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https://www.readbyqxmd.com/read/28441746/high-performance-prediction-of-human-estrogen-receptor-agonists-based-on-chemical-structures
#1
Yuki Asako, Yoshihiro Uesawa
Many agonists for the estrogen receptor are known to disrupt endocrine functioning. We have developed a computational model that predicts agonists for the estrogen receptor ligand-binding domain in an assay system. Our model was entered into the Tox21 Data Challenge 2014, a computational toxicology competition organized by the National Center for Advancing Translational Sciences. This competition aims to find high-performance predictive models for various adverse-outcome pathways, including the estrogen receptor...
April 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28441725/sweet-taste-receptor-activation-in-the-gut-is-of-limited-importance-for-glucose-stimulated-glp-1-and-gip-secretion
#2
Monika Y Saltiel, Rune E Kuhre, Charlotte B Christiansen, Rasmus Eliasen, Kilian W Conde-Frieboes, Mette M Rosenkilde, Jens J Holst
Glucose stimulates the secretion of the incretin hormones: glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). It is debated whether the sweet taste receptor (STR) triggers this secretion. We investigated the role of STR activation for glucose-stimulated incretin secretion from an isolated perfused rat small intestine and whether selective STR activation by artificial sweeteners stimulates secretion. Intra-luminal administration of the STR agonists, acesulfame K (3.85% w/v), but not sucralose (1...
April 22, 2017: Nutrients
https://www.readbyqxmd.com/read/28441717/dexmedetomidine-relieves-formaldehyde-induced-pain-in-rats-through-both-%C3%AE-2-adrenoceptor-and-imidazoline-receptor
#3
Hong Zhang, Xiang Yan, De-Gui Wang, Yu-Fang Leng, Zhan-Hai Wan, Yong-Qiang Liu, Yan Zhang
Dexmedetomidine (DEX) is a highly selective α2 adrenergic receptor agonist. In this study, we investigated the analgesic effect and the underlying mechanisms of DEX on inflammatory visceral pain in rats. Twenty-five male Sprague Dawley (SD) rats were randomly divided into 5 groups, including control, sham, low dose DEX, medium dose DEX and high dose DEX group. Pain was induced with 10% formalin and scored every 15min till 2 h-post the induction. Hematoxylin-eosin (HE) staining was used to evaluate the toxicity of DEX on spinal cord neurons...
April 21, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28441661/defective-platelet-activation-and-bleeding-complications-upon-cholestasis-in-mice
#4
Nina Sarah Gowert, Meike Klier, Maria Reich, Friedrich Reusswig, Lili Donner, Verena Keitel, Dieter Häussinger, Margitta Elvers
BACKGROUND/AIMS: Platelets are essential mediators of hemostasis to avoid excessive blood loss. Cirrhosis and chronic liver diseases are characterized by alterations in hemostasis. Alterations in the secondary hemostasis have been well studied, while defects in primary hemostasis, especially the consequences of cholestatic liver disease on platelet function are not well defined. METHODS: After bile duct ligation (BDL) platelet activation and thrombus formation were analyzed in mice...
April 20, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28441276/augs-consensus-statement-association-of-anticholinergic-medication-use-and-cognition-in-women-with-overactive-bladder
#5
(no author information available yet)
Overactive bladder affects a significant portion of the overall population and has substantial impact on daily activities and quality-of-life. When considering treatment, behavioral therapies should be instituted first, followed by medical therapies. Anticholinergic medications and beta-3 agonists are often used as initial pharmacologic therapy, but caution should be taken in prescribing anticholinergic medications in frail or cognitively impaired patients. Recently, concerns have developed regarding anticholinergic medications and the associated risk of cognitive impairment, dementia, and Alzheimer disease in the general population...
May 2017: Female Pelvic Medicine & Reconstructive Surgery
https://www.readbyqxmd.com/read/28441273/case-report-of-physiologic-phenibut-dependence-treated-with-a-phenobarbital-taper-in-a-patient-being-treated-with-buprenorphine
#6
Emily Brunner, Robert Levy
: This case report describes the development of dependence to phenibut, a gamma-aminobutyric acid-receptor type B agonist, in a patient concurrently being treated with buprenorphine. The patient experienced withdrawal symptoms which were successfully treated with a phenobarbital taper based on a protocol to treat sedative use disorder. This case report provided an example of the development of a phenibut use disorder and also brought up a public health question of whether phenibut should therefore be officially classified and monitored...
April 24, 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28441106/jwh-122-consumption-adverse-effects-a-case-of-hallucinogen-persisting-perception-disorder-five-year-follow-up
#7
Maurizio Coppola, Raffaella Mondola
Synthetic cannabinoid receptor agonists are a heterogeneous group of psychotropic drugs functionally related to Δ9-tetrahydrocannabinol. These substances, marketed as cannabis substitutes, have been associated with numerous cases of severe intoxication and death across the world. In our article, we describe a case of hallucinogen persisting perception disorder developing in a natural cannabis user after consumption of JWH-122, a naphthoylindole largely used since 2010. Clinical symptomatology persisted for about four years and was alleviated through treatment with clonazepam...
April 25, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28441050/comparison-of-platelet-function-and-viscoelastic-test-results-between-healthy-dogs-and-dogs-with-naturally-occurring-chronic-kidney-disease
#8
Alicia Dudley, Julie K Byron, Mary Jo Burkhard, Emma Warry, Julien Guillaumin
OBJECTIVE To compare platelet function and viscoelastic test results between healthy dogs and dogs with chronic kidney disease (CKD) to assess whether dogs with CKD have platelet dysfunction and altered blood coagulation. ANIMALS 10 healthy control dogs and 11 dogs with naturally occurring CKD. PROCEDURES Blood and urine were collected once from each dog for a CBC, serum biochemical analysis, urinalysis, and determination of the urine protein-to-creatinine ratio, prothrombin time, activated partial thromboplastin time, plasma fibrinogen concentration, and antithrombin activity...
May 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28440739/featured-article-pharmacological-postconditioning-with-delta-opioid-attenuates-myocardial-reperfusion-injury-in-isolated-porcine-hearts
#9
Maria Seewald, James A Coles, Daniel C Sigg, Paul A Iaizzo
Ischemic preconditioning has been utilized to protect the heart from ischemia prior to ischemia onset, whereas postconditioning is employed to minimize the consequences of ischemia at the onset of reperfusion. The underlying mechanisms and pathways of ischemic pre- and postconditioning continue to be investigated as therapeutic targets. We evaluated the administration of a delta opioid agonist or cariporide on various parameters associated with myocardial reperfusion injury upon reperfusion of isolated porcine hearts...
May 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28440715/gnrh-agonist-triggering-for-final-oocyte-maturation-in-gnrh-antagonist-ivf-cycles-induces-decreased-lh-pulse-rate-and-amplitude-in-early-luteal-phase-a-possible-luteolysis-mechanism
#10
Samer Tannus, Yechiel Burke, Christopher R McCartney, Shahar Kol
The use of GnRH agonist to trigger final oocyte maturation in GnRH-antagonist in vitro fertilization (IVF) cycles has been shown to significantly reduce or even eliminate the risk of ovarian hyperstimulation syndrome (OHSS) by inducing rapid luteolysis early in the luteal phase. The exact mechanism of this early luteolysis is still widely unknown. Since luteinizing hormone (LH) has a major role in corpus luteum support, we sought to explore the pattern of LH secretion early in the luteal phase. Ten high risk patients for developing OHSS and triggered with GnRH agonist were included...
April 25, 2017: Gynecological Endocrinology
https://www.readbyqxmd.com/read/28440686/severe-ovarian-hyperstimulation-syndrome-after-combined-gnrh-agonist-and-low-dose-human-chorionic-gonadotropin-trigger-in-a-patient-with-a-single-kidney
#11
Nigel Pereira, Jovana P Lekovich, Isaac Kligman, Zev Rosenwaks
Ovarian hyperstimulation syndrome (OHSS) following gonadotropin-releasing hormone agonist (GnRH-a) trigger is rare. Here, we report a case of severe OHSS after combined GnRH-a and low-dose human chorionic gonadotropin (hCG) trigger in a patient with a single kidney. The patient is a 32-year-old women with a two-year history of infertility. The patient's history was significant for a single kidney, that is, she had donated a kidney to a family member three years ago. The patient underwent controlled ovarian stimulation (COS) for in vitro fertilization (IVF) and received a combined 2 mg GnRH-a and 1500 IU hCG ovulatory trigger...
April 25, 2017: Gynecological Endocrinology
https://www.readbyqxmd.com/read/28440494/low-dose-paclitaxel-suppresses-the-induction-of-m2%C3%A2-macrophages-in-gastric-cancer
#12
Takahisa Yamaguchi, Sachio Fushida, Yasuhiko Yamamoto, Tomoya Tsukada, Jun Kinoshita, Katsunobu Oyama, Tomoharu Miyashita, Hidehiro Tajima, Itasu Ninomiya, Seiichi Munesue, Ai Harashima, Shinichi Harada, Hiroshi Yamamoto, Tetsuo Ohta
Tumor-associated macrophages of the M2 phenotype promote tumor proliferation and are associated with a poor prognosis in patients with various malignancies, including gastric cancer with peritoneal dissemination. The present study assessed whether paclitaxel (PTX) suppresses M2 macrophages, by acting as a Toll-like receptor 4 (TLR4) agonist. Macrophages derived from the THP-1 monocytic cell line and peripheral blood mononuclear cell (PBMC)-derived macrophages were cultured with gastric cancer cells in medium containing PTX, at a concentration that did not affect cell proliferation...
April 19, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28440451/ppar%C3%AE-activation-protects-h9c2-cardiomyoblasts-from-lps%C3%A2-induced-apoptosis-through-the-heme-oxygenase%C3%A2-1%C3%A2-mediated-suppression-of-nf%C3%A2-%C3%AE%C2%BAb-activation
#13
Yao Shi, Hong Jiang, Xiaobo Yang
The aim of the present study was to investigate the protective effect of the selective peroxisome proliferator-activated receptor δ (PPARδ) agonist GW501516 (GW) on lipopolysaccharide (LPS)‑induced apoptosis in the rat cardiomyoblast cell line H9c2, and to investigate the possible underlying mechanisms. Cell viability was estimated using the MTT assay. Apoptosis was estimated by flow cytometry using Annexin V‑fluorescein isothiocyanate/propidium iodide staining and caspase‑3 activity assay. The protein level of heme oxygenase‑1 (HO‑1), cleaved caspase‑3 (CC3), apoptosis regulator Bcl‑2 (bcl‑2), apoptosis regulator BAX (bax) and nuclear factor‑κB (NF‑κB) p65 was measured by western blot analysis...
April 19, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28440280/targeting-asic3-for-relieving-mice-fibromyalgia-pain-roles-of-electroacupuncture-opioid-and-adenosine
#14
Liang-Ta Yen, Ching-Liang Hsieh, Hsin-Cheng Hsu, Yi-Wen Lin
Many scientists are seeking better therapies for treating fibromyalgia (FM) pain. We used a mouse model of FM to determine if ASIC3 and its relevant signaling pathway participated in FM pain. We demonstrated that FM-induced mechanical hyperalgesia was attenuated by electroacupuncture (EA). The decrease in fatigue-induced lower motor function in FM mice was also reversed by EA. These EA-based effects were abolished by the opioid receptor antagonist naloxone and the adenosine A1 receptor antagonist rolofylline...
April 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28440199/anti-hyperglycemic-agents-for-the-treatment-of-type-2-diabetes-mellitus-role-in-cardioprotection-during-the-last-decade
#15
Duygu Kocyigit, Kadri Murat Gurses, Muhammed Ulvi Yalcin, Lale Tokgozoglu
Type 2 diabetic patients are known to have a tendency to develop cardiovascular (CV) disease (CVD), and related unfavourable outcomes such as heart failure, myocardial infarction (MI), cerebrovascular events (eg. stroke), and related mortality. Long- term clinical trials have revealed contradictory findings regarding the relationship between glycemic control and CV benefits due to variations in the key characteristics of the study population. During the last decade, number of pharmacological agents used for glucose- lowering in the treatment of type 2 diabetes mellitus (T2DM) has increased owing to the introduction of dipeptidyl peptidase- IV (DPP- IV) inhibitors, glucagon- like peptide- 1 (GLP- 1) receptor agonists, and sodium-glucose co-transporter 2 (SGLT- 2) inhibitors...
April 23, 2017: Endocrine, Metabolic & Immune Disorders Drug Targets
https://www.readbyqxmd.com/read/28440186/the-double-roles-of-the-prostaglandin-e2-ep2-receptor-in-intracerebral-hemorrhage
#16
Xu Luo, Qiquan Zhu, Jie Zhang, Qin Huang, Zongyi Xie, Yuan Cheng
Intracerebral hemorrhage (ICH), a subtype of stroke, brings high morbidity and mortality to human beings. Multiple studies indicate that neuroinflammation, excitotoxicity, oxidative stress, cytotoxicity resulted from the degradation products of blood clot play vital roles in ICH-induced secondary brain injury, which contributes to deterioration of neurological outcome. Prostaglandin E2 (PGE2), a type of prostanoids commonly up-regulated in these progresses, is known to modulate numerous cellular and molecular processes and involve in various diseases, including ICH, cerebral ischemic, Alzheimer's disease (AD) and amyotrophic lateral sclerosis (ALS) etc...
April 24, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28439968/effects-of-an-ep2-and-ep3-receptor-dual-agonist-ono-8055-on-a-radical-hysterectomy-induced-underactive-bladder-model-in-monkeys
#17
Hidekazu Matsuya, Noritoshi Sekido, Jun Kida, Hiroko Mashimo, Daisuke Wakamatsu, Hiroki Okada
OBJECTIVES: The objective was to develop an underactive bladder (UAB) model in primates and to evaluate the potential of prostanoid EP2 and EP3 receptor dual agonist ONO-8055 to become a therapeutic agent for UAB. METHODS: A surgical procedure resembling radical hysterectomy was performed on female cynomolgus monkeys. Subsequently, in vitro muscle strip studies were performed using bladder muscle strips from normal monkeys and monkeys that underwent surgery. In addition, uroflowmetric data were obtained at specified days after the surgery...
April 25, 2017: Lower Urinary Tract Symptoms
https://www.readbyqxmd.com/read/28439947/sirt1-hsf1-hsps-pathway-is-essential-for-exenatide-alleviated-lipid-induced-hepatic-endoplasmic-reticulum-stress
#18
Xiaobin Zheng, Fen Xu, Hua Liang, Huanyi Cao, Mengyin Cai, Wen Xu, Jianping Weng
Recent studies have indicated lipid-induced endoplasmic reticulum (ER) stress to be a major contributor to the progression of hepatic steatosis. Exenatide (Exendin-4), a glucagon-like peptide-1 receptor agonist, is known to improve hepatic steatosis with accumulating evidence. In this study, we investigated whether exenatide could alleviate lipid-induced hepatic ER stress through mammal sirtuin1 (SIRT1) and illustrated the detailed mechanisms. Male C57BL/6J mice challenged with a high-fat diet (HFD) were then treated with exenatide or normal saline by intraperitoneal injection for 4 weeks...
April 25, 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/28439871/application-of-chemical-genomics-to-plant-bacteria-communication-a-high-throughput-system-to-identify-novel-molecules-modulating-the-induction-of-bacterial-virulence-genes-by-plant-signals
#19
Elodie Vandelle, Maria Rita Puttilli, Andrea Chini, Giulia Devescovi, Vittorio Venturi, Annalisa Polverari
The life cycle of bacterial phytopathogens consists of a benign epiphytic phase, during which the bacteria grow in the soil or on the plant surface, and a virulent endophytic phase involving the penetration of host defenses and the colonization of plant tissues. Innovative strategies are urgently required to integrate copper treatments that control the epiphytic phase with complementary tools that control the virulent endophytic phase, thus reducing the quantity of chemicals applied to economically and ecologically acceptable levels...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28439742/exploration-of-the-binding-affinities-between-ecdysone-agonists-and-ecr-usp-by-docking-and-mm-pb-gbsa-approaches
#20
Xueping Hu, Jin Xie, Song Hu, Li Zhang, Yanhong Dong
Ecdysone receptor (EcR) is a significant target in the identification of new environmentally friendly pesticides. There are two types of ecdysone agonists: steroidal ecdysone agonists and dibenzoylhydrazines (DBHs). In this study, various modeling methods (homology modeling, molecular docking, MD simulation, binding free energy calculation, and per-residue binding free energy decomposition) were utilized to study the different binding mechanisms of two types of ecdysone agonists. Our theoretical results indicated that the relative binding potencies of DBHs can be ranked sufficiently accurately using the MOE docking method...
May 2017: Journal of Molecular Modeling
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