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https://www.readbyqxmd.com/read/29793210/polypharmacological-profile-of-1-2-dihydro-2-oxo-pyridine-3-carboxamides-in-the-endocannabinoid-system
#1
Andrea Chicca, Chiara Arena, Simone Bertini, Francesca Gado, Elena Ciaglia, Mario Abate, Maria Digiacomo, Margherita Lapillo, Giulio Poli, Maurizio Bifulco, Marco Macchia, Tiziano Tuccinardi, Jürg Gertsch, Clementina Manera
The endocannabinoid system (ECS) represents one of the major neuromodulatory systems involved in different physiological and pathological processes. Multi-target compounds exert their activities by acting via multiple mechanisms of action and represent a promising pharmacological modulation of the ECS. In this work we report 4-substituted and 4,5-disubstituted 1,2-dihydro-2-oxo-pyridine-3-carboxamide derivatives with a broad spectrum of affinity and functional activity towards both cannabinoid receptors and additional effects on the main components of the ECS...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793158/botulinum-toxin-type-a-affects-mechanics-of-non-injected-antagonistic-rat-muscles
#2
Filiz Ateş, Can A Yucesoy
Botulinum toxin type A (BTX-A) effects on the mechanics of non-injected antagonistic muscles are unknown. The aim was to test the following hypotheses in a rat model: BTX-A injected into gastrocnemius medialis (GM) and lateralis (GL) (1) decreases forces of the antagonistic tibialis anterior (TA) and extensor digitorum longus (EDL), (2) reduces length range of force exertion and (3) increases passive forces of the TA, and (4) changes inter-antagonistic and inter-synergistic epimuscular myofascial force transmission (EMFT)...
May 17, 2018: Journal of the Mechanical Behavior of Biomedical Materials
https://www.readbyqxmd.com/read/29792868/ah6809-decreases-production-of-inflammatory-mediators-by-pge-2-ep2-camp-signaling-pathway-in-an-experimentally-induced-pure-cerebral-concussion-in-rats
#3
Ping Li, Hongyan Jiang, Haiying Wu, Deye Wu, Hengxi Li, Jianyun Yu, Jianghua Lai
Increasing evidence suggests that PGE2 metabolic pathway is involved in pathological changes of the secondary brain injury after traumatic brain injury. However, the underlying mechanisms, in particular, the correlation between various key enzymes and the brain injury, has remained to be fully explored. More specifically, it remains to be ascertained whether AH6809 (an EP2 receptor antagonist) would interfere with the downstream of the PGE2 , regulate the inflammatory mediators and improve neuronal damage in the hippocampus by PGE2 - EP2 - cAMP signaling pathway...
May 21, 2018: Brain Research
https://www.readbyqxmd.com/read/29792867/effects-of-amphetamine-exposure-during-adolescence-on-behavior-and-prelimbic-cortex-neuron-activity-in-adulthood
#4
Luke K Sherrill, Joshua M Gulley
Repeated exposure to psychostimulants during adolescence produces long-lasting changes in behavior that may be mediated by disrupted development of the mesocorticolimbic dopamine system. Here, we tested this hypothesis by assessing the effects of amphetamine (AMPH) and dopamine receptor-selective drugs on behavior and neuron activity in the prelimbic region of the medial prefrontal cortex (PFC). Adolescent male, Sprague-Dawley rats were given saline or 3 mg/kg AMPH between postnatal day (P) 27 and P45. In Experiment 1, locomotor behavior was assessed during adulthood following challenges with a dopamine D1 (SKF 82958) or D2 (quinpirole) receptor-selective agonist...
May 21, 2018: Brain Research
https://www.readbyqxmd.com/read/29792859/long-non-coding-rna-miat-is-estrogen-responsive-and-promotes-estrogen-induced-proliferation-in-er-positive-breast-cancer-cells
#5
Yuehua Li, Baohong Jiang, Xiaoping Wu, Qin Huang, Wenqi Chen, Hongbo Zhu, Xiaofei Qu, Liming Xie, Xin Ma, Guo Huang
Estrogen drives the development and progression of estrogen receptor (ER)-positive breast cancer. However, the detailed mechanism underlying ER-driven carcinogenesis remains unclear despite extensive studies. Previously reports indicated higher expression of long non-coding RNA (lncRNA) myocardial infarction associated transcript (MIAT) in ER-positive breast cancer tissues than in ER-negative tissues. However, the functional relevance of MIAT in ER-positive breast cancer tumorigenesis was poorly understood...
May 21, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29792846/adenosine-receptor-distribution-in-rhesus-monkey-ocular-tissue
#6
Krista M Beach, Li-Fang Hung, Baskar Arumugam, Earl L Smith, Lisa A Ostrin
Adenosine receptor (ADOR) antagonists, such as 7-methylxanthine (7-MX), have been shown to slow myopia progression in humans and animal models. Adenosine receptors are found throughout the body, and regulate the release of neurotransmitters such as dopamine and glutamate. However, the role of adenosine in eye growth is unclear. Evidence suggests that 7-MX increases scleral collagen fibril diameter, hence preventing axial elongation. This study used immunohistochemistry (IHC) and reverse-transcription quantitative polymerase chain reaction (RT-qPCR) to examine the distribution of the four ADORs in the normal monkey eye to help elucidate potential mechanisms of action...
May 21, 2018: Experimental Eye Research
https://www.readbyqxmd.com/read/29792826/fast-evolving-human-specific-neural-enhancers-are-associated-with-aging-related-diseases
#7
Han Chen, Chunyan Li, Zhicheng Zhou, Han Liang
The antagonistic pleiotropy theory hypothesizes that evolutionary adaptations maximizing the fitness in early age increase disease burden after reproduction. This theory remains largely untested at the molecular level. Here, we analyzed enhancer evolution in primates to investigate the relationships between aging-related diseases and enhancers acquired after the human-chimpanzee divergence. We report a 5-fold increased evolutionary rate of enhancers that are activated in neural tissues, leading to fixation of ∼100 human-specific enhancers potentially under adaptation...
May 23, 2018: Cell Systems
https://www.readbyqxmd.com/read/29792714/docking-screens-for-dual-inhibitors-of-disparate-drug-targets-for-parkinson-s-disease
#8
Mariama Jaiteh, Alexey Zeifman, Marcus Saarinen, Per Svenningsson, José M Brea, Maria Isabel Loza, Jens Carlsson
Modulation of multiple biological targets with a single drug can lead to synergistic therapeutic effects and has been demonstrated to be essential for efficient treatment of CNS disorders. However, rational design of compounds that interact with several targets is very challenging. Here, we demonstrate that structure-based virtual screening can guide the discovery of multi-target ligands of unrelated proteins relevant for Parkinson's disease. A library with 5.4 million molecules was docked to crystal structures of the A2A adenosine receptor (A2AAR) and monoamine oxidase B (MAO-B)...
May 24, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29792524/managing-comorbid-cardiovascular-disease-and-sleep-apnea-with-pharmacotherapy
#9
Jacek Wolf, Krzysztof Narkiewicz
Highly prevalent sleep disordered breathing (SDB) has been recognized as an independent cardiovascular disease (CVD) risk factor. Although these two entities often coexist, there is a shortage of sufficiently-powered studies testing the interplay between the course of sleep apnea and CVD pharmacotherapy. The mutual relationship between treated/untreated obstructive sleep apnea (OSA) with ongoing cardiovascular pharmacotherapies is an evident gap in clinical expertise. Areas covered: In this article, the authors review the available evidence and outline future research directions concerning the reciprocal relationship between the pharmacological treatment of CVD and SDB...
May 24, 2018: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29792395/how-are-patients-with-heart-failure-treated-in-primary-care
#10
Hélène Vaillant-Roussel, Bruno Pereira, Sylvaine Gibot-Boeuf, Romain Eschalier, Claude Dubray, Rémy Boussageon, Philippe Vorilhon
OBJECTIVE: The aim of this study was to assess the adherence of general practitioners (GPs) to guidelines in patients with heart failure with reduced ejection fraction (HFrEF) and to describe GPs' prescribing behavior regarding patients with heart failure with preserved ejection fraction (HFpEF). MATERIALS AND METHODS: Cross-sectional study as part of the ETIC trial. Five classes of drugs were described: angiotensin-converting enzyme inhibitors (ACEIs) or angiotensin receptor blockers (ARBs); β-blockers (BBs); mineralocorticoid receptor antagonists (MRAs); diuretics (thiazide or loop diuretics); and digoxin...
May 24, 2018: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29792186/involvement-of-the-cb-2-cannabinoid-receptor-in-cell-growth-inhibition-and-g0-g1-cell-cycle-arrest-via-the-cannabinoid-agonist-win-55-212-2-in-renal-cell-carcinoma
#11
Mohammed I Khan, Anna A Sobocińska, Klaudia K Brodaczewska, Katarzyna Zielniok, Malgorzata Gajewska, Claudine Kieda, Anna M Czarnecka, Cezary Szczylik
BACKGROUND: The anti-tumor properties of cannabinoids have been investigated in many in vitro and in vivo studies. Many of these anti-tumor effects are mediated via cannabinoid receptor types 1 and 2 (CB1 and CB2 ), comprising the endocannabinoid system (ECS). In this study, we investigated the ECS based on CB 1 and CB 2 receptor gene and protein expression in renal cell carcinoma (RCC) cell lines. In view of their further use for potential treatments, we thus investigated the roles of CB1 and CB2 receptors in the anti-proliferative action and signal transduction triggered by synthetic cannabinoid agonists [such as JWH-133 and WIN 55,212-2 (WIN-55)] in RCC cell lines...
May 23, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29792150/synthesis-and-biological-evaluation-of-novel-2-3-disubstituted-benzofuran-analogues-of-gaba-as-neurotropic-agents
#12
Arturo Coaviche-Yoval, Hector Luna, Ricardo Tovar-Miranda, Marvin Antonio Soriano-Ursua, Jose G Trujillo-Ferrara
BACKGROUND: Benzofurans are heterocyclic compounds with neurotropic activity. Some have been developed for the treatment of acute and degenerative neuronal injuries. OBJECTIVE: To evaluate the in silico binding of some promising benzofurans on the GABA receptors, and the in vivo neurotropic activity of benzofuran analogues (BZF 6-10) of gamma-aminobutyric acid (GABA) on a seizure model. METHODS: The ligands with the best physicochemical attributes were docked on two GABA receptors (the alpha-1 subunit of GABAA-R and GBR1 subunit of GABAB-R)...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29791808/pseudomonads-contribute-to-regulation-of-i-pratylenchus-penetrans-i-nematoda-populations-on-apple
#13
Tristan T Watson, Tom A Forge, Louise M Nelson
Inoculation with antagonistic soil microorganisms has shown potential to suppress replant disease of apple in orchard soils. <i>Pseudomonas</i> spp. may have potential to reduce <i>Pratylenchus penetrans</i> populations on apple. <i>Pseudomonas</i> spp. were isolated from the rhizosphere of sweet cherry, screened for antagonistic characteristics, and two highly antagonistic <i>Pseudomonas</i> isolates, P10-32 and P10-42, were evaluated for growth promotion of apple seedlings, suppression of <i>P...
May 23, 2018: Canadian Journal of Microbiology
https://www.readbyqxmd.com/read/29791207/activation-of-trpv4-stimulates-transepithelial-ion-flux-in-a-porcine-choroid-plexus-cell-line
#14
Daniel Preston, Stefanie Simpson, Dan Halm, Alexandra Hochstetler, Christian Schwerk, Horst Schroten, Bonnie L Blazer-Yost
The choroid plexus (CP) epithelium plays a major role in the production of cerebrospinal fluid (CSF). A polarized cell line, the porcine choroid plexus - Riems (PCP-R) line, that exhibits many of the characteristics of the native epithelium, was used to study the effect of activation of the transient receptor potential vanilloid 4 (TRPV4) cation channel found in the PCP-R cells as well as in the native epithelium. Ussing-style electrophysiological experiments showed that activation of TRPV4 with a specific agonist, GSK 1016790A, resulted in an immediate increase in both transepithelial ion flux and conductance...
May 23, 2018: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/29791013/frontline-science-buprenorphine-decreases-ccl2-mediated-migration-of-cd14-cd16-monocytes
#15
Matias Jaureguiberry-Bravo, Lillie Lopez, Joan W Berman
HIV infection of the CNS causes neuroinflammation and damage that contributes to the development of HIV-associated neurocognitive disorders (HAND) in greater than 50% of HIV-infected individuals, despite antiretroviral therapy (ART). Opioid abuse is a major risk factor for HIV infection. It has been shown that opioids can contribute to increased HIV CNS pathogenesis, in part, by modulating the function of immune cells. HIV enters the CNS within two weeks after peripheral infection by transmigration of infected monocytes across the blood brain barrier (BBB)...
May 23, 2018: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/29790837/modulation-of-spinal-motor-networks-by-astrocyte-derived-adenosine-is-dependent-on-d1-like-dopamine-receptor-signalling
#16
David Acton, Matthew J Broadhead, Gareth Brian Miles
Astrocytes modulate many neuronal networks, including spinal networks responsible for the generation of locomotor behaviour. Astrocytic modulation of spinal motor circuits involves release of ATP from astrocytes, hydrolysation of ATP to adenosine, and subsequent activation of neuronal A1 adenosine receptors (A1Rs). The net effect of this pathway is a reduction in the frequency of locomotor-related activity. Recently, it was proposed that A1Rs modulate burst frequency by blocking the D1-like dopamine receptor (D1LR) signalling pathway; however, adenosine also modulates ventral horn circuits by dopamine-independent pathways...
May 23, 2018: Journal of Neurophysiology
https://www.readbyqxmd.com/read/29790836/minocycline-promotes-post-hemorrhagic-neurogenesis-via-m2-microglia-polarization-via-up-regulation-of-the-trkb-bdnf-pathway-in-rats
#17
Miao Hongsheng, Runming Li, Cong Han, Xiuzhen Lu, Hang Zhang
Intracerebral hemorrhage (ICH) is a devastating disease worldwide with increasing mortality. The present study investigated whether minocycline was neuroprotective and induced M2 microglial polarization via up-regulation of the TrkB/BDNF pathway after ICH. ICH was induced via injection of autologous blood into 150 Sprague-Dawley (S-D) rats. A selective TrkB antagonist (ANA 12) and agonist (HIOC) were used to investigate the mechanism of minocycline-induced neuroprotection. Minocycline improved ICH-induced neurological deficits and reduced M1 microglia marker protein (CD68, CD16) expression as well as M2 microglial polarization (CD206 and arginase 1 protein)...
May 23, 2018: Journal of Neurophysiology
https://www.readbyqxmd.com/read/29790666/rolapitant-for-the-prevention-of-nausea-in-patients-receiving-highly-or-moderately-emetogenic-chemotherapy
#18
Rudolph M Navari, Bernardo L Rapoport, Dan Powers, Sujata Arora, Rebecca Clark-Snow
Most patients receiving highly or moderately emetogenic chemotherapy experience chemotherapy-induced nausea and vomiting without antiemetic prophylaxis. While neurokinin-1 receptor antagonists (NK-1RAs) effectively prevent emesis, their ability to prevent nausea has not been established. We evaluated the efficacy of the long-acting NK-1RA rolapitant in preventing chemotherapy-induced nausea using post hoc analyses of data from 3 phase 3 trials. Patients were randomized to receive 180 mg oral rolapitant or placebo approximately 1-2 hours before chemotherapy in combination with a 5-hydroxytryptamine type 3 RA and dexamethasone...
May 23, 2018: Cancer Medicine
https://www.readbyqxmd.com/read/29790645/fibrinogen-prothrombin-time-derived-method-is-not-useful-in-patients-anticoagulated-with-low-molecular-weight-heparins-or-rivaroxaban
#19
C Duboscq, M Martinuzzo, J M Ceresetto, M Lopez, L Barrera, J Oyhamburu, G Stemmelin
BACKGROUND: Fibrinogen prothrombin time derived method (FIBPT-d) with photo-optical coagulometers is easy and economical. However, there are few reports on the behavior of this test on samples from patients anticoagulated with direct oral anticoagulants (DOACs) or low molecular weight heparin (LMWH). OBJECTIVE: To compare fibrinogen results obtained by Clauss method (FIB C) and FIBPT-d with two thromboplastins in anticoagulated patients. POPULATION: 295 consecutive anticoagulated patients: 99 vitamin K antagonist (VKA), 49 unfractionated heparin (UFH), 47 LMWH, 50 rivaroxaban and 50 dabigatran; and 100 healthy controls (NC)...
May 23, 2018: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/29790626/sphingosine-1-phosphate-promotes-the-proliferation-and-attenuates-apoptosis-of-endothelial-progenitor-cells-via-s1pr1-s1pr3-pi3k-akt-pathway
#20
Hang Wang, Hao Huang, Shi-Fang Ding
Sphingosine-1-phosphate (S1P) is a bioactive lysophospholipid that involves in numerous pathophysiological processes. Endothelial progenitor cells (EPCs) play a crucial role in endothelial repair and tumor angiogenesis. The aim of study was to determine the effects of S1P on proliferation and anti-apoptosis of EPCs and their signaling pathways. In this study, we showed that S1P, SEW2871 (a selective S1P receptor 1 (S1PR1) agonist ), or CYM5541 (a selective S1P receptor 3 (S1PR3) allosteric agonist promotes the proliferation and attenuates apoptosis of bone marrow (BM)-derived EPCs...
May 23, 2018: Cell Biology International
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