Готові списки джерел за темами / P2X3 antagonist

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Добірка наукової літератури з теми "P2X3 antagonist"

Автор: Grafiati
Опубліковано: 14 березня 2023

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Статті в журналах з теми "P2X3 antagonist"

1

Coutinho-Silva, Robson, Lynn Stahl, Kwok-Kuen Cheung, et al. "P2X and P2Y purinergic receptors on human intestinal epithelial carcinoma cells: effects of extracellular nucleotides on apoptosis and cell proliferation." American Journal of Physiology-Gastrointestinal and Liver Physiology 288, no. 5 (2005): G1024—G1035. http://dx.doi.org/10.1152/ajpgi.00211.2004.

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Анотація:
Extracellular nucleotides interact with purinergic receptors, which regulate ion transport in a variety of epithelia. With the use of two different human epithelial carcinoma cell lines (HCT8 and Caco-2), we have shown by RT-PCR that the cells express mRNA for P2X1, P2X3, P2X4, P2X5, P2X6, P2X7, P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, and P2Y12 receptors. Protein expression for P2Y1 and P2Y2 receptors was also demonstrated immunohistochemically, and P2X receptor subtype protein was present in the following decreasing order: P2X4 > P2X7 > P2X1 > P2X3 > P2X6 > P2X5 >> P2X2. The funct
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2

Nakamura, Ei'Ichiro, Yasuhito Uezono, Ken'Ichiro Narusawa, et al. "ATP activates DNA synthesis by acting on P2X receptors in human osteoblast-like MG-63 cells." American Journal of Physiology-Cell Physiology 279, no. 2 (2000): C510—C519. http://dx.doi.org/10.1152/ajpcell.2000.279.2.c510.

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Анотація:
In human osteoblast-like MG-63 cells, extracellular ATP increased [3H]thymidine incorporation and cell proliferation and synergistically enhanced platelet-derived growth factor- or insulin-like growth factor I-induced [3H]thymidine incorporation. ATP-induced [3H]thymidine incorporation was mimicked by the nonhydrolyzable ATP analogs adenosine 5′- O-(3-thiotriphosphate) and adenosine 5′-adenylylimidodiphosphate and was inhibited by the P2 purinoceptor antagonist suramin, suggesting involvement of P2 purinoceptors. The P2Y receptor agonist UTP and UDP and a P2Y receptor antagonist reactive blue
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3

Nunes, Ana R., Raul Chavez-Valdez, Tarrah Ezell, David F. Donnelly, Joel C. Glover, and Estelle B. Gauda. "Effect of development on [Ca2+]i transients to ATP in petrosal ganglion neurons: a pharmacological approach using optical recording." Journal of Applied Physiology 112, no. 8 (2012): 1393–402. http://dx.doi.org/10.1152/japplphysiol.00511.2011.

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Анотація:
ATP, acting through P2X2/P2X3 receptor-channel complexes, plays an important role in carotid body chemoexcitation in response to natural stimuli in the rat. Since the channels are permeable to calcium, P2X activation by ATP should induce changes in intracellular calcium ([Ca2+]i). Here, we describe a novel ex vivo approach using fluorescence [Ca2+]i imaging that allows screening of retrogradely labeled chemoafferent neurons in the petrosal ganglion of the rat. ATP-induced [Ca2+]i responses were characterized at postnatal days (P) 5–8 and P19–25. While all labeled cells showed a brisk increase
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4

Gui, Yu, ZengYong Wang, XiaoRui Sun, et al. "Uridine adenosine tetraphosphate induces contraction of airway smooth muscle." American Journal of Physiology-Lung Cellular and Molecular Physiology 301, no. 5 (2011): L789—L794. http://dx.doi.org/10.1152/ajplung.00203.2011.

Повний текст джерела
Анотація:
Contraction of airway smooth muscle (ASM) plays an important role in the regulation of air flow and is potentially involved in the pathophysiology of certain respiratory diseases. Extracellular nucleotides regulate ASM contraction via purinergic receptors, but the signaling mechanisms involved are not fully understood. Uridine adenosine tetraphosphate (Up4A) contains both pyrimidine and purine moieties, which are known to potentially activate P2X and P2Y receptors. Both P2X and P2Y receptors have been identified in the lung, including airway epithelial cells and ASM. We report here a study of
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5

Hu, Bo, Chen Yu Chiang, James W. Hu, Jonathan O. Dostrovsky, and Barry J. Sessle. "P2X Receptors in Trigeminal Subnucleus Caudalis Modulate Central Sensitization in Trigeminal Subnucleus Oralis." Journal of Neurophysiology 88, no. 4 (2002): 1614–24. http://dx.doi.org/10.1152/jn.2002.88.4.1614.

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Анотація:
This study investigated the role of trigeminal subnucleus caudalis (Vc) P2X receptors in the mediation of central sensitization induced in nociceptive neurons in subnucleus oralis (Vo) by mustard oil (MO) application to the tooth pulp in anesthetized rats. MO application produced a long-lasting central sensitization reflected in neuroplastic changes (i.e., increases in neuronal mechanoreceptive field size and responses to innocuous and noxious mechanical stimuli) in Vo nociceptive neurons. Twenty minutes after MO application, the intrathecal (i.t.) administration to the rostral Vc of the selec
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6

Gomes, Dayane A., Zhilin Song, Wanida Stevens, and Celia D. Sladek. "Sustained stimulation of vasopressin and oxytocin release by ATP and phenylephrine requires recruitment of desensitization-resistant P2X purinergic receptors." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 297, no. 4 (2009): R940—R949. http://dx.doi.org/10.1152/ajpregu.00358.2009.

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Анотація:
Coexposure of hypothalamo-neurohypophyseal system explants to ATP and phenylephrine [PE; an α1-adrenergic receptor (α1-AR) agonist] induces an extended elevation in vasopressin and oxytocin (VP/OT) release. New evidence is presented that this extended response is mediated by recruitment of desensitization-resistant ionotropic purinergic receptor subtypes (P2X-Rs): 1) Antagonists of the P2X2/3 and P2X7-Rs truncated the sustained VP/OT release induced by ATP+PE but did not alter the transient response to ATP alone. 2) The P2X2/3 and P2X7-R antagonists did not alter either ATP or ATP+PE-induced i
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7

Burgard, Edward C., Wende Niforatos, Tim van Biesen, et al. "P2X Receptor–Mediated Ionic Currents in Dorsal Root Ganglion Neurons." Journal of Neurophysiology 82, no. 3 (1999): 1590–98. http://dx.doi.org/10.1152/jn.1999.82.3.1590.

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Анотація:
Nociceptive neurons in the dorsal root ganglia (DRG) are activated by extracellular ATP, implicating P2X receptors as potential mediators of painful stimuli. However, the P2X receptor subtype(s) underlying this activity remain in question. Using electrophysiological techniques, the effects of P2X receptor agonists and antagonists were examined on acutely dissociated adult rat lumbar DRG neurons. Putative P2X-expressing nociceptors were identified by labeling neurons with the lectin IB4. These neurons could be grouped into three categories based on response kinetics to extracellularly applied A
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8

Kiyatkin, Michael E., Bin Feng, Erica S. Schwartz, and G. F. Gebhart. "Combined genetic and pharmacological inhibition of TRPV1 and P2X3 attenuates colorectal hypersensitivity and afferent sensitization." American Journal of Physiology-Gastrointestinal and Liver Physiology 305, no. 9 (2013): G638—G648. http://dx.doi.org/10.1152/ajpgi.00180.2013.

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Анотація:
The ligand-gated channels transient receptor potential vanilloid 1 (TRPV1) and P2X3 have been reported to facilitate colorectal afferent neuron sensitization, thus contributing to organ hypersensitivity and pain. In the present study, we hypothesized that TRPV1 and P2X3 cooperate to modulate colorectal nociception and afferent sensitivity. To test this hypothesis, we employed TRPV1-P2X3 double knockout (TPDKO) mice and channel-selective pharmacological antagonists and evaluated combined channel contributions to behavioral responses to colorectal distension (CRD) and afferent fiber responses to
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9

Niane, Lalah M., David F. Donnelly, Vincent Joseph, and Aida Bairam. "Ventilatory and carotid body chemoreceptor responses to purinergic P2X receptor antagonists in newborn rats." Journal of Applied Physiology 110, no. 1 (2011): 83–94. http://dx.doi.org/10.1152/japplphysiol.00871.2010.

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Анотація:
Adenosine triphosphate, acting through purinergic P2X receptors, has been shown to stimulate ventilation and increase carotid body chemoreceptor activity in adult rats. However, its role during postnatal development of the ventilatory response to hypoxia is yet unknown. Using whole body plethysmography, we measured ventilation in normoxia and in moderate hypoxia (12% fraction of inspired O2, 20 min) before and after intraperitoneal injection of suramin (P2X2 and P2X3 receptor antagonist, 40 mg/kg) in 4-, 7-, 12-, and 21-day-old rats. Suramin reduced baseline breathing (∼20%) and the response t
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10

LIGHT, ALAN R., YING WU, RONALD W. HUGHEN, and PETER B. GUTHRIE. "Purinergic receptors activating rapid intracellular Ca2+ increases in microglia." Neuron Glia Biology 2, no. 2 (2005): 125–38. http://dx.doi.org/10.1017/s1740925x05000323.

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Анотація:
We provide both molecular and pharmacological evidence that the metabotropic, purinergic, P2Y6, P2Y12 and P2Y13 receptors and the ionotropic P2X4 receptor contribute strongly to the rapid calcium response caused by ATP and its analogues in mouse microglia. Real-time PCR demonstrates that the most prevalent P2 receptor in microglia is P2Y6 followed, in order, by P2X4, P2Y12, and P2X7 = P2Y13. Only very small quantities of mRNA for P2Y1, P2Y2, P2Y4, P2Y14, P2X3 and P2X5 were found. Dose-response curves of the rapid calcium response gave a potency order of: 2MeSADP>ADP=UDP=IDP=UTP>ATP>Bz
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Дисертації з теми "P2X3 antagonist"

1

Helms, Nick. "Wechselwirkungen von Agonisten und kompetitiven Antagonisten mit der Ligandenbindungsstelle des schnell desensitisierenden P2X3-Rezeptors." Doctoral thesis, Universitätsbibliothek Leipzig, 2016. http://nbn-resolving.de/urn:nbn:de:bsz:15-qucosa-197364.

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Анотація:
Purinerge P2X3-Rezeptoren spielen eine bedeutende Rolle in der Vermittlung chronischer Schmerzen, welche ein führendes Problem des Gesundheitswesens mit vielen sozioökonomischen Konsequenzen darstellen. Die Tatsache, dass P2X3-Rezeptoren fast ausschließlich von nozizeptiven Neuronen exprimiert werden, macht sie trotz ihres besonderen Desensitisierungsverhaltens zu vielversprechenden Angriffspunkten zukünftiger Schmerztherapien, beispielsweise mithilfe kompetitiver Antagonisten an diesen Rezeptoren. Zur Analyse der Wechselwirkungen zwischen Agonist und kompetitivem Antagonist wird meist der Sch
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2

Farmer, Louise Katie. "The molecular basis of antagonism at cardiovascular P2X1 and P2X4 receptors." Thesis, University of Leicester, 2014. http://hdl.handle.net/2381/40322.

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Анотація:
Structural information for the zebrafish P2X4 receptor in both an agonist bound and unbound resting state provided a major advance in understanding agonist action and has given insight into movement that occurs in the receptor upon ATP binding. Despite agonist action now being well characterised, the molecular basis of antagonism is poorly understood. In this thesis the mechanism of antagonist action at the hP2X1 receptor has been investigated through determining properties of chimeras and mutant receptors based on differences between antagonist sensitive and insensitive P2X receptors. The ant
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3

Jackson, Alexander Rodney. "Pharmacological Evaluation of Cyanoguanidine P2X7 Receptor Antagonists." Thesis, The University of Sydney, 2017. http://hdl.handle.net/2123/17186.

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Анотація:
ABSTRACT BACKGROUND AND AIMS: The P2X7 receptor (P2X7R) is an ATP-gated, non-selective cation channel highly expressed on monocytes, macrophages and microglia. Prolonged activation of the P2X7R by ATP leads to cytolytic pore formation and the release of inflammatory mediators including interleukin-1β and prostaglandin E2. Accumulating evidence suggests a role for the P2X7R in neuroinflammation and thus P2X7R antagonists might be useful in diseases including chronic pain, depression and Alzheimer’s disease. Both negative allosteric modulators of the P2X7R, such as the adamantyl benzamides, and
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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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Анотація:
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

Rashed, Mahmoud [Verfasser]. "Syntheses and structure-activity relationships of novel P2X3 receptor antagonists / Mahmoud Rashed." Bonn : Universitäts- und Landesbibliothek Bonn, 2018. http://d-nb.info/1160594392/34.

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6

Palaskali, Sascha [Verfasser]. "Charakterisierung von Cyclothiazid als Antagonist von humanen P2X7-Rezeptoren / Sascha Palaskali." Ulm : Universität Ulm. Medizinische Fakultät, 2011. http://d-nb.info/1018024883/34.

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7

Fischer, Wolfgang, Heike Franke, Ute Krügel, et al. "Critical evaluation of P2X7 receptor antagonists in selected seizure models." Universitätsbibliothek Leipzig, 2016. http://nbn-resolving.de/urn:nbn:de:bsz:15-qucosa-206115.

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Анотація:
The ATP-gated P2X7 receptor (P2X7R) is a non-selective cation channel which senses high extracellular ATP concentrations and has been suggested as a target for the treatment of neuroinflammation and neurodegenerative diseases. The use of P2X7R antagonists may therefore be a viable approach for treating CNS pathologies, including epileptic disorders. Recent studies showed anticonvulsant potential of P2X7R antagonists in certain animal models. To extend this work, we tested three CNS-permeable P2X7R blocker (Brilliant Blue G, AFC-5128, JNJ-47965567) and a natural compound derivative (tanshinone
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8

Huo, Hong. "The molecular basis of antagonism by PPADS at the human P2X1 receptor." Thesis, University of Leicester, 2018. http://hdl.handle.net/2381/42934.

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Анотація:
P2X receptors (P2XRs) activated by ATP are widely expressed throughout the human body and mediate various physiological and pathophysiological roles. Crystal structures have provided a major advance in understanding agonist and subtype selective antagonist actions. However, the molecular basis of antagonism of general antagonists is poorly understood. PPADS is an effective antagonist at most mammalian P2XRs. Previous studies suggested lysine residue 249 (K249) (numbering for P2X1R) was involved in PPADS action. The aim of this study was to determine the PPADS binding site in a molecular model
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9

Ahmad, Izzuddin. "Identification and structure activity relationship of small molecule antagonists of the human P2X4 receptor." Thesis, University of East Anglia, 2018. https://ueaeprints.uea.ac.uk/68205/.

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Анотація:
P2X4 is a purinergic receptor distributed all over the body with various roles. Among them, it was reportedly overexpressed in several neuronal and immune cell types following peripheral nerve injury and its activation leads to neuropathic pain. Several compounds were found to block P2X4 but none has gone into a clinical stage, probably due to insufficient information about the compound itself and P2X4 in general. One of such compounds, 5-(3-Bromophenyl)-1,3-dihydro-2H-Benzofuro[3,2-e]-1,4-diazepin-2-one (5-BDBD) is known to be widely used in P2X4-related studies despite its limited informatio
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10

Bezerra, Rômulo José Soares. "Triagem de extratos vegetais e fúngicos de diferentes biomas para identificação de antagonistas do receptor P2X7." reponame:Repositório Institucional da FIOCRUZ, 2012. https://www.arca.fiocruz.br/handle/icict/13174.

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Анотація:
Made available in DSpace on 2016-03-15T14:19:06Z (GMT). No. of bitstreams: 2 romulo_bezerra_ioc_dout_2012.pdf: 7162611 bytes, checksum: 3d02f06c712f13335b047fc33620dd3c (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2016-02-23<br>O P2X7 é um receptor purinérgico que está envolvido em importantes funções fisiológicas e metabólicas, mas também tem participação em diversas patologias, principalmente aquelas de caráter inflamatório. Apesar de sua relevância, ainda não se têm disponíveis antagonistas específicos que possam ser utilizados na
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Частини книг з теми "P2X3 antagonist"

1

Gelin, Christine F., Anindya Bhattacharya, and Michael A. Letavic. "P2X7 receptor antagonists for the treatment of systemic inflammatory disorders." In Progress in Medicinal Chemistry. Elsevier, 2020. http://dx.doi.org/10.1016/bs.pmch.2019.11.002.

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2

Souza, Roberta Figueiroa, Mariá Munhoz Evangelinellis, Cristina Eusébio Mendes, Marta Righetti, Múcio Cevulla Silva Lourenço, and Patricia Castelucci. "P2X7 RECEPTOR ANTAGONIST RECOVERS ILEUM MYENTERIC NEURONS AFTER EXPERIMENTAL ULCERATIVE COLITIS." In Novas tecnologias e as competências técnico-científicas nas ciências biológicas. Atena Editora, 2022. http://dx.doi.org/10.22533/at.ed.9682223084.

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3

Chrovian, Christa C., Jason C. Rech, Anindya Bhattacharya, and Michael A. Letavic. "P2X7 Antagonists as Potential Therapeutic Agents for the Treatment of CNS Disorders." In Progress in Medicinal Chemistry. Elsevier, 2014. http://dx.doi.org/10.1016/b978-0-444-63380-4.00002-0.

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Тези доповідей конференцій з теми "P2X3 antagonist"

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Smith, Jaclyn, and Rachel Giles. "Novel P2X3 antagonist can SOOTHE chronic cough." In ATS 2022 International Conference, edited by Richard Dekhuijzen. Medicom Medical Publishers, 2022. http://dx.doi.org/10.55788/7e412546.

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2

Friedrich, Christian, Klaus Francke, Surinder S. Birring, et al. "Safety and efficacy of P2X3 antagonist BAY 1902607 in refractory chronic cough." In ERS International Congress 2020 abstracts. European Respiratory Society, 2020. http://dx.doi.org/10.1183/13993003.congress-2020.4566.

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3

Martinez, F. J., A. Afzal, M. M. Kitt, et al. "The Treatment of Chronic Cough in Idiopathic Pulmonary Fibrosis Patients with Gefapixant, a P2x3 Receptor Antagonist." In American Thoracic Society 2019 International Conference, May 17-22, 2019 - Dallas, TX. American Thoracic Society, 2019. http://dx.doi.org/10.1164/ajrccm-conference.2019.199.1_meetingabstracts.a2638.

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Garceau, D., N. Chauret, and L. Harvey. "BLU-5937 a Highly Selective P2X3 Homotrimeric Receptor Antagonist with Improved Taste Safety Profile in Healthy Subjects." In American Thoracic Society 2019 International Conference, May 17-22, 2019 - Dallas, TX. American Thoracic Society, 2019. http://dx.doi.org/10.1164/ajrccm-conference.2019.199.1_meetingabstracts.a7396.

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Morice, A. H., J. Smith, L. McGarvey, et al. "Safety and Efficacy of BAY 1817080, a P2X3 Receptor Antagonist, in Patients with Refractory Chronic Cough (RCC)." In American Thoracic Society 2020 International Conference, May 15-20, 2020 - Philadelphia, PA. American Thoracic Society, 2020. http://dx.doi.org/10.1164/ajrccm-conference.2020.201.1_meetingabstracts.a7648.

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Ishihara, Hiroyuki, Hideaki Hida, Mitsuaki Machida, Yoshiyuki Tsuda, and Sayaka Miyazaki. "Design of phase 2b randomised controlled trial of S-600918, P2X3 receptor antagonist for refractory chronic cough." In ERS International Congress 2020 abstracts. European Respiratory Society, 2020. http://dx.doi.org/10.1183/13993003.congress-2020.2271.

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Smith, Jaclyn, Lorcan P. Mcgarvey, Alyn H. Morice, et al. "The effect of baseline factors on treatment response with MK-7264, a P2X3 antagonist, in refractory chronic cough." In ERS International Congress 2018 abstracts. European Respiratory Society, 2018. http://dx.doi.org/10.1183/13993003.congress-2018.pa811.

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McGarvey, Lorcan, Jaclyn Smith, Surinder Birring, et al. "Characterization of chronic cough patients participating in a phase 2b clinical trial of gefapixant, a P2X3 receptor antagonist." In ERS International Congress 2019 abstracts. European Respiratory Society, 2019. http://dx.doi.org/10.1183/13993003.congress-2019.pa612.

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Birring, Surinder S., Lorcan Mcgarvey, Jaclyn Smith, et al. "Baseline patient burden in chronic cough from a Phase 2b clinical trial of gefapixant, a P2X3 receptor antagonist." In ERS International Congress 2019 abstracts. European Respiratory Society, 2019. http://dx.doi.org/10.1183/13993003.congress-2019.pa613.

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Bonuccelli, C. M., J. Smith, S. S. Birring, et al. "Design of SOOTHE, a Phase 2b Dose Finding Study with BLU-5937, a Selective P2X3 Antagonist, in Refractory Chronic Cough." In American Thoracic Society 2021 International Conference, May 14-19, 2021 - San Diego, CA. American Thoracic Society, 2021. http://dx.doi.org/10.1164/ajrccm-conference.2021.203.1_meetingabstracts.a2356.

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