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https://www.readbyqxmd.com/read/29778010/exposure-to-cannabinoid-agonist-win-55-212-2-during-early-adolescence-increases-alcohol-preference-and-anxiety-in-cd1-mice
#1
Jimena Laura Frontera, Victoria María Gonzalez Pini, Fernando Luis Messore, Alicia Brusco
The endocannabinoid (eCB) system is involved in the modulation of the reward system and participates in the reinforcing effects of different drugs of abuse, including alcohol. The most abundant receptor of the eCB system in the central nervous system is the CB1 receptor (CB1R), which is predominantly expressed in areas involved in drug addiction, such as the nucleus accumbens, the ventral tegmental area, the substantia nigra and the raphe nucleus. CB1R is expressed in early stages during development, and reaches maximum levels during early adolescence...
May 16, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29777865/a-prospective-non-interventional-registry-study-of-patients-initiating-a-course-of-drug-therapy-for-overactive-bladder-perspective-rationale-design-and-methodology
#2
Eric S Rovner, Kevin V Carlson, Anna S Deal, Kavita V Nair, Eva E Oakkar, Julie Park, Eric Gemmen, Rita M Kristy, Katherine L Gooch, Carol R Schermer
INTRODUCTION: Pharmacotherapy of overactive bladder (OAB) typically involves treatment with an antimuscarinic or mirabegron, a β3-adrenoceptor agonist, but real-world evidence on their use, including treatment access, persistence, and switching, is limited. Here, we describe the design of a prospective, multicenter, non-interventional registry of patients beginning a new course of OAB pharmacological therapy in routine clinical practice. METHODS: Adults with an OAB diagnosis for at least 3 months who either initiated a new course of mirabegron or antimuscarinic, or who switched therapy were enrolled into PERSPECTIVE (A Prospective, Non-intErventional Registry Study of Patients Initiating a Course of Drug Therapy for OveractIVE Bladder)...
May 16, 2018: Contemporary Clinical Trials
https://www.readbyqxmd.com/read/29777833/endocrine-disrupting-activities-and-immunomodulatory-effects-in-lymphoblastoid-cell-lines-of-diclofenac-4-hydroxydiclofenac-and-paracetamol
#3
Ivana Klopčič, Tijana Markovič, Irena Mlinarič-Raščan, Marija Sollner Dolenc
A critical literature review reveals that knowledge of side effects of pharmaceuticals diclofenac and paracetamol is extremely important because of their widespread use and occurrence in the environment. In order to delineate whether these compounds have endocrine activity and influence on the immune system, we assessed the potential endocrine disrupting and immunomodulatory activities of: diclofenac (DIC), its metabolite 4-hydroxydiclofenac (4-HD) and paracetamol (PAR). Herein, we report on their impact on estrogen receptor (ER), androgen receptor (AR), glucocorticoid receptor (GR) and thyroid hormone receptor (TR)...
May 16, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29777637/thymol-inhibits-oral-squamous-cell-carcinoma-growth-via-mitochondria-mediated-apoptosis
#4
Jorge J De La Chapa, Prajjal Kanti Singha, Debbie R Lee, Cara B Gonzales
BACKGROUND: Thymol is a Transient Receptor Potential Ankyrin Subtype 1 channel, (TRPA1) agonist found in thyme and oregano. Thymol has antioxidant, anti-inflammatory, and antimicrobial properties; thus thymol is added to many commercially available products including Listerine mouthwash. Thymol is also cytotoxic to HL-60 (acute promyelotic leukemia) cells in vitro. Therefore, we evaluated the effects of thymol against oral squamous cell carcinoma (OSCC) and its anticancer mechanism-of-action...
May 19, 2018: Journal of Oral Pathology & Medicine
https://www.readbyqxmd.com/read/29777633/hypertrophic-effect-of-inhaled-beta-2-agonist-with-and-without-concurrent-exercise-training-a-randomized-controlled-trial
#5
Søren Jessen, Johan Onslev, Anders Lemminger, Vibeke Backer, Jens Bangsbo, Morten Hostrup
INTRODUCTION: Due to a high prevalence of asthma and exercise-induced bronchoconstriction in elite athletes, there is a high use of beta2 -adrenoceptor agonists (beta2 -agonists) in the athletic population. While anabolic in rodents, no study has been able to detect hypertrophy in humans after chronic beta2 -agonist inhalation. METHODS: We investigated if inhaled beta2 -agonist, terbutaline, alters body composition and metabolic rate with and without concurrent exercise training in healthy young men...
May 19, 2018: Scandinavian Journal of Medicine & Science in Sports
https://www.readbyqxmd.com/read/29777582/comparative-study-of-liraglutide-and-insulin-glargine-on-glycemic-control-and-pancreatic-%C3%AE-cell-function-in-db-db-mice
#6
Yanli Li, Jia Zheng, Yunfeng Shen, Wangen Li, Meimei Liu, Jun Wang, Surong Zhu, Meihua Wu
BACKGROUND The aim of this study was to compare the effects of liraglutide, a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist, and insulin glargine, a long-acting insulin analog, on glycemic control and pancreatic β-cell function in db/db mice. MATERIAL AND METHODS Eight-week-old male db/db mice (n=40) were divided into five groups: the vehicle-treated group (VG) (n=8); the insulin glargine-treated group (GG) (dose, 450 mg/kg) (n=8), the low-dose liraglutide-treated group (LLG) (dose, 75 μg/kg) (n=8), the mid-dose liraglutide-treated group (MLG) (150 μg/kg) (n=8), and the high-dose liraglutide-treated group (HLG) (300 μg/kg) (n=8), treated with subcutaneous injection once daily, from 8-14 weeks-of-age...
May 19, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29777569/improving-metabolic-stability-with-deuterium-the-discovery-of-hwl-066-a-potent-and-long-acting-free-fatty-acid-receptor-1-agonists
#7
Chunxia Liu, Zheng Li, Wei Shi, Huilan Li, Nasi Wang, Yuxuan Dai, Chen Liao, Wenlong Huang, Hai Qian
The free fatty acid receptor 1 (FFA1) is a potential target due to its function in enhancing of glucose-stimulated insulin secretion. The FFA1 agonist GW9508 has great potential for the treatment of type 2 diabetes mellitus, but it has been suffering from high plasma clearance probably because the phenylpropanoic acid is vulnerable to β-oxidation. To identify orally available analog without influence on the unique pharmacological mechanism of GW9508, we tried to interdict the metabolically labile group by incorporating two deuterium atoms at the α-position of phenylpropionic acid affording compound 4 (HWL-066)...
May 18, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29777544/gingipains-disrupt-f-actin-and-cause-osteoblast-apoptosis-via-integrin-%C3%AE-1
#8
Q Qiu, F Zhang, J Wu, N Xu, M Liang
BACKGROUND AND OBJECTIVE: The aim of this study was to explore the cellular mechanisms underlying gingipain-caused changes in cell morphology and apoptosis of osteoblasts. MATERIAL AND METHODS: Human calvarial osteoblasts and mouse osteoblasts MC3T3-E1 were treated with gingipain extracts from Porphyromonas gingivalis stain W83. Apoptosis was detected with annexin V and propidium iodide flow cytometry analysis or terminal deoxynucleotidyl transferase mediated dUTP nick-end labeling staining...
May 18, 2018: Journal of Periodontal Research
https://www.readbyqxmd.com/read/29777154/calcimimetic-acts-on-enteric-neuronal-casr-to-reverse-cholera-toxin-induced-intestinal-electrolyte-secretion
#9
Lieqi Tang, Lingli Jiang, Megan E McIntyre, Ekaterina Petrova, Sam X Cheng
Treatment of acute secretory diarrheal illnesses remains a global challenge. Enterotoxins produce secretion through direct epithelial action and indirectly by activating enteric nervous system (ENS). Using a microperfused colonic crypt technique, we have previously shown that R568, a calcimimetic that activates the calcium-sensing receptor (CaSR), can act on intestinal epithelium and reverse cholera toxin-induced fluid secretion. In the present study, using the Ussing chamber technique in conjunction with a tissue-specific knockout approach, we show that the effects of cholera toxin and CaSR agonists on electrolyte secretion by the intestine can also be attributed to opposing actions of the toxin and CaSR on the activity of the ENS...
May 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29777058/gpr40-is-a-low-affinity-epoxyeicosatrienoic-acid-receptor-in-vascular-cells
#10
Sang Kyu Park, Anja Herrnreiter, Sandra L Pfister, Kathryn M Gauthier, Benjamin A Falck, John R Falck, William B Campbell
Endothelium-derived epoxyeicosatrienoic acids (EETs) have numerous vascular activities mediated by G protein--coupled receptors. Long-chain free fatty acids and EETs activate GPR40, prompting us to investigate the role of GPR40 in some vascular EET activities. 14,15-EET, 11,12-EET, arachidonic acid, and the GPR40 agonist GW9508 increase intracellular calcium concentrations in human GPR40-overexpressing HEK293 cells (EC50 = 0.58 ± 0.08 μM, 0.91 ± 0.08 μM, 3.9 ± 0.06 μM and 19 ± 0.37 nM, respectively)...
May 18, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29776968/liraglutide-modulates-appetite-and-body-weight-via-glp-1r-expressing-glutamatergic-neurons
#11
Jessica M Adams, Hongjuan Pei, Darleen A Sandoval, Randy J Seeley, Rui B Chang, Stephen D Liberles, David P Olson
Glucagon-like peptide-1 receptor (GLP-1R) agonists are FDA-approved weight loss drugs. Despite their widespread use, the sites of action through which GLP-1R agonists (GLP1RAs) impact appetite and body weight are still not fully understood. Here, we determined whether GLP-1Rs in either GABAergic or glutamatergic neurons are necessary for the acute and chronic effects of the GLP1RA liraglutide on food intake, visceral illness, body weight and neural network activation. We found that mice lacking GLP-1Rs in vGAT -expressing GABAergic neurons responded identically to controls in all parameters measured, whereas deletion of GLP-1Rs in vGlut2 -expressing glutamatergic neurons eliminated liraglutide-induced weight loss and visceral illness and severely attenuated its effects on feeding...
May 18, 2018: Diabetes
https://www.readbyqxmd.com/read/29776605/g-protein-coupled-receptor-resensitization-paradigms
#12
Manveen K Gupta, Maradumane L Mohan, Sathyamangla V Naga Prasad
Cellular responses to extracellular milieu/environment are driven by cell surface receptors that transmit the signal into the cells resulting in a synchronized and measured response. The ability to provide such exquisite responses to changes in external environment is mediated by the tight and yet, deliberate regulation of cell surface receptor function. In this regard, the seven transmembrane G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors that regulate responses like cardiac contractility, vision, and olfaction including platelet activation...
2018: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/29776604/biased-agonism-antagonism-of-cardiovascular-gpcrs-for-heart-failure-therapy
#13
Victoria L Desimine, Katie A McCrink, Barbara M Parker, Shelby L Wertz, Jennifer Maning, Anastasios Lymperopoulos
G protein-coupled receptors (GPCRs) are among the most important drug targets currently used in clinic, including drugs for cardiovascular indications. We now know that, in addition to activating heterotrimeric G protein-dependent signaling pathways, GPCRs can also activate G protein-independent signaling, mainly via the βarrestins. The major role of βarrestin1 and -2, also known as arrestin2 or -3, respectively, is to desensitize GPCRs, i.e., uncoupled them from G proteins, and to subsequently internalize the receptor...
2018: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/29776406/the-effect-of-dpp-4-inhibition-to-improve-functional-outcome-after-stroke-is-mediated-by-the-sdf-1%C3%AE-cxcr4-pathway
#14
Fausto Chiazza, Harald Tammen, Hiranya Pintana, Grazyna Lietzau, Massimo Collino, Thomas Nyström, Thomas Klein, Vladimer Darsalia, Cesare Patrone
BACKGROUND: Dipeptidyl peptidase-4 (DPP-4) inhibitors (gliptins) are approved drugs for the treatment of hyperglycemia in patients with type 2 diabetes. These effects are mainly mediated by inhibiting endogenous glucagon-like peptide-1 (GLP-1) cleavage. Interestingly, gliptins can also improve stroke outcome in rodents independently from GLP1. However, the underlying mechanisms are unknown. Stromal cell-derived factor-1α (SDF-1α) is a DPP-4 substrate and CXCR4 agonist promoting beneficial effects in injured brains...
May 19, 2018: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/29776349/randomised-controlled-trial-rct-of-cannabinoid-replacement-therapy-nabiximols-for-the-management-of-treatment-resistant-cannabis-dependent-patients-a-study-protocol
#15
Anjali K Bhardwaj, David J Allsop, Jan Copeland, Iain S McGregor, Adrian Dunlop, Marian Shanahan, Raimondo Bruno, Nghi Phung, Mark Montebello, Craig Sadler, Jessica Gugusheff, Melissa Jackson, Jennifer Luksza, Nicholas Lintzeris
BACKGROUND: The cannabis extract nabiximols (Sativex®) effectively supresses withdrawal symptoms and cravings in treatment resistant cannabis dependent individuals, who have high relapse rates following conventional withdrawal treatments. This study examines the efficacy, safety and cost-effectiveness of longer-term nabiximols treatment for outpatient cannabis dependent patients who have not responded to previous conventional treatment approaches. METHODS/DESIGN: A phase III multi-site outpatient, randomised, double-blinded, placebo controlled parallel design, comparing a 12-week course of nabiximols to placebo, with follow up at 24 weeks after enrolment...
May 18, 2018: BMC Psychiatry
https://www.readbyqxmd.com/read/29775956/typology-of-new-psychoactive-substance-use-among-the-general-australian-population
#16
Rachel Sutherland, Amy Peacock, Amanda Roxburgh, Monica J Barratt, Lucinda Burns, Raimondo Bruno
AIM: The aim of this study was to examine the typology of Australian illicit drug consumers to determine whether those who use new psychoactive substances (NPS) differ from those using other illicit substances. METHODS: Data were from the 2013 National Drug Strategy Household Survey, a representative population study; analyses were limited to participants reporting past year illicit drug use (including NPS; n = 3309). Latent class analysis identified groups based on past year substance use, and a weighted multivariable, multinomial regression model was used to examine characteristics associated with group membership...
May 3, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29775950/drechmerin-h-a-novel-1-2-2-18-diseco-indole-diterpenoid-from-the-fungus-drechmeria-sp-as-a-natural-agonist-of-human-pregnane-x-receptor
#17
Jian-Chao Zhao, Zhi-Lin Luan, Jia-Hao Liang, Zhong-Bin Cheng, Cheng-Peng Sun, Ya-Li Wang, Meng-Yue Zhang, Tian-Yuan Zhang, Yong Wang, Tian-Mei Yang, Ying-Ying Wu, Yi-Xuan Zhang, Xin-Yu Zhao, Xiao-Chi Ma
A novel 1(2), 2(18)-diseco indole diterpenoid, drechmerin H (1), was isolated from the fermentation broth of Drechmeria sp. together with a new indole diterpenoid, 2'-epi terpendole A (3), and a known analogue, terpendole A (2). Their structures were determined by HRESIMS, 1D and 2D NMR, ECD, and X-ray single crystal diffraction analyses as well as quantum chemical calculation. The abosulte configuration of terpendole A (2) was determined for the first time. Compound 1 displayed the significant agonistic effect on pregnane X receptor (PXR) with EC50 value of 134...
May 9, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29775649/expression-and-function-of-tlr4-induced-b1r-bradykinin-receptor-on-cardiac-fibroblasts
#18
Claudia Muñoz-Rodríguez, Samuel Fernández, José Miguel Osorio, Francisco Olivares, Renatto Anfossi, Samir Bolivar, Claudio Humeres, Pía Boza, Raúl Vivar, Viviana Pardo-Jimenez, Karen E Hemmings, Neil A Turner, Guillermo Díaz-Araya
Cardiac fibroblasts (CF) are key cells for maintaining extracellular matrix (ECM) protein homeostasis in the heart, and for cardiac repair through CF-to-cardiac myofibroblast (CMF) differentiation. Additionally, CF play an important role in the inflammatory process after cardiac injury, and they express Toll like receptor 4 (TLR4), B1 and B2 bradykinin receptors (B1R and B2R) which are important in the inflammatory response. B1R and B2R are induced by proinflammatory cytokines and their activation by bradykinin (BK: B2R agonist) or des-arg-kallidin (DAKD: B1R agonist), induces NO and PGI2 production which is key for reducing collagen I levels...
May 15, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29775630/the-basolateral-amygdala-dopaminergic-system-contributes-to-the-improving-effect-of-nicotine-on-stress-induced-memory-impairment-in-rats
#19
Elnaz Keshavarzian, Zahra Ghasemzadeh, Ameneh Rezayof
Stress seems to be an important risk factor in the beginning and continuing stages of cigarette tobacco smoking in humans. Considering that both of nicotine administration and stress exposure affect cognitive functions including memory formation, the aim of the present study was 1) to evaluate the effect of subcutaneous (s.c.) administration of nicotine on memory formation under stress and 2) to assess the possible role of the basolateral amygdala (BLA) dopamine D1 and D2 receptors in the effect of nicotine on stress-induced memory retrieval impairment...
May 15, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29775561/isolation-and-characterization-of-a-novel-anti-salbutamol-chicken-scfv-for-human-doping-urinalysis
#20
Warren Lee, Syed A Ali, Leow Chiuan Yee, Tan Soo Choon, Leow Chiuan Herng
Anti-salbutamol antibodies remain as important tools for the detection of salbutamol abuse in athletic doping. This study evaluated the feasibility and efficiency of the chicken (Gallus gallus domesticus) as an immunization host to generate anti-salbutamol scFv antibodies by phage display. A phage display antibody library was constructed from a single chicken immunized against salbutamol-KLH conjugate. After a stringent biopanning strategy, a novel scFv clone which was inhibited by free salbutamol recorded the highest affinity...
May 15, 2018: Analytical Biochemistry
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