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Bradykinin receptor

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https://www.readbyqxmd.com/read/28421141/excess-of-aminopeptidase-a-in-the-brain-elevates-blood-pressure-via-the-angiotensin-ii-type-1-and-bradykinin-b2-receptors-without-dipsogenic-effect
#1
Takuto Nakamura, Masanobu Yamazato, Akio Ishida, Yusuke Ohya
Aminopeptidase A (APA) cleaves angiotensin (Ang) II, kallidin, and other related peptides. In the brain, it activates the renin angiotensin system and causes hypertension. Limited data are available on the dipsogenic effect of APA and pressor effect of degraded peptides of APA such as bradykinin. Wistar-Kyoto rats received intracerebroventricular (icv) APA in a conscious, unrestrained state after pretreatment with (i) vehicle, (ii) 80 μg of telmisartan, an Ang II type-1 (AT1) receptor blocker, (iii) 800 nmol of amastatin, an aminopeptidase inhibitor, and (iv) 1 nmol of HOE-140, a bradykinin B2 receptor blocker...
2017: International Journal of Hypertension
https://www.readbyqxmd.com/read/28398146/protective-action-of-b1r-antagonist-against-cerebral-ischemia-reperfusion-injury-through-suppressing-mir-200c-expression-of-microglia-derived-microvesicles
#2
Min Tang, Ping Liu, Xia Li, Jian-Wen Wang, Xiong-Chao Zhu, Fang-Ping He
BACKGROUND AND OBJECTIVE: Cerebral ischemia-reperfusion (I/R) injury is a common side-effect for cerebral ischemic disease and its therapeutic regimen is limited. Kinin is pro-inflammatory peptide that is released and acts at the site of injury and inflammation such as brain and it works through bradykinin 1 receptor (B1R). The present study was to examine the effect of B1R antagonist on cerebral I/R injury and the potential mechanism. METHODS: Cerebral I/R injury was induced in mice by transient middle cerebral artery occlusion (MCAO)...
April 11, 2017: Neurological Research
https://www.readbyqxmd.com/read/28390948/relationship-of-angiotensin-i-converting-enzyme-ace-and-bradykinin-b2-receptor-bdkrb2-polymorphism-with-diabetic-nephropathy
#3
Honghong Zou, Guoqing Wu, Jinlei Lv, Gaosi Xu
PURPOSE: To determine whether ACE(2) I/D and BDKRB2(3) +9/-9 polymorphism causatively affect diabetic nephropathy progression. RESULTS: STZ-induced metabolic disorder, as well as inflammatory responses, was significantly aggravated in ACE II-B2R(4)+9bp, ACE DD-B2R+9bp, or ACE DD-B2R-9bp diabetic mice but not ACE II-B2R-9bp, indicating the genetic susceptibility of ACE DD or B2R+9bp to diabetic nephropathy. Furthermore, ACE II-B2R+9bp, ACE DD-B2R+9bp, or ACE DD-B2R-9bp rather than ACE II-B2R-9bp, worsened renal performance and enhanced pathological alterations induced by STZ...
April 5, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28374922/synovial-membrane-receptors-as-therapeutic-targets-a-review-of-receptor-localization-structure-and-function
#4
REVIEW
Stephanie A Kleine, Steven C Budsberg
Joint pathology and degeneration is a significant cause of pain. The synovial membrane plays an important role in maintenance of the joint, contributes to the pathology of many arthropathies and may be adversely affected in joint disease. Improving knowledge of the receptors present within the synovium will aid in a better understanding of joint pathology and the development of new treatments for diseases such as osteoarthritis and rheumatoid arthritis. Knowledge of the location and function of synovial membrane receptors (both in healthy and diseased synovium) may provide important targets in the treatment of various arthropathies...
April 4, 2017: Journal of Orthopaedic Research: Official Publication of the Orthopaedic Research Society
https://www.readbyqxmd.com/read/28373410/bradykinin-b2-receptor-activation-regulates-renin-in-m-1-cells-via-protein-kinase-c-and-nitric-oxide
#5
Lucienne S Lara, Camille R T Bourgeois, Samir S El-Dahr, Minolfa C Prieto
In the collecting duct (CD), the interactions of renin angiotensin system (RAS) and kallikrein-kinin system (KKS) modulate Na(+) reabsorption, volume homeostasis, and blood pressure. In this study, we used a mouse kidney cortical CD cell line (M-1 cells) to test the hypothesis that in the CD, the activation of bradykinin B2 receptor (B2R) increases renin synthesis and release. Physiological concentrations of bradykinin (BK) treatment of M-1 cells increased renin mRNA and prorenin and renin protein contents in a dose-dependent manner and increased threefold renin content in the cell culture media...
April 2017: Physiological Reports
https://www.readbyqxmd.com/read/28370444/the-icatibant-outcome-survey-experience-of-hereditary-angioedema-management-from-six-european-countries
#6
T Caballero, W Aberer, H J Longhurst, M Maurer, A Zanichelli, A Perrin, L Bouillet, I Andresen
BACKGROUND: Hereditary angioedema (HAE) due to C1 INH deficiency (C1-INH-HAE) is a rare, potentially fatal, bradykinin-mediated disease. Icatibant is a bradykinin B2 receptor antagonist originally approved in 2008 in the European Union and 2011 in the United States, as an acute therapy option for HAE attacks in adults. OBJECTIVE: To compare demographics, disease characteristics and treatment outcomes of icatibant-treated HAE attacks in patients with C1-INH-HAE enrolled in the Icatibant Outcome Survey across six European countries: Austria, France, Germany, Italy, Spain and the United Kingdom...
April 1, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/28352319/characterizing-nanoscale-changes-in-the-activity-of-vegfr-2-on-glioma-microvascular-endothelial-cell-membranes-using-atomic-force-microscopy
#7
Dexiang Zhou, Shengquan Zhan, Dong Zhou, Peng Wang, Guangzhong Chen, Kun Qin, Xiaofeng Lin
The aim of the current study was to demonstrate the distribution of VEGFR-2 on glioma microvascular endothelial cells on a nanoscale and investigate changes in VEGFR-2 activity following treatment with the VEGFR-2 inhibitor and agonist sorafenib and bradykinin, respectively. Three groups were evaluated in this study: Control glioma microvascular endothelial cells, sorafenib-treated glioma microvascular endothelial cells and bradykinin-treated glioma microvascular endothelial cells. Changes in the activity of VEGFR-2 on the glioma microvascular endothelial cell membranes following treatment with sorafenib and bradykinin were characterized by atomic force microscopy (AFM)...
February 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28344594/articular-inflammation-induced-by-an-enzymatically-inactive-lys49-phospholipase-a2-activation-of-endogenous-phospholipases-contributes-to-the-pronociceptive-effect
#8
Renata Gonçalves Dias, Sandra Coccuzzo Sampaio, Morena Brazil Sant'Anna, Fernando Queiroz Cunha, José María Gutiérrez, Bruno Lomonte, Yara Cury, Gisele Picolo
BACKGROUND: Arthritis is a set of inflammatory conditions that induce aching, stiffness, swelling, pain and may cause functional disability with severe consequences to the patient's lives. These are multi-mediated pathologies that cannot be effectively protected and/or treated. Therefore, the aim of this study was to establish a new model of acute arthritis, using a Lys49-PLA2 (Bothrops asper myotoxin II; MT-II) to induce articular inflammation. METHODS: The articular inflammation was induced by MT-II (10 μg/joint) injection into the left tibio-tarsal or femoral-tibial-patellar joints...
2017: Journal of Venomous Animals and Toxins Including Tropical Diseases
https://www.readbyqxmd.com/read/28326642/neprilysin-inhibition-in-heart-failure-mechanisms-and-substrates-beyond-modulating-natriuretic-peptides
#9
REVIEW
Emilia D'Elia, Attilio Iacovoni, Muthiah Vaduganathan, Ferdinando L Lorini, Stefano Perlini, Michele Senni
The autonomic nervous system, the renin-angiotensin-aldosterone system, and the natriuretic peptide system represent critical regulatory pathways in heart failure and as such have been the major targets of pharmacological development. The introduction and approval of angiotensin receptor neprilysin inhibitors (ARNi) have broadened the available drug treatments of patients with chronic heart failure with reduced ejection fraction. Neprilysin catalyses the degradation of a number of vasodilator peptides, including the natriuretic peptides, bradykinin, substance P, and adrenomedullin, as well as vasoconstrictor peptides, including endothelin-1 and angiotensin I and II...
March 21, 2017: European Journal of Heart Failure
https://www.readbyqxmd.com/read/28322750/supradural-inflammatory-soup-in-awake-and-freely-moving-rats-induces-facial-allodynia-that-is-blocked-by-putative-immune-modulators
#10
Julie Wieseler, Amanda Ellis, Andrew McFadden, Kendra Stone, Kimberley Brown, Sara Cady, Leandro F Bastos, David Sprunger, Niloofar Rezvani, Kirk Johnson, Kenner C Rice, Steven F Maier, Linda R Watkins
Facial allodynia is a migraine symptom that is generally considered to represent a pivotal point in migraine progression. Treatment before development of facial allodynia tends to be more successful than treatment afterwards. As such, understanding the underlying mechanisms of facial allodynia may lead to a better understanding of the mechanisms underlying migraine. Migraine facial allodynia is modeled by applying inflammatory soup (histamine, bradykinin, serotonin, prostaglandin E2) over the dura. Whether glial and/or immune activation contributes to such pain is unknown...
March 16, 2017: Brain Research
https://www.readbyqxmd.com/read/28315051/development-of-antibody-modified-chitosan-nanoparticles-for-the-targeted-delivery-of-sirna-across-the-blood-brain-barrier-as-a-strategy-for-inhibiting-hiv-replication-in-astrocytes
#11
Jijin Gu, Karam Al-Bayati, Emmanuel A Ho
RNA interference (RNAi)-mediated gene silencing offers a novel treatment and prevention strategy for human immunodeficiency virus (HIV) infection. HIV was found to infect and replicate in human brain cells and can cause neuroinfections and neurological deterioration. We designed dual-antibody-modified chitosan/small interfering RNA (siRNA) nanoparticles to deliver siRNA across the blood-brain barrier (BBB) targeting HIV-infected brain astrocytes as a strategy for inhibiting HIV replication. We hypothesized that transferrin antibody and bradykinin B2 antibody could specifically bind to the transferrin receptor (TfR) and bradykinin B2 receptor (B2R), respectively, and deliver siRNA across the BBB into astrocytes as potential targeting ligands...
March 17, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28288820/resveratrol-inhibits-bk-induced-cox-2-transcription-by-suppressing-acetylation-of-ap-1-and-nf-%C3%AE%C2%BAb-in-human-rheumatoid-arthritis-synovial-fibroblasts
#12
Chuen-Mao Yang, Yu-Wen Chen, Pei-Ling Chi, Chih-Chung Lin, Li-Der Hsiao
Bradykinin (BK) induces inflammation in rheumatoid arthritis (RA). Resveratrol is a potent activator of Sirt1 which could modulate inflammation through deacetylating histones of transcription factors. Here, we investigated the mechanisms underlying BK-induced COX-2 expression which is modulated by resveratrol/Sirt1 in human rheumatoid arthritis synovial fibroblasts (RASFs). We found that BK-induced COX-2 protein and mRNA expression associated with PGE2 synthesis, and promoter activity was mediated through B2R receptors, which were attenuated by selective B2R antagonist Hoe140 or transfection with B2R siRNA...
March 11, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28283888/kinin-receptors-sensitize-trpv4-channel-and-induce-mechanical-hyperalgesia-relevance-to-paclitaxel-induced-peripheral-neuropathy-in-mice
#13
Robson Costa, Maíra A Bicca, Marianne N Manjavachi, Gabriela C Segat, Fabiana Chaves Dias, Elizabeth S Fernandes, João B Calixto
Kinin B1 (B1R) and B2 receptors (B2R) and the transient receptor potential vanilloid 4 (TRPV4) channel are known to play a critical role in the peripheral neuropathy induced by paclitaxel (PTX) in rodents. However, the downstream pathways activated by kinin receptors as well as the sensitizers of the TRPV4 channel involved in this process remain unknown. Herein, we investigated whether kinins sensitize TRPV4 channels in order to maintain PTX-induced peripheral neuropathy in mice. The mechanical hyperalgesia induced by bradykinin (BK, a B2R agonist) or des-Arg(9)-BK (DABK, a B1R agonist) was inhibited by the selective TRPV4 antagonist HC-067047...
March 10, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28226311/effects-of-root-extracts-of-eurycoma-longifolia-jack-on-corpus-cavernosum-of-rat
#14
Bae Huey Tee, See Ziau Hoe, Swee Hung Cheah, Sau Kuen Lam
OBJECTIVE: This study was conducted to investigate the mechanisms of action of Eurycoma longifolia in rat corpus cavernosum. MATERIALS AND METHODS: Tincture of the roots was concentrated to dryness by evaporating the ethanol in vacuo. This ethanolic extract was partitioned into five fractions sequentially with hexane, dichloromethane, ethyl acetate, butanol and water. The corpus cavernosum relaxant activity of each fraction was investigated. Dichloromethanic (DCM) fraction which showed the highest potency in relaxing phenylephrine-precontracted corpora cavernosa was purified by column chromatography...
February 22, 2017: Medical Principles and Practice: International Journal of the Kuwait University, Health Science Centre
https://www.readbyqxmd.com/read/28196712/ipomoea-pes-caprae-l-r-br-convolvulaceae-as-a-topical-herbal-medicine-to-relieve-pain-and-inflammation-promising-tool-against-effects-due-to-toxin-skin-contact
#15
Cristiane da Silva Barth, Hugo Guilherme Tolentino de Souza, Lilian W Rocha, Gislaine Francieli da Silva, Mariana Ferreira Dos Anjos, Veronica D'Avila Pastor, Tania Mari Belle Bresolin, Angelica Garcia Couto, José Roberto Santin, Nara Lins Meira Quintão
ETHNOPHARMACOLOGICAL RELEVANCE: Ipomoea pes-caprae is known as bayhops, beach morning glory or goat's foot, and in Brazil as salsa-de-praia. Its leaves are used in worldwide folk medicine for the relief of jellyfish-stings symptoms. The literature only reports the anti-inflammatory and neutralizing effects of a nonpolar plant derived, without validating the popular use or exploring the mechanism of action. AIM OF THE STUDY: This study aimed to evaluate and validate the topical effects of a semisolid containing hydroethanolic extract obtained from the aerial parts of I...
February 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28192151/angiotensin-1-7-dependent-vasorelaxation-of-the-renal-artery-exhibits-unique-angiotensin-and-bradykinin-receptor-selectivity
#16
Mariam H M Yousif, Ibrahim F Benter, Debra I Diz, Mark C Chappell
Angiotensin-(1-7) [Ang-(1-7)] exhibits blood pressure lowering actions, inhibits cell growth, and reduces tissue inflammation and fibrosis which may functionally antagonize an activated Ang II-AT1 receptor axis. Since the vascular actions of Ang-(1-7) and the associated receptor/signaling pathways vary in different vascular beds, the current study established the vasorelaxant properties of the heptapeptide in the renal artery of male Wistar male rats. Ang-(1-7) produced an endothelium-dependent vasodilator relaxation of isolated renal artery segments pre-contracted by a sub-maximal concentration of phenylephrine (PE) (3×10(-7)M)...
February 10, 2017: Peptides
https://www.readbyqxmd.com/read/28163105/nerve-growth-factor-derivative-ngf61-100-promotes-outgrowth-of-primary-sensory-neurons-with-reduced-signs-of-nociceptive-sensitization
#17
C Severini, P Petrocchi Passeri, M T Ciotti, F Florenzano, C Petrella, F Malerba, B Bruni, M D'Onofrio, I Arisi, R Brandi, R Possenti, P Calissano, A Cattaneo
Nerve Growth Factor (NGF) is being considered as a therapeutic candidate for Alzheimer's disease. However, the development of an NGF-based therapy is limited by its potent pain activity. We have developed a "painless" derivative form of human NGF (NGF61/100), characterized by identical neurotrophic properties but a reduced nociceptive sensitization activity in vivo. Here we characterized the response of rat dorsal root ganglia neurons (DRG) to the NGF derivative NGF61/100, in comparison to that of control NGF (NGF61), analyzing the expression of noxious pro-nociceptive mediators...
February 2, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28133580/species-specific-pharmacology-of-maximakinin-an-amphibian-homologue-of-bradykinin-putative-prodrug-activity-at-the-human-b2-receptor-and-peptidase-resistance-in-rats
#18
Xavier Charest-Morin, Hélène Bachelard, Melissa Jean, Francois Marceau
Maximakinin (MK), an amphibian peptide possessing the C-terminal sequence of bradykinin (BK), is a BK B2 receptor (B2R) agonist eliciting prolonged signaling. We reinvestigated this 19-mer for species-specific pharmacologic profile, in vivo confirmation of resistance to inactivation by angiotensin converting enzyme (ACE), value as a module for the design of fusion proteins that bind to the B2R in mammalian species and potential activity as a histamine releaser. Competition of the binding of [(3)H]BK to recombinant human myc-B2Rs in cells that express these receptors revealed that MK possessed a tenuous fraction (<0...
2017: PeerJ
https://www.readbyqxmd.com/read/28133468/changing-the-treatment-of-heart-failure-with-reduced-ejection-fraction-clinical-use-of-sacubitril-valsartan-combination
#19
REVIEW
Edgardo Kaplinsky
Despite significant therapeutic advances, patients with chronic heart failure (HF) remain at high risk of morbidity and mortality. Sacubitril valsartan (previously known as LCZ696) is a new oral agent approved for the treatment of symptomatic chronic heart failure in adults with reduced ejection fraction. It is described as the first in class angiotensin receptor neprilysin inhibitor (ARNI) since it incorporates the neprilysin inhibitor, sacubitril and the angiotensin II receptor antagonist, valsartan. Neprilysin is an endopeptidase that breaks down several vasoactive peptides including natriuretic peptides (NPs), bradykinin, endothelin and angiotensin II (Ang-II)...
November 2016: Journal of Geriatric Cardiology: JGC
https://www.readbyqxmd.com/read/28131783/antihyperalgesic-effect-of-cb1-receptor-activation-involves-the-modulation-of-p2x3-receptor-in-the-primary-afferent-neuron
#20
Maria Cláudia Gonçalves Oliveira-Fusaro, Cristiane Isabel Silva Zanoni, Gilson Gonçalves Dos Santos, Luis Paulo Manzo, Dionéia Araldi, Ivan José Magayewski Bonet, Cláudia Herrera Tambeli, Elayne Vieira Dias, Carlos Amilcar Parada
Cannabinoid system is a potential target for pain control. Cannabinoid receptor 1 (CB1) activation play a role in the analgesic effect of cannabinoids once it is expressed in primary afferent neurons. This study investigates whether the anti-hyperalgesic effect of CB1 receptor activation involves P2X3 receptor in primary afferent neurons. Mechanical hyperalgesia was evaluated by electronic von Frey test. Cannabinoid effect was evaluated using anandamide or ACEA, a non-selective or a selective CB1 receptor agonists, respectively; AM251, a CB1 receptor antagonist, and antisense ODN for CB1 receptor...
January 25, 2017: European Journal of Pharmacology
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