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https://www.readbyqxmd.com/read/29677442/synthesis-and-pharmacological-evaluation-of-novel-c-8-substituted-tetrahydroquinolines-as-balanced-affinity-mu-delta-opioid-ligands-for-the-treatment-of-pain
#1
Anthony F Nastase, Nicholas W Griggs, Jessica P Anand, Thomas J Fernandez, Aubrie A Harland, Tyler J Trask, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg
The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a -opioid receptor (MOR) agonist/-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position...
April 20, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29677303/association-between-use-of-sodium-glucose-cotransporter-2-inhibitors-glucagon-like-peptide-1-agonists-and-dipeptidyl-peptidase-4-inhibitors-with-all-cause-mortality-in-patients-with-type-2-diabetes-a-systematic-review-and-meta-analysis
#2
Sean L Zheng, Alistair J Roddick, Rochan Aghar-Jaffar, Matthew J Shun-Shin, Darrel Francis, Nick Oliver, Karim Meeran
Importance: The comparative clinical efficacy of sodium-glucose cotransporter 2 (SGLT-2) inhibitors, glucagon-like peptide 1 (GLP-1) agonists, and dipeptidyl peptidase 4 (DPP-4) inhibitors for treatment of type 2 diabetes is unknown. Objective: To compare the efficacies of SGLT-2 inhibitors, GLP-1 agonists, and DPP-4 inhibitors on mortality and cardiovascular end points using network meta-analysis. Data Sources: MEDLINE, Embase, Cochrane Library Central Register of Controlled Trials, and published meta-analyses from inception through October 11, 2017...
April 17, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29677206/synergistic-interaction-between-a-pde5-inhibitor-sildenafil-and-a-new-adenosine-a2a-receptor-agonist-lassbio-1359-improves-pulmonary-hypertension-in-rats
#3
Allan K Alencar, Fábio I Carvalho, Ananssa M Silva, Sabrina T Martinez, Jorge A Calasans-Maia, Carlos M Fraga, Eliezer J Barreiro, Gisele Zapata-Sudo, Roberto T Sudo
INTRODUCTION: Pulmonary hypertension (PH) is characterized by enhanced pulmonary vascular resistance, which causes right ventricle (RV) pressure overload and results in right sided heart failure and death. This work investigated the effectiveness of a combined therapy with PDE5 inhibitor (PDE5i) and a new adenosine A2A receptor (A2AR) agonist in mitigating monocrotaline (MCT) induced PH in rats. METHODS: An in vitro isobolographic analysis was performed to identify possible synergistic relaxation effect between sildenafil and LASSBio 1359 in rat pulmonary arteries (PAs)...
2018: PloS One
https://www.readbyqxmd.com/read/29677019/mu-opioid-receptors-in-nociceptive-afferents-produce-a-sustained-suppression-of-hyperalgesia-in-chronic-pain
#4
Amie Severino, Wenling Chen, Joshua K Hakimian, Brigitte L Kieffer, Claire Gaveriaux-Ruff, Wendy Walwyn, Juan Carlos Marvizon
The latent sensitization model of chronic pain reveals that recovery from some types of long-term hyperalgesia is an altered state in which nociceptive sensitization persists but is suppressed by the ongoing activity of analgesic receptors such as µ-opioid receptors (MORs). To determine whether these MORs are the ones present in nociceptive afferents, we bred mice expressing Cre-recombinase under the Nav1.8 channel promoter (Nav1.8cre) with MOR-floxed mice (flMOR). These Nav1.8cre/flMOR mice had reduced MOR expression in primary afferents, as revealed by quantitative PCR, in situ hybridization and immunofluorescence colocalization with the neuropeptide CGRP...
April 17, 2018: Pain
https://www.readbyqxmd.com/read/29676804/the-biphasic-effect-of-extracellular-glucose-concentration-on-carbachol-induced-fluid-secretion-from-mouse-submandibular-glands
#5
Momomi Terachi, Chikara Hirono, Michinori Kitagawa, Makoto Sugita
Cholinergic agonists evoke elevations of the cytoplasmic free-calcium concentration ([Ca2+ ]i ) to stimulate fluid secretion in salivary glands. Salivary flow rates are significantly reduced in diabetic patients. However, it remains elusive how salivary secretion is impaired in diabetes. Here, we used an ex vivo submandibular gland perfusion technique to characterize the dependency of salivary flow rates on extracellular glucose concentration and activities of glucose transporters expressed in the glands. The cholinergic agonist carbachol (CCh) induced sustained fluid secretion, the rates of which were modulated by the extracellular glucose concentration in a biphasic manner...
April 20, 2018: European Journal of Oral Sciences
https://www.readbyqxmd.com/read/29676616/laboratory-practical-to-study-the-differential-innervation-pathways-of-urinary-tract-smooth-muscle
#6
Benjamin E Rembetski, Caroline A Cobine, Bernard T Drumm
In the mammalian lower urinary tract, there is a reciprocal relationship between the contractile state of the bladder and urethra. As the bladder fills with urine, it remains relaxed to accommodate increases in volume, while the urethra remains contracted to prevent leakage of urine from the bladder to the exterior. Disruptions to the normal contractile state of the bladder and urethra can lead to abnormal micturition patterns and urinary incontinence. While both the bladder and urethra are smooth-muscle organs, they are differentially contracted by input from cholinergic and sympathetic nerves, respectively...
June 1, 2018: Advances in Physiology Education
https://www.readbyqxmd.com/read/29676521/inhibitory-regulation-of-skin-fibrosis-in-systemic-sclerosis-by-apelin-apj-signaling
#7
Yoko Yokoyama, Akiko Sekiguchi, Chisako Fujiwara, Akihiko Uchiyama, Akihito Uehara, Sachiko Ogino, Ryoko Torii, Osamu Ishikawa, Sei-Ichiro Motegi
OBJECTIVE: Apelin/APJ signaling has been identified to regulate cardiac and arterial fibrosis and involved in the pathogenesis of pulmonary arterial hypertension. Objective was to elucidate the role of apelin in skin fibrosis in systemic sclerosis (SSc). METHODS: Expressions of apelin/APJ in normal and SSc fibroblasts were compared. Effects of siRNA depletion and the addition of apelin in fibroblasts were analyzed. Effect of apelin injections on bleomycin-induced dermal fibrosis in mice was investigated...
April 20, 2018: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/29675956/clonidine-modulates-the-activity-of-the-subthalamic-supplementary-motor-loop-evidence-from-a-pharmacological-study-combining-dbs-and-eeg-recordings-in-parkinsonian-patients
#8
Charlotte Spay, Marion Albares, Guillaume Lio, Stephane Thobois, Emmanuel Broussolle, Brian Lau, Benedicte Ballanger, Philippe Boulinguez
Clonidine is an anti-hypertensive medication which acts as an alpha-adrenergic receptors agonist. As the noradrenergic system is likely to support cognitive functions including attention and executive control, other clinical uses of clonidine have recently gained popularity for the treatment of neuropsychiatric disorders like attention-deficit hyperactivity disorder or Tourette syndrome, but the mechanism of action is still unclear. Here, we test the hypothesis that the noradrenergic system regulates the activity of subthalamo-motor cortical loops, and that this influence can be modulated by clonidine...
April 20, 2018: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29675928/differential-cardiac-sympatho-inhibitory-responses-produced-by-the-agonists-b-ht-933-quinpirole-and-immepip-in-normoglycemic-and-diabetic-pithed-rats
#9
Eduardo Rivera-Mancilla, Alain H Altamirano-Espinoza, Guadalupe Manrique-Maldonado, Belinda Villanueva-Castillo, Carlos M Villalón
This study compared the cardiac sympatho-inhibitory responses produced by agonists at α2 -adrenergic (B-HT 933), dopamine D2 -like (quinpirole) and histamine H3 /H4 (immepip) receptors between normoglycemic and streptozotocin-pretreated (diabetic) pithed rats. Intravenous (i.v.) continuous infusions of B-HT 933, quinpirole or immepip were used in normoglycemic and diabetic pithed rats to analyse their sympatho-inhibitory effects on the electrically-stimulated cardioaccelerator sympathetic outflow. Both in normoglycemic and diabetic animals, B-HT 933 (until 100 μg/kg...
April 19, 2018: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/29675927/tributyltin-reduces-the-levels-of-serum-adiponectin-and-activity-of-akt-and-induces-metabolic-syndrome-in-male-mice
#10
Haotian Yan, Hao Guo, Dong Cheng, Ruirui Kou, Cuili Zhang, Jiliang Si
Tributyltin (TBT), a proven environmental obesogen, functions as a nanomolar agonist of the peroxisome proliferator activated receptor-γ (PPARγ). However, the adverse effects of TBT on metabolism are incompletely understood. In this study, male ICR mice were administered TBT (5 and 50 μg·kg- 1 ) by an intraperitoneal injection once every 3 days for 30 days from 28 days of age and bred for another 30 days after the last administration of TBT. We analyzed the effects of these exposures on the fat depot weights, serum lipid profile, serum leptin and adiponectin, hepatic lipid accumulation, and activity of AKT in the liver and skeletal muscle isolated from mice 8 mins after receiving an insulin injection...
April 20, 2018: Environmental Toxicology
https://www.readbyqxmd.com/read/29675893/characteristics-of-opioid-maintained-clients-smoking-fentanyl-patches-the-importance-of-confirmatory-drug-analysis-illustrated-by-a-case-series-and-mini-review
#11
Andreas Kimergård, Jacklyn Dunne, Anette Bøgen, Peter Hindersson, Torben Breindahl
The increase in opioid prescribing in many European countries over the last decade has raised concerns about associated diversion, overdose and mortality. Fentanyl is one of these synthetic opioids that is typically prescribed as a transdermal patch for pain that requires continuous pain relief and has been the focus of investigations due to reports of overdose and death. We report a case series of 14 drug addiction treatment entrants who entered treatment in one service located in the region of Southern Denmark from August 2015 to December 2015 for smoking fentanyl patches...
April 19, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29675856/adreno-muscarinic-synergy-in-the-male-human-urinary-outflow-tract
#12
Sebastian Walther, Frank Strittmatter, Martin Hennenberg, Christian Gratzke, Christian G Stief, Alexander Roosen
AIM: To examine putative interaction between adrenergic and muscarinic contractile activation in the human urinary outflow tract. METHODS: Tissue from the trigone and prostatic urethra was obtained from 12 cystectomy and 16 prostatectomy specimen. Contractions were elicited by exposure to exogenous agonists before and after inhibition of Rho kinase and protein kinase c (PKC). Immunofluorescence and Western-blot studies were performed using antibodies to muscarinic M3-receptors (M3-R) and alpha1A-adrenoreceptors (alpha1A-AR)...
April 20, 2018: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/29675798/a-systematic-literature-review-and-network-meta-analysis-comparing-once-weekly-semaglutide-with-other-glp-1-receptor-agonists-in-patients-with-type-2-diabetes-previously-receiving-1-2-oral-anti-diabetic-drugs
#13
Michal Witkowski, Lars Wilkinson, Neil Webb, Alan Weids, Divina Glah, Hrvoje Vrazic
INTRODUCTION: Once-weekly semaglutide is a new glucagon-like peptide-1 (GLP-1) analogue administered at a 1.0 or 0.5 mg dose. As head-to-head trials assessing once-weekly semaglutide as an add-on to 1-2 oral anti-diabetic drugs (OADs) vs other GLP-1 receptor agonists (GLP-1 RAs) are limited, a network meta-analysis (NMA) was performed. The objective was to assess the relative efficacy and safety of once-weekly semaglutide vs GLP-1 RAs in patients with type 2 diabetes (T2D) inadequately controlled on 1-2 OADs...
April 19, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/29675797/treatment-intensification-in-type-2-diabetes-a-real-world-study-of-2-oad-regimens-glp-1-ras-or-basal-insulin
#14
Lawrence Blonde, Denis Raccah, Elisheva Lew, Juliana Meyers, Elena Nikonova, Mayank Ajmera, Keith L Davis, Monica Bertolini, Bruno Guerci
INTRODUCTION: Treatment guidelines recommend a stepwise approach to glycemia management in patients with type 2 diabetes (T2D), but this may result in uncontrolled glycated hemoglobin A1c (HbA1c) between steps. This retrospective analysis compared clinical and economic outcomes among patients with uncontrolled T2D initiating two oral antidiabetes drugs (OADs), glucagon-like peptide-1 receptor agonists (GLP-1 RAs), or basal insulin in a real-world setting. METHODS: Adults with T2D on OAD monotherapy were identified in the MarketScan claims database (2007-2014)...
April 19, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/29675711/%C3%AE-2-adrenoceptor-signaling-reduction-is-involved-in-the-inflammatory-response-of-fibroblast-like-synoviocytes-from-adjuvant-induced-arthritic-rats
#15
Huaxun Wu, Jingyu Chen, Chun Wang, Lihua Liu, Yujing Wu, Yunfang Zhang, Aiwu Zhou, Lingling Zhang, Wei Wei
OBJECTIVE: To investigate the effects of β-AR signaling on fibroblast-like synoviocytes (FLS) from adjuvant-induced arthritis (AA) rats and the partial mechanisms focused on β-AR desensitization mediated by GRK2 and β-arrestin2. METHODS: Animals were divided into a control group and an AA model group, and FLSs were cultured. Arthritis index, histopathology of joints, epinephrine (Epi) and norepinephrine (NE) were detected in vivo. The effect of the β-AR agonist isoprenaline (ISO) and the β2 -AR agonist salbutamol on FLS cell viability were detected by CCK8...
April 19, 2018: Inflammopharmacology
https://www.readbyqxmd.com/read/29675582/multifunctional-opioid-ligands
#16
Jessica P Anand, Deanna Montgomery
The opioid receptor system plays a major role in the regulation of mood, reward, and pain. The opioid receptors therefore make attractive targets for the treatment of many different conditions, including pain, depression, and addiction. However, stimulation or blockade of any one opioid receptor type often leads to on-target adverse effects that limit the clinical utility of a selective opioid agonist or antagonist. Literature precedent suggests that the opioid receptors do not act in isolation and that interactions among the opioid receptors and between the opioid receptors and other proteins may produce clinically useful targets...
April 20, 2018: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/29675488/trans-dermal-estrogen-oestrogel-for-endometrial-preparation-in-freeze-embryo-transfer-cycle-an-rct
#17
Ensieh Shahrokh Tehraninejad, Roya Kabodmehri, Batol Hosein Rashidi, Mina Jafarabadi, Fateme Keikha, Masomeh Masomi, Fedieh Hagholahi
Background: Estrogen and progesterone are two crucial factors for endometrial preparation in frozen embryo transfer (FET) cycles. Studies assessing different forms of estradiol in FET have published already but literature lacks enough surveys on transdermal estrogen application in reproductive medicine. Objective: To investigate the effects of trans dermal estrogen (Oestrogel) on pregnancy rates in patients that candidate for FET cycle. Materials and Methods: In this randomized clinical trial, 100 women undergoing FET cycles referred to Imam Khomeeini Hospital were enrolled in two groups, randomly...
January 2018: International Journal of Reproductive Biomedicine (Yazd, Iran)
https://www.readbyqxmd.com/read/29675483/fresh-versus-frozen-embryo-transfer-after-gonadotropin-releasing-hormone-agonist-trigger-in-gonadotropin-releasing-hormone-antagonist-cycles-among-high-responder-women-a-randomized-multi-center-study
#18
Abbas Aflatoonian, Mahnaz Mansoori-Torshizi, Maryam Farid Mojtahedi, Behrouz Aflatoonian, Mohammaad Ali Khalili, Mohammad Hossein Amir-Arjmand, Mehrdad Soleimani, Nastaran Aflatoonian, Homa Oskouian, Nasim Tabibnejad, Peter Humaidan
Background: The use of embryo cryopreservation excludes the possible detrimental effects of ovarian stimulation on the endometrium, and higher reproductive outcomes following this policy have been reported. Moreover, gonadotropin-releasing hormone agonist trigger in gonadotropin-releasing hormone (GnRH) antagonist cycles as a substitute for standard human chorionic gonadotropin trigger, minimizes the risk of ovarian hyperstimulation syndrome (OHSS) in fresh as well as frozen embryo transfer cycles (FET)...
January 2018: International Journal of Reproductive Biomedicine (Yazd, Iran)
https://www.readbyqxmd.com/read/29675448/intestinal-farnesoid-x-receptor-activation-by-pharmacologic-inhibition-of-the-organic-solute-transporter-%C3%AE-%C3%AE
#19
Sandra M W van de Wiel, D Rudi de Waart, Ronald P J Oude Elferink, Stan F J van de Graaf
Background & Aims: The organic solute transporter α-β (OSTα-OSTβ) mainly facilitates transport of bile acids across the basolateral membrane of ileal enterocytes. Therefore, inhibition of OSTα-OSTβ might have similar beneficial metabolic effects as intestine-specific agonists of the major nuclear receptor for bile acids, the farnesoid X receptor (FXR). However, no OSTα-OSTβ inhibitors have yet been identified. Methods: Here, we developed a screen to identify specific inhibitors of OSTα-OSTβ using a genetically encoded Förster Resonance Energy Transfer (FRET)-bile acid sensor that enables rapid visualization of bile acid efflux in living cells...
March 2018: Cellular and Molecular Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/29675368/mincle-in-the-innate-immune-response-of-mice-fungal-keratitis
#20
Guo-Rong Yu, Jing Lin, Jie Zhang, Cheng-Ye Che, Xu-Dong Peng, Cui Li, Li-Ting Hu, Guo-Qiang Zhu, Kun He, Gui-Qiu Zhao
AIM: To investigate how macrophage inducible C-type lectin (Mincle) influences inflammation in mice fungal keratitis induced by Aspergillus fumigatus ( A. fumigatus ). METHODS: C57BL/6 mice were infected with A. fumigatus after pretreated with Mincle agonist TDB or Mincle neutralizing antibody (MincleAb), taking DMSO or IgG as control group respectively. The cornea lesions were monitored with slit-lamp microscope and evaluated by clinical score. Mincle expression was assessed using reverse transcription-ploymerase chain reaction (RT-PCR) and immunostaining...
2018: International Journal of Ophthalmology
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