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https://www.readbyqxmd.com/read/28944993/evaluation-of-prolonged-exposure-to-varenicline-in-adult-rats-hematological-biochemical-and-anatomopathological-studies
#1
Julia Zaccarelli-Magalhães, Natalia Moreira, Thaisa Meira Sandini, Gabriel Ramos de Abreu, Angélica Maria Sánchez-Sarmiento, Esther Lopes Ricci, André Rinaldi Fukushima, Helenice de Souza Spinosa
Varenicline is a synthetic chemical substance produced from the alkaloid cytisine, used for smoking treatment, which acts as a partial agonist for α4β2 and α3β4 nicotinic cholinergic receptors and as a total agonist for α7 receptor. While there are studies regarding varenicline's non-smoking-related effects, as in treatment for drug dependence, there are no studies in the literature evaluating the long-term toxicity of varenicline through a physiological approach. Thus, the aim of this study was to evaluate possible toxicity through hematological, biochemical and anatomopathological parameters of prolonged exposure (30 days) to varenicline in rats...
September 25, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28944927/%C3%AE-7-nicotinic-acetylcholine-receptor-agonist-attenuates-the-cerebral-injury-in-a-rat-model-of-cardiopulmonary-bypass-by-activating-the-akt-gsk3%C3%AE-pathway
#2
Yingjie Sun, Dandan Song, Mei Wang, Keyan Chen, Tiezheng Zhang
α7 nicotinic acetylcholine receptor (α7nAchR) agonist treatment may provide a promising therapeutic effect for cerebral injuries. However, it is unclear whether the activation of α7nAchR agonist may reduce cerebral injuries induced by cardiopulmonary bypass (CPB). A total of 96 male Sprague‑Dawley rats were randomly divided into four groups (n=24/group): i) Sham operation group; ii) CPB group; iii) CPB + α7nAchR agonist group; and iv) CPB + α7nAchR agonist + α7nAchR antagonist group. Following treatment, 24 rats from each group were sacrificed and the serum and hippocampal tissues were collected...
September 25, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944835/xanomeline-derivative-euk1001-attenuates-alzheimer-s-disease-pathology-in-a-triple-transgenic-mouse-model
#3
Ziyan Li, Kaili Jia, Yale Duan, Dong Wang, Zongli Zhou, Suzhen Dong
Agonists of M1 muscarinic acetylcholine receptors are promising therapeutic agents for the treatment of Alzheimer's disease (AD). An example of one of these agents is xanomeline, which has been a leading candidate, however induces various unwanted adverse effects. 3‑[3‑(3‑florophenyl‑2‑propyn‑1‑ylthio)‑1,2,5‑thiadiazol-4-yl]-1,2,5,6-tetrahydro‑1‑methylpyridine oxalate (EUK1001), a fluorinated derivative of xanomeline, has been demonstrated to attenuate AD‑like neurodegenerative pathology in presenilin‑deficient mice, which has no β‑amyloid (Aβ) pathology...
September 18, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944831/vitamin-d-alleviates-lipopolysaccharide%C3%A2-induced-acute-lung-injury-via-regulation-of-the-renin%C3%A2-angiotensin-system
#4
Jun Xu, Jialai Yang, Jian Chen, Qingli Luo, Qiu Zhang, Hong Zhang
Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS) are the clinical manifestations of severe lung damage and respiratory failure. ALI and ARDS result are associated with high mortality in patients. At present, no effective treatments for ALI and ARDS exist. It is established that vitamin D exhibits anti‑inflammatory effects, however, the specific effect of vitamin D on ALI remains largely unknown. The aim of the present study was to investigate whether, and by which mechanism, vitamin D alleviates lipopolysaccharide (LPS)‑induced ALI...
September 20, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944773/the-effect-of-treatment-with-guanfacine-an-alpha2-adrenergic-agonist-on-dopaminergic-tone-in-tobacco-smokers-an-11-c-flb457-pet-study
#5
Christine M Sandiego, David Matuskey, Meaghan Lavery, Erin McGovern, Yiyun Huang, Nabeel Nabulsi, Jim Ropchan, Marina R Picciotto, Evan D Morris, Sherry A McKee, Kelly P Cosgrove
Guanfacine, a noradrenergic alpha2a agonist, reduced tobacco smoking in a 4-week trial and in animal models has been shown to reduce cortical dopamine release, which is critically involved in the reinforcing effect of tobacco smoking. We measured amphetamine-induced extrastriatal dopamine release before and after treatment with guanfacine with [(11)C]FLB457, a dopamine D2/D3 receptor radiotracer, and positron emission tomography (PET). Sixteen tobacco smokers had one set of [(11)C]FLB457 PET scans on the same day, one before and one at 2...
September 25, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28944554/limited-potential-of-cebranopadol-to-produce-opioid-type-physical-dependence-in-rodents
#6
Thomas M Tzschentke, Babette Y Kögel, Stefanie Frosch, Klaus Linz
Cebranopadol is a novel potent analgesic agonist at the nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors. As NOP receptor activation has been shown to reduce side effects related to the activation of μ-opioid peptide (MOP) receptors, the present study evaluated opioid-type physical dependence produced by cebranopadol in mice and rats. In a naloxone-precipitated withdrawal assay in mice, a regimen of seven escalating doses of cebranopadol over 2 days produced only very limited physical dependence as evidenced by very little withdrawal symptoms (jumping) even at cebranopadol doses clearly exceeding the analgesic dose range...
September 25, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28944482/molecular-mechanism-for-muscarinic-m1-receptor-mediated-endocytosis-of-twik-related-acid-sensitive-k-1-channels-in-rat-adrenal-medullary-cells
#7
Hidetada Matsuoka, Masumi Inoue
Activation of muscarinic receptor (mAChR) in rat adrenal medullary (AM) cells induces depolarization through the inhibition of TWIK-related acid-sensitive K(+) (TASK)1 channels. Here, pharmacological and immunological approaches were used to elucidate the molecular mechanism for this mAChR-mediated inhibition. TASK1-like immunoreactive (IR) material was mainly located at the cell periphery in dissociated rat AM cells, and its majority was internalized in response to muscarine. The muscarine-induced inward current and translocation of TASK1 were suppressed by dynasore, a dynamin inhibitor...
September 25, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28944428/effect-of-grp119-receptor-agonist-compound-mbx-2982-on-activity-of-human-glucokinase
#8
A A Spasov, V A Kosolapov, D A Babkov, O Yu Maika
Validation of the method for studies of glucokinase activators by the spectrophotometric method in an in vitro test system is carried out. The advantage of NAD coenzyme vs. thio-NAD is proven. Manifest activation of glucokinase by MBX-2982 compound (GPR119 agonist) in a wide range of concentrations is demonstrated experimentally.
September 25, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28943916/blockade-of-sonic-hedgehog-signaling-decreases-viability-and-induces-apoptosis-in-retinoblastoma-cells-the-key-role-of-the-pi3k-akt-pathway
#9
Zhidu Song, Yuanyuan Du, Ying Tao
Retinoblastoma (RB) is the most common type of malignant intraocular cancer in teenagers. One of the proteins abnormally expressed during oncogenesis of RB is sonic hedgehog (SHH), which possesses the capability to selectively activate transcription factors of different genes. However, the detailed function of SHH in RB remains unknown. Thus, the present study sought to investigate the role of SHH in the development of RB. The human RB WERI-Rb-1 cell line was used as an in vitro model for the knockdown of SHH by a specific short hairpin RNA (shRNA)...
October 2017: Oncology Letters
https://www.readbyqxmd.com/read/28943448/molecular-integration-of-incretin-and-glucocorticoid-action-reverses-immunometabolic-dysfunction-and-obesity
#10
Carmelo Quarta, Christoffer Clemmensen, Zhimeng Zhu, Bin Yang, Sini S Joseph, Dominik Lutter, Chun-Xia Yi, Elisabeth Graf, Cristina García-Cáceres, Beata Legutko, Katrin Fischer, Robert Brommage, Philippe Zizzari, Bernardo S Franklin, Martin Krueger, Marco Koch, Sabine Vettorazzi, Pengyun Li, Susanna M Hofmann, Mostafa Bakhti, Aimée Bastidas-Ponce, Heiko Lickert, Tim M Strom, Valerie Gailus-Durner, Ingo Bechmann, Diego Perez-Tilve, Jan Tuckermann, Martin Hrabě de Angelis, Darleen Sandoval, Daniela Cota, Eicke Latz, Randy J Seeley, Timo D Müller, Richard D DiMarchi, Brian Finan, Matthias H Tschöp
Chronic inflammation has been proposed to contribute to the pathogenesis of diet-induced obesity. However, scarce therapeutic options are available to treat obesity and the associated immunometabolic complications. Glucocorticoids are routinely employed for the management of inflammatory diseases, but their pleiotropic nature leads to detrimental metabolic side effects. We developed a glucagon-like peptide-1 (GLP-1)-dexamethasone co-agonist in which GLP-1 selectively delivers dexamethasone to GLP-1 receptor-expressing cells...
September 19, 2017: Cell Metabolism
https://www.readbyqxmd.com/read/28943320/purinergic-and-adenosine-receptors-contribute-to-hypoxic-hyperventilation-in-zebrafish-danio-rerio
#11
Alisha J Coe, Alexina J Picard, Michael G Jonz
The chemoreceptors involved in oxygen sensing in teleost fish are neuroepithelial cells (NECs) in the gills, and are analogous to glomus cells in the mammalian carotid body. Purinergic signalling mechanisms involving the neurotransmitters, ATP and adenosine, have been identified in mediating hypoxic signalling in the carotid body, but these pathways are not well understood in the fish gill. The present study used a behavioural assay to screen for the effects of drugs, that target purinergic and adenosine receptors, on the hyperventilatory response to hypoxia in larval zebrafish (Danio rerio) in order to determine if the receptors on which these drugs act may be involved in hypoxic signalling...
September 21, 2017: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
https://www.readbyqxmd.com/read/28943268/regulated-efflux-of-photoreceptor-outer-segment-derived-cholesterol-by-human-rpe-cells
#12
Federica Storti, Gabriele Raphael, Vera Griesser, Katrin Klee, Faye Drawnel, Carolin Willburger, Rebecca Scholz, Thomas Langmann, Arnold von Eckardstein, Jürgen Fingerle, Christian Grimm, Cyrille Maugeais
Genetic studies have linked age-related macular degeneration (AMD) to genes involved in high-density lipoprotein (HDL) metabolism, including ATP-binding cassette transporter A1 (ABCA1). The retinal pigment epithelium (RPE) handles large amounts of lipids, among others cholesterol, partially derived from internalized photoreceptor outer segments (OS) and lipids physiologically accumulate in the aging eye. To analyze the potential function of ABCA1 in the eye, we measured cholesterol efflux, the first step of HDL generation, in RPE cells...
September 21, 2017: Experimental Eye Research
https://www.readbyqxmd.com/read/28943106/at2-receptor-agonist-compound-21-a-silver-lining-for-diabetic-nephropathy
#13
REVIEW
Anuradha Pandey, Anil Bhanudas Gaikwad
The currently available therapies for diabetic nephropathy, one of the leading causes of renal failure globally are based on inhibition of renin angiotensin system. However, recently, the focus has shifted towards activation of its protective arm rather than the inhibition of deteriorative axis, using specific agonists. Compound 21 (C21), a novel non-peptide Angiotensin II type 2 receptor (AT2) agonist, recently granted orphan drug status for the treatment of a rare disease, idiopathic pulmonary fibrosis has also shown a potent anti-inflammatory, anti-fibrotic, antioxidant and anti-apoptotic potential in various diseases including heart failure, myocardial infarction, chronic inflammatory diseases, and neurological diseases such as ischemic stroke...
September 21, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28943105/a549-cells-as-a-model-to-study-endogenous-lpa1-receptor-signaling-and-regulation
#14
Gabriel Carmona-Rosas, Marco A Alfonzo-Méndez, David A Hernández-Espinosa, M Teresa Romero-Ávila, J Adolfo García-Sáinz
Lysophosphatidic acid (LPA) modulates the function of many organs, including the lung. A549 is a lung carcinoma-derived cell line, frequently used as a model for type II pneumocytes. Here we show that these cells expressed messenger RNA coding for LPA1-3 receptors with the following order of abundance: LPA1 > LPA2 > LPA3 and that LPA was able to increase intracellular calcium, extracellular signal-regulated kinases 1/2 phosphorylation, and cell contraction. These effects were blocked by Ki16425, an antagonist selective for LPA1 and LPA3 receptors, and by the LPA1-selective antagonist, AM095...
September 21, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28942992/a-new-drosophila-octopamine-receptor-responds-to-serotonin
#15
Yi-Xiang Qi, Gang Xu, Gui-Xiang Gu, Fen Mao, Gong-Yin Ye, Weiwei Liu, Jia Huang
As the counterparts of the vertebrate adrenergic transmitters, octopamine and tyramine are important physiological regulators in invertebrates. They control and modulate many physiological and behavioral functions in insects. In this study, we reported the pharmacological properties of a new α2-adrenergic-like octopamine receptor (CG18208) from Drosophila melanogaster, named DmOctα2R. This new receptor gene encodes two transcripts by alternative splicing. The long isoform DmOctα2R-L differs from the short isoform DmOctα2R-S by the presence of an additional 29 amino acids within the third intracellular loop...
September 21, 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28942790/glucagon-like-peptide-1-receptor-agonists-a-class-update-for-treating-type-2-diabetes
#16
REVIEW
Julie A Lovshin
Current management options for treating type 2 diabetes are diverse. Many different classes of antidiabetes therapies are used in clinic, and several new candidates are in late-phase clinical trial. This therapeutic abundance is a windfall for patients because it facilitates individualized patient care. Evidence-based positioning of these agents is challenging, however, requiring comprehensive and balanced familiarity with each drug class. In this review, I provide a clinical update of glucagon-like peptide-1 receptor agonists (GLP-1RAs), a class of incretin-based, injectable antidiabetes therapies which improve fasting and postprandial blood glucose control through glucose-dependent pancreatic islet cell hormone secretion without significant risks for hypoglycemia...
October 2017: Canadian Journal of Diabetes
https://www.readbyqxmd.com/read/28942644/an-endocannabinoid-uptake-inhibitor-from-black-pepper-exerts-pronounced-anti-inflammatory-effects-in-mice
#17
Inés Reynoso Moreno, Israel Najar-Guerrero, Noe Escareno, Mario Eduardo Flores, Jürg Gertsch, Juan Manuel Viveros-Paredes
Guineensine is a dietary N-isobutylamide widely present in black and long pepper (Piper nigrum and P. longum) previously shown to inhibit cellular endocannabinoid uptake. Given the role of endocannabinoids in inflammation and pain reduction, here we evaluated guineensine in mouse models of acute and inflammatory pain and endotoxemia. Significant dose-dependent anti-inflammatory effects (95.6 ± 3.1 % inhibition of inflammatory pain at 2.5 mg/kg i.p. and 50.0 ± 15.9 % inhibition of edema formation at 5 mg/kg i...
September 24, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28942578/intranasal-sumatriptan-for-acute-migraine-attacks-a-systematic-review-and-meta-analysis
#18
Amr Menshawy, Hussien Ahmed, Ammar Ismail, Abdelrahman Ibrahim Abushouk, Esraa Ghanem, Ravikishore Pallanti, Ahmed Negida
We performed this systematic review and meta-analysis to evaluate the tolerability and efficacy of intranasal sumatriptan, a selective serotonin agonist, compared to placebo or other migraine therapeutics for the treatment of acute migraine attacks. We searched PubMed, SCOPUS, Embase, and Cochrane CENTRAL for relevant randomized controlled trials (RCTs). Data were extracted from eligible studies and pooled as risk ratios (RR), using RevMan software. We performed subgroup and meta-regression analyses for different doses and treatment endpoints...
September 23, 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28942287/the-costs-of-crime-associated-with-stimulant-use-in-a-canadian-setting
#19
Benjamin Enns, Emanuel Krebs, Kora DeBeck, Kanna Hayashi, M-J Milloy, Lindsey Richardson, Evan Wood, Bohdan Nosyk
BACKGROUND: Costs attributable to criminal activity are a major component of the economic burden of substance use disorders, yet there is a paucity of empirical evidence on this topic. Our aim was to estimate the costs of crime associated with different forms and intensities of stimulant use. METHODS: Retrospective cohort study, including individuals from three prospective cohorts in Vancouver, Canada, measured biannually (2011-2015), reporting stimulant use at baseline assessment...
September 14, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28941781/glucocorticoids-and-toll-like-receptor-2-cooperatively-induce-acute-phase-serum-amyloid-a
#20
Qi Su, Günther Weindl
Serum amyloid A (SAA) is a highly conserved acute-phase protein and extrahepatic produced SAA1/2 contributes to cutaneous inflammation. Prolonged systemic or topical treatment with glucocorticoids can provoke skin diseases such as steroid-induced acne. Glucocorticoids increase Toll-like receptor 2 (TLR2) expression, however, an inflammatory mediator linked to this side effect remains elusive. We report that TLR2 agonists in combination with dexamethasone substantially increase SAA expression and production in human keratinocytes and epithelial cells...
September 20, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
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