as an attractive target for the treatment of Parkinson's disease (PD). Evidence suggests that antagonists of the A2A receptor (A2A antagonists) partially alleviate the symptoms of PD, prevent the development of motor complications and may also slow the underlying neurodegenerative process. It was recently reported that several members of the (E)-8-styrylcaffeine class of A2A antagonists also are potent inhibitors of monoamine oxidase B (MAO-B).<br>Thesis (Ph.D. (Pharmaceutical Chemistry))--North-West University, Potchefstroom Campus, 2009.

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20

Mazzali, Marilda 1963. "Proposta para o tratamento da policitemia pos-transplantes renal : antagonista dos receptores de adenosina e inibidor de enzima conversora da angiotensina." [s.n.], 1996. http://repositorio.unicamp.br/jspui/handle/REPOSIP/309430.

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Orientador: Gentil Alves Filho<br>Tese (doutorado) - Universidade Estadual de Campinas, Faculdade de Ciencias medicas<br>Made available in DSpace on 2018-07-21T15:36:59Z (GMT). No. of bitstreams: 1 Mazzali_Marilda_D.pdf: 3503386 bytes, checksum: e50d45cdecf9e3a0e4c21b6829105625 (MD5) Previous issue date: 1996<br>Resumo: A policitemia é uma complicação freqüente após o transplante renal, estando associada a um maior risco de fenômenos tromboembólicos. Apesar de controvérsias a respeito de sua patogênese, várias terapêuticas têm sido propostas. Para analisar o efeito de dois grupos de drogas s

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21

Gull, Mazhar [Verfasser], and André [Akademischer Betreuer] Brändli. "In vivo pharmacological profiling in Xenopus embryos defines a subset of A1 adenosine receptor-selective antagonists with potent anti-angiogenic activities / Mazhar Gull ; Betreuer: André Brändli." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2017. http://d-nb.info/1137226765/34.

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22

Sandqvist, Anna. "Vardenafil and methylarginines in pulmonary hypertension." Doctoral thesis, Umeå universitet, Klinisk farmakologi, 2016. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-113903.

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Background: Pulmonary hypertension (PH) is a rare condition characterized by endothelial dysfunction and vascular remodelling, leading to increased pulmonary vascular resistance (PVR) and right ventricular heart failure. Endothelial dysfunction is associated with an imbalance between vasoconstrictor compounds, such as endothelin and thromboxane A2, and vasodilator compounds, such as prostacyclin and nitric oxide (NO). Asymmetric dimethylarginine (ADMA), a methyl derivate of L-arginine, inhibits synthesis of NO. Vardenafil, a phosphodiesterase type 5 inhibitor (PDE5-inhibitors), causes vasodila

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23

Fromonot, Julien. "Implication de l'adénosine en physiopathologie cardiovasculaire." Thesis, Aix-Marseille, 2015. http://www.theses.fr/2015AIXM5041.

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L’adénosine (ADO) est un nucléoside ubiquitaire issu de l’ATP et du cycle de la méthionine. Via les récepteurs A1 (A1R), elle favorise la fibrillation atriale (FA). Via les récepteurs A2A (A2AR), elle induit une dilatation coronaire. L’ADO est donc un intermédiaire métabolique et un neurotransmetteur du système cardiovasculaire.La 1ère étude montre que, chez les patients coronariens, l’ADO est corrélée à l’homocystéine (Hcy) et l’uricémie. De plus, l’ADO et l’Hcy sont corrélées au score évaluant l’étendue de l’athérosclérose (score SYNTAX). Enfin, sur un modèle d’hépatocyte, l’ADO induit la pr

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24

Duroux, Romain. "Conception, synthèse et évaluation d'antagonistes des récepteurs A2A." Thesis, Lille 2, 2017. http://www.theses.fr/2017LIL2S015/document.

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La maladie d’Alzheimer (MA) est la maladie neurodégénérative touchant le plus de personnes dans le monde. Jusqu’à présent, aucun traitement curatif n’existe pour soigner cette maladie, d’où la nécessité d’identifier et d’étudier de nouvelles cibles thérapeutiques.La découverte des effets bénéfiques de la caféine, antagoniste du récepteur à adénosine A2A (A2AR), conjuguée à une surexpression de ce dernier chez les patients atteints de la MA, font de ce récepteur une cible d’intérêt. En effet, des antagonistes des A2ARs ont montré leur capacité à améliorer les performances cognitives de par une

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25

Dziedzic, Katarzyna. "Charakterystyka molekularnego mechanizmu działania innowacyjnych związków małocząsteczkowych w immunoterapii nowotworów." Praca doktorska, 2022. https://ruj.uj.edu.pl/xmlui/handle/item/287974.

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26

Katsidzira, Runako Masline. "Affinity of dihydropyrimidone analogues for adenosine A1 and A2A receptors / Runako Masline Katsidzira." Thesis, 2014. http://hdl.handle.net/10394/10747.

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Parkinson’s disease (PD) is a neurodegenerative disorder that is characterised by a reduction of dopamine concentration in the striatum due to degeneration of dopaminergic neurons in the substantia nigra. Currently, first line treatment of PD includes the use of dopamine precursors, dopamine agonists and inhibitors of enzymatic degradation of dopamine, in an effort to restore dopamine levels and/or its effects. However, all these therapeutic strategies are only symptomatic and unfortunately do not slow, stop or reverse the progression of PD. From the discovery of adenosine A2A receptor-dopamin

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27

En-ChiuanChang and 張恩銓. "Syntheses and Applications of Adenosine Receptor Antagonists and Electroluminescent Materials from Sydnones." Thesis, 2013. http://ndltd.ncl.edu.tw/handle/67075494771744921409.

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博士<br>國立成功大學<br>化學系碩博士班<br>101<br>Pyrazole is the aromatic heterocyclic compound with the five-membered ring, and it is usually considered a kind of alkaloid. Derivatives of pyrazole are important compounds in pharmaceutical industry, and they are used for their antipyretic, anti-inflammatory, antipyretic, tranquilizing, muscle relaxing and antibacterial activities. In addition, they are also applied in organic light-emitting diode(OLED). The potential therapeutical applications of antagonizing the A3 adenosine receptor(A3 AR) by derivatives of pyrazole have been investigated in recent yea

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Neves, Ana Catarina Rodrigues. "The impact of elevated hydrostatic pressure in microglia : chances in the adenosinergic system and inflammatory responses." Master's thesis, 2015. http://hdl.handle.net/10316/29950.

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Dissertação de mestrado em Investigação Biométrica, apresentada à Faculdade de Medicina da Universidade de Coimbra<br>O glaucoma é uma doença neurodegenerativa e sem cura, caracterizada pela morte das células ganglionares da retina e pela atrofia do nervo ótico. É a segunda causa de cegueira irreversível em todo o mundo, estimando-se que a sua prevalência aumente para o dobro até 2040. O aumento da pressão intraocular (PIO) é considerado o principal fator de risco para o desenvolvimento de glaucoma e, os atuais tratamentos focam-se no controlo da PIO. Contudo, alguns doentes continuam a perder

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