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https://www.readbyqxmd.com/read/28727908/leveraging-a-clinical-phase-ib-proof-of-concept-study-for-the-gpr40-agonist-mk-8666-in-patients-with-type-2-diabetes-for-model-informed-phase-ii-dose-selection
#1
A W Krug, P Vaddady, R A Railkar, B J Musser, J Cote, Agh Ederveen, D G Krefetz, E DeNoia, A L Free, L Morrow, M V Chakravarthy, E Kauh, D A Tatosian, P A Kothare
GPR40 mediates free fatty acid-induced insulin secretion in beta cells. We investigated the safety, pharmacokinetics, and glucose response of MK-8666, a partial GPR40 agonist, after once-daily multiple dosing in type 2 diabetes patients. This double-blind, multisite, parallel-group study randomized 63 patients (placebo, n = 18; 50 mg, n = 9; 150 mg, n = 18; 500 mg, n = 18) for 14-day treatment. The results showed no serious adverse effects or treatment-related hypoglycemia. One patient (150-mg group) showed mild-to-moderate transaminitis at the end of dosing...
July 20, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/28727644/cariprazine-specificity-profile-in-the-treatment-of-acute-schizophrenia-a-meta-analysis-and-meta-regression-of-randomized-controlled-trials
#2
Filippo Corponi, Alessandro Serretti, Stuart Montgomery, Chiara Fabbri
Cariprazine is a new dopamine D2 and D3 receptor partial agonist antipsychotic. Meta-analytic evidence of efficacy in acute schizophrenia and specific groups of patients is lacking. We carried out a meta-analysis in patients with acute schizophrenia to evaluate the efficacy of cariprazine over placebo and active comparators in overall symptoms, positive and negative symptoms and quality of life. Low and high (≥6 mg/day) doses were tested separately. The possible effect of clinical-demographic modulators was also tested...
July 19, 2017: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28726982/effects-of-ractopamine-hydrochloride-on-growth-performance-carcass-characteristics-and-physiological-response-to-different-handling-techniques
#3
J A Hagenmaier, C D Reinhardt, M J Ritter, M S Calvo-Lorenzo, G J Vogel, C A Guthrie, M G Siemens, K F Lechtenberg, D J Rezac, D U Thomson
Feedlot cattle ( = 128; BW = 549 ± 60 kg) were used to evaluate the effects of ractopamine hydrochloride (RAC) on growth performance, physiological response to handling, and mobility during shipment for slaughter in a study utilizing a split-plot design with a 2 × 2 factorial arrangement of treatments: 1) diet (CON [no β-adrenergic agonist] vs. RAC [400 mg·animal·d ractopamine hydrochloride for 28 d]) and 2) handling intensity (HI; low-stress handling [LSH; cattle moved at a walking pace with no electric prod use] vs...
May 2017: Journal of Animal Science
https://www.readbyqxmd.com/read/28725924/effect-of-training-status-on-beta-range-corticomuscular-coherence-in-agonist-vs-antagonist-muscles-during-isometric-knee-contractions
#4
Fabien Dal Maso, Marieke Longcamp, Sylvain Cremoux, David Amarantini
Antagonist muscle co-activation is thought to be partially regulated by cortical influences, but direct motor cortex involvement is not fully understood. Corticomuscular coherence (CMC) measures direct functional coupling of the motor cortex and muscles. As antagonist co-activation differs according to training status, comparison of CMC in agonist and antagonist muscles and in strength-trained and endurance-trained individuals may provide in-depth knowledge of cortical implication in antagonist muscle co-activation...
July 19, 2017: Experimental Brain Research. Experimentelle Hirnforschung. Expérimentation Cérébrale
https://www.readbyqxmd.com/read/28724496/effects-of-time-and-storage-conditions-on-the-chemical-and-microbiologic-stability-of-diluted-buprenorphine-for-injection
#5
Johnathan M DenHerder, Ralph L Reed, Jennifer L Sargent, Gerd Bobe, Jan F Stevens, Helen E Diggs
Buprenorphine is a partial μ-opioid agonist used for analgesia. Due to the small size of laboratory rodents, buprenorphine HCl is typically diluted 10- or 20-fold with a sterile diluent, such as saline, for accurate dosing. Protocols for preparing and storing diluted buprenorphine vary by institution, and little published information is available regarding stability and beyond-use dating of specific buprenorphine preparations. The purpose of this study was to determine the chemical and microbiologic stability of diluted buprenorphine stored for a maximum of 180 d...
July 1, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28723517/practice-patterns-compared-with-evidence-based-strategies-for-the-management-of-androgen-deprivation-therapy-induced-side-effects-in-prostate-cancer-patients-results-of-a-european-web-based-survey
#6
Renée Bultijnck, Cristian Surcel, Guillaume Ploussard, Alberto Briganti, Pieter De Visschere, Jurgen Fütterer, Pirus Ghadjar, Gianluca Giannarini, Hendrik Isbarn, Christophe Massard, Prasanna Sooriakumaran, Massimo Valerio, Roderick van den Bergh, Piet Ost
BACKGROUND: Evidence-based recommendations are available for the management of androgen deprivation therapy (ADT)-induced side effects; however, there are no data on the implementation of the recommendations into daily practice patterns. OBJECTIVE: To compare practice patterns in the management of ADT-induced side effects with evidence-based strategies. DESIGN, SETTING, AND PARTICIPANTS: A European Web-based survey was conducted from January 16, 2015, to June 24, 2015...
December 2016: European Urology Focus
https://www.readbyqxmd.com/read/28722223/the-role-of-%C3%AE-adrenergic-receptors-and-p38mapk-signaling-pathways-in-physiological-processes-of-cardiosphere-derived-cells
#7
Wen-Bo Zhang, Yun-Qi Liu, Xi Zhang, Lin Lin, Sheng-Li Yin
The effects of β adrenergic receptors (β-ARs) and p38 mitogen-activated protein kinases (MAPK) pathways on cardiosphere-derived cells (CDCs) are largely unknown. This study aimed to investigate the roles of β-ARs and p38MAPK pathways on the proliferation, apoptosis and differentiation capacity of CDCs. The CDCs were treated with β1-AR blocker (Met group), β2-AR antagonist (ICI group) and p38MAPK inhibitor (SB group), nonselective β-AR blocker (PRO group), and β-AR agonist (ISO group). The viability, apoptotic rate and differentiation status of CDCs were determined by MST-1 assay, flow cytometery, and Western blot, respectively...
July 19, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28722168/role-of-palmitoylation-of-cysteine-415-in-functional-coupling-cb1-receptor-to-g%C3%AE-i2-protein
#8
Sergio Oddi, Antonio Totaro, Lucia Scipioni, Beatrice Dufrusine, Tomasz Maciej Stepniewski, Jana Selent, Mauro Maccarrone, Enrico Dainese
In this study, we investigated the role of CB1 palmitoylation in modulating the functional interaction with G proteins both in the absence and in the presence of agonist binding. Our data show that the non-palmitoylated CB1 receptor significantly reduced its association with Gαi2 . The agonist-stimulation induced a partial dissociation of Gαi2 proteins from the wild-type receptor, while on the C415A mutant the agonist binding was not able to induce a significant dissociation of Gαi2 from the receptor. Our data suggest that the lack of palmitoyl chain hampers the ability of the receptor to functionally interact with the Gαi2 and indicate that the palmitoyl chain is responsible for the functional transmission of the agonist-induced conformational change of the receptor to the G protein...
July 19, 2017: Biotechnology and Applied Biochemistry
https://www.readbyqxmd.com/read/28722020/a-critical-role-of-gas6-axl-signal-in-allergic-airway-responses-during-rsv-vaccine-enhanced-disease
#9
Takehiko Shibata, Manabu Ato
Respiratory syncytial virus (RSV) is a common virus that causes lower respiratory infections across a wide range of ages. A licensed RSV vaccine is not available because vaccination with formalin-inactivated RSV (FI-RSV) and the subsequent RSV infection cause not only insufficient induction of neutralizing antibodies but also severe allergic airway responses, termed FI-RSV vaccine enhanced disease (FI-RSV VED). However, the underlying mechanism has not been identified, although a Th2-biased immune response is known to be a hallmark of this disease...
July 19, 2017: Immunology and Cell Biology
https://www.readbyqxmd.com/read/28720775/metformin-ameliorates-the-phenotype-transition-of-peritoneal-mesothelial-cells-and-peritoneal-fibrosis-via-a-modulation-of-oxidative-stress
#10
Hyun-Soo Shin, Jiyeon Ko, Dal-Ah Kim, Eun-Sun Ryu, Hye-Myung Ryu, Sun-Hee Park, Yong-Lim Kim, Eok-Soo Oh, Duk-Hee Kang
Phenotype transition of peritoneum is an early mechanism of peritoneal fibrosis. Metformin, 5'-adenosine monophosphate-activated protein kinase (AMPK) activator, has recently received a new attention due to its preventive effect on organ fibrosis and cancer metastasis by inhibiting epithelial-to-mesenchymal transition (EMT). We investigated the effect of metformin on EMT of human peritoneal mesothelial cells (HPMC) and animal model of peritoneal dialysis (PD). TGF-β1-induced EMT in HPMC was ameliorated by metformin...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28720478/monoamine-receptor-interaction-profiles-of-4-thio-substituted-phenethylamines-2c-t-drugs
#11
REVIEW
Dino Luethi, Daniel Trachsel, Marius C Hoener, Matthias E Liechti
BACKGROUND: 4-Thio-substituted phenethylamines (2C-T drugs) are potent psychedelics with poorly defined pharmacological properties. Because of their psychedelic effects, 2C-T drugs are sometimes sold as new psychoactive substances (NPSs). The aim of the present study was to characterize the monoamine receptor and transporter interaction profiles of a series of 2C-T drugs. METHODS: We determined the binding affinities of 2C-T drugs at monoamine receptors and transporters in human cells that were transfected with the respective receptors or transporters...
July 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28716269/dopamine-agonist-withdrawal-syndrome-daws-in-a-tertiary-parkinson-disease-treatment-center
#12
Shnehal Patel, Xiomara Garcia, Mohammad Edrees Mohammad, Xin Xin Yu, Katelyn Vlastaris, Kaley O'Donnell, Kathryn Sutton, Hubert H Fernandez
INTRODUCTION: Dopamine agonists are a mainstay of treatment for patients with Parkinson disease (PD). However, side effects limit their use, often necessitating dose change. Upon withdrawal, patients may experience dopamine agonist withdrawal syndrome (DAWS). To date, there is no established protocol for the prevention or treatment of DAWS. METHODS: We performed a retrospective chart review of PD patients who were taking a dopamine agonist. RESULTS: In our large cohort of 313 PD patients who were on a dopamine agonist, we found that 39...
August 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28716170/sinonasal-t2r-mediated-nitric-oxide-production-in-response-to-bacillus-cereus
#13
Ryan M Carey, Alan D Workman, Carol H Yan, Bei Chen, Nithin D Adappa, James N Palmer, David W Kennedy, Robert J Lee, Noam A Cohen
BACKGROUND: Upper airway epithelial cells produce bactericidal nitric oxide (NO) in response to both gram-positive and gram-negative bacteria. Our previous work demonstrated that T2R38, a bitter taste receptor (T2R) expressed in airway epithelium, produces NO in response to quorum-sensing molecules secreted by Pseudomonas aeruginosa. We also demonstrated that Staphylococci products elicit an NO response when using a T2R-independent pathway. When screening additional human pathogens for epithelial T2R activation, we found that the gram-positive aerobe Bacillus cereus secretes a T2R agonist that yields NO production...
July 1, 2017: American Journal of Rhinology & Allergy
https://www.readbyqxmd.com/read/28705810/the-butyrophilin-3a1-intracellular-domain-undergoes-a-conformational-change-involving-the-juxtamembrane-region
#14
Khiem Nguyen, Jin Li, Robbins Puthenveetil, Xiaochen Lin, Michael M Poe, Chia-Hung Christine Hsiao, Olga Vinogradova, Andrew J Wiemer
Small isoprenoid diphosphates, such as (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate (HMBPP), are ligands of the internal domain of BTN3A1. Ligand binding in target cells promotes activation of Vγ9Vδ2 T cells. We demonstrate by small-angle X-ray scattering (SAXS) that HMBPP binding to the internal domain of BTN3A1 induces a conformational change in the position of the B30.2 domain relative to the juxtamembrane (JM) region. To better understand the molecular details of this conformational rearrangement, NMR spectroscopy was used to discover that the JM region interacts with HMBPP, specifically at the diphosphate...
July 13, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28697115/selective-progesterone-receptor-modulators-for-the-treatment-of-uterine-leiomyomas
#15
Myriam Safrai, Henry H Chill, Adi Reuveni Salzman, Asher Shushan
Uterine leiomyomas have drawn much attention since being described more than 200 years ago. These common benign uterine tumors often present with prolonged menstrual bleeding, pelvic pressure, and reproductive disorders and pose a true financial burden on health care systems all over the world. Over the past few decades, surgical treatment of uterine leiomyomas has received most of the focus compared with other treatment options. Choosing the appropriate surgical technique depends on many factors such as uterine leiomyoma location, patient's age, interest in future fertility, concomitant comorbidities, and the patient's preference...
July 7, 2017: Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28696131/partial-dopamine-agonist-induced-pathological-gambling-and-impulse-control-deficit-on-low-dose-aripiprazole
#16
Evan Peterson, Rosaria Forlano
OBJECTIVE: To describe a case of aripiprazole-induced problem gambling and impulse-control deficit in a gambling-naïve patient following commencement of low-dose aripiprazole. METHOD: Case report. RESULTS: This case adds to the literature on the dopamine partial agonist aripiprazole causing or exacerbating problem gambling, and extends that literature to low-dose use of aripiprazole in the gambling naïve. CONCLUSIONS: When commencing a patient on aripiprazole the possibility of emergence of problem gambling and other impulse-control deficits should be monitored, even in those with no history of similar behaviours and even on a low dose...
July 1, 2017: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
https://www.readbyqxmd.com/read/28695626/mucosal-glucagon-like-peptide-1-glp-1-responses-are-mediated-by-calcitonin-gene-related-peptide-cgrp-in-the-mouse-colon-and-both-peptide-responses-are-area-specific
#17
I R Tough, R Moodaley, H M Cox
BACKGROUND: Glucagon-like peptide (GLP)-1 is an incretin hormone and its mimetics are proven antidiabetic and antiobesity drugs. GLP-1 exerts antimotility and mucosal proliferative activities but its epithelial ion transport effects are uncharacterized and these may contribute to the gastrointestinal (GI) disturbance, i.e., diarrhea experienced with some GLP-1 mimetics. Our aim was to establish GLP-1 agonist mechanisms and identify potential mucosal mediator(s) in the colonic tissue from C57BL/6J mice...
July 11, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28694780/the-effect-of-pungent-and-tingling-compounds-from-piper-nigrum-l-on-background-k-currents
#18
Leopoldo R Beltrán, Corinna Dawid, Madeline Beltrán, Janina Levermann, Sascha Titt, Sini Thomas, Viktoria Pürschel, Miriam Satalik, Günter Gisselmann, Thomas Hofmann, Hanns Hatt
Black peppercorns (Piper nigrum L.) elicit a pungent and tingling oral impression. Their pungency is partially explained by the agonist activity of some of their active principles, especially piperine, on TRP channels. However, we recently showed that piperine, as well as other pungent compounds, also possess a marked effect on two-pore domain (KCNK, K2P) K(+) channels. Members of this family play a key role in maintaining the resting membrane potential of excitable cells. Interestingly, tingling compounds have been shown to induce neuronal excitation by inhibiting KCNK channels...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28693859/the-%C3%AE-3%C3%AE-4-nachr-partial-agonist-at-1001-attenuates-stress-induced-reinstatement-of-nicotine-seeking-in-a-rat-model-of-relapse-and-induces-minimal-withdrawal-in-dependent-rats
#19
Menglu Yuan, Ariana M Malagon, Dennis Yasuda, James D Belluzzi, Frances M Leslie, Nurulain T Zaveri
The strong reinforcing effects of nicotine and the negative symptoms such as anxiety experienced during a quit attempt often lead to relapse and low success rates for smoking cessation. Treatments that not only block the reinforcing effects of nicotine but also attenuate the motivation to relapse are needed to improve cessation rates. Recent genetic and preclinical studies have highlighted the involvement of the α3, β4, and α5 nicotinic acetylcholine receptor (nAChR) subunits and the α3β4 nAChR subtype in nicotine dependence and withdrawal...
July 7, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28692485/safety-and-tolerability-of-cariprazine-in-patients-with-acute-exacerbation-of-schizophrenia-a-pooled-analysis-of-four-phase-ii-iii-randomized-double-blind-placebo-controlled-studies
#20
Willie Earley, Suresh Durgam, Kaifeng Lu, István Laszlovszky, Marc Debelle, John M Kane
Cariprazine, a potent dopamine D3 and D2 receptor partial agonist antipsychotic with preferential binding to D3 receptors, is Food and Drug Administration approved for treating schizophrenia and manic or mixed episodes of bipolar I disorder. A post-hoc safety/tolerability analysis of data from the four acute trials in the cariprazine schizophrenia clinical development program (NCT00404573; NCT00694707; NCT01104766; NCT01104779) was carried out using the overall safety population (all patients who received ≥1 dose of study drug) and modal daily dose subgroups (1...
July 7, 2017: International Clinical Psychopharmacology
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