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https://www.readbyqxmd.com/read/29352769/resolvin-e1-resolvin-d1-and-resolvin-d2-inhibit-constriction-of-rat-thoracic-aorta-and-human-pulmonary-artery-induced-by-the-thromboxane-mimetic-u46619
#1
Melanie Jannaway, Christopher Torrens, Jane A Warner, Anthony P Sampson
BACKGROUND AND PURPOSE: Omega-6 fatty acid-derived lipid mediators such as prostanoids, thromboxane and leukotrienes have well-established roles in regulating both inflammation and smooth muscle contractility. Resolvins are derived from omega-3 fatty acids and have important roles in promoting the resolution of inflammation, but their activity on smooth muscle contractility is unknown. We investigated whether resolvin E1 (RvE1), resolvin D1 (RvD1) and resolvin D2 (RvD2) can modulate contractions of isolated segments of rat thoracic aorta (RTA) or human pulmonary artery (HPA) induced by the α1 -adrenoceptor agonist phenylephrine or the stable thromboxane A2 mimetic U46619...
January 20, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29352512/trpv1-antagonists-that-cause-hypothermia-instead-of-hyperthermia-in-rodents-compounds-pharmacological-profiles-in-vivo-targets-thermoeffectors-recruited-and-implications-for-drug-development
#2
Andras Garami, Eszter Pakai, Heath A McDonald, Regina M Reilly, Arthur Gomtsyan, Joshua J Corrigan, Erika Pinter, Dawn X D Zhu, Sonya G Lehto, Narender R Gavva, Philip R Kym, Andrej A Romanovsky
AIM: Thermoregulatory side effects hinder the development of transient receptor potential vanilloid-1 (TRPV1) antagonists as new painkillers. While many antagonists cause hyperthermia, a well-studied effect, some cause hypothermia. The mechanisms of this hypothermia are unknown and were studied herein. METHODS: Two hypothermia-inducing TRPV1 antagonists, the newly synthesized A-1165901 and the known AMG7905, were used in physiological experiments in rats and mice...
January 20, 2018: Acta Physiologica
https://www.readbyqxmd.com/read/29352503/in-vivo-effects-of-%C3%AE-opioid-receptor-agonist-%C3%AE-opioid-receptor-antagonist-peptidomimetics-following-acute-and-repeated-administration
#3
Jessica P Anand, Kelsey E Kochan, Anthony F Nastase, Deanna Montgomery, Nicholas W Griggs, John R Traynor, Henry I Mosberg, Emily M Jutkiewicz
BACKGROUND AND PURPOSE: Mu opioid receptor (μ-receptor) agonists are used for pain management, but produce adverse effects including tolerance, dependence, and euphoria. The co-administration of a μ-receptor agonist with a delta opioid receptor (δ-receptor) antagonist has been shown to produce antinociception with reduced development of some side effects. We characterized the effects of three μ-receptor agonist/δ-receptor antagonist peptidomimetics in vivo after acute and repeated administration to determine if this profile provides a viable alternative to traditional opioid analgesics...
January 19, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29352428/hnf4%C3%AE-is-involved-in-the-regulation-of-vertebrate-lc-pufa-biosynthesis-insights-into-the-regulatory-role-of-hnf4%C3%AE-on-expression-of-liver-fatty-acyl-desaturases-in-the-marine-teleost-siganus-canaliculatus
#4
Shuqi Wang, Junliang Chen, Danli Jiang, Qinghao Zhang, Cuihong You, Douglas R Tocher, Óscar Monroig, Yewei Dong, Yuanyou Li
Long-chain polyunsaturated fatty acid (LC-PUFA) biosynthesis is an important metabolic pathway in vertebrates, especially fish, considering they are the major source of n-3 LC-PUFA in the human diet. However, most fish have only limited capability for biosynthesis of LC-PUFA. The rabbitfish (Siganus canaliculatus) is able to synthesize LC-PUFA as it has all the key enzyme activities required including Δ6Δ5 Fads2, Δ4 Fads2, Elovl5, and Elovl4. We previously reported a direct interaction between the transcription factor Hnf4α and the promoter regions of Δ4 and Δ6Δ5 Fads2, which suggested that Hnf4α was involved in the transcriptional regulation of fads2 in rabbitfish...
January 19, 2018: Fish Physiology and Biochemistry
https://www.readbyqxmd.com/read/29352328/attenuation-of-serotonin-induced-itch-by-sumatriptan-possible-involvement-of-endogenous-opioids
#5
Nazgol-Sadat Haddadi, Arash Foroutan, Saeed Shakiba, Khashayar Afshari, Sattar Ostadhadi, Maryam Daneshpazhooh, Ahmad-Reza Dehpour
Serotonin (5-hydroxytryptamine or 5-HT) is a neurotransmitter in itch and impaired serotonin signaling has been linked to a variety of itch conditions. Intradermal injection of 5-HT induces scratching behavior in mice through stimulation of 5-HT receptors. Previous studies have demonstrated that selective 5-HT1B/1D receptors agonists, including sumatriptan, inhibits neurotransmission. We have also reported that sumatriptan suppresses chloroquine-induced itch. Therefore, we investigated if sumatriptan has inhibitory effects on serotonin-induced itch in mice...
January 19, 2018: Archives of Dermatological Research
https://www.readbyqxmd.com/read/29352320/high-level-production-and-purification-in-a-functional-state-of-an-extrasynaptic-gamma-aminobutyric-acid-type-a-receptor-containing-%C3%AE-4%C3%AE-3%C3%AE-subunits
#6
Xiaojuan Zhou, Rooma Desai, Yinghui Zhang, Wojciech J Stec, Keith W Miller, Youssef Jounaidi
The inhibitory γ-aminobutyric acid type A receptors are implicated in numerous physiological processes, including cognition and inhibition of neurotransmission, rendering them important molecular targets for many classes of drugs. Functionally, the entire GABAAR family of receptors can be subdivided into phasic, fast acting synaptic receptors, composed of α-, β- and γ-subunits, and tonic extrasynaptic receptors, many of which contain the δ-subunit in addition to α- and β-subunits. Whereas the subunit arrangement of the former group is agreed upon, that of the αβδ GABAARs remains unresolved by electrophysiological and pharmacological research...
2018: PloS One
https://www.readbyqxmd.com/read/29352184/expression-and-relevance-of-the-g-protein-gated-k-channel-in-the-mouse-ventricle
#7
Allison Anderson, Kanchan Kulkarni, Ezequiel Marron Fernandez de Velasco, Nicholas Carlblom, Zhilian Xia, Atsushi Nakano, Kirill A Martemyanov, Elena G Tolkacheva, Kevin Wickman
The atrial G protein-gated inwardly rectifying K+ (GIRK) channel is a critical mediator of parasympathetic influence on cardiac physiology. Here, we probed the details and relevance of the GIRK channel in mouse ventricle. mRNAs for the atrial GIRK channel subunits (GIRK1, GIRK4), M2 muscarinic receptor (M2R), and RGS6, a negative regulator of atrial GIRK-dependent signaling, were detected in mouse ventricle at relatively low levels. The cholinergic agonist carbachol (CCh) activated small GIRK currents in adult wild-type ventricular myocytes that exhibited relatively slow kinetics and low CCh sensitivity; these currents were absent in ventricular myocytes from Girk1-/- or Girk4-/- mice...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29352161/the-action-of-a-negative-allosteric-modulator-at-the-dopamine-d2-receptor-is-dependent-upon-sodium-ions
#8
Christopher J Draper-Joyce, Ravi Kumar Verma, Mayako Michino, Jeremy Shonberg, Anitha Kopinathan, Carmen Klein Herenbrink, Peter J Scammells, Ben Capuano, Ara M Abramyan, David M Thal, Jonathan A Javitch, Arthur Christopoulos, Lei Shi, J Robert Lane
Sodium ions (Na+) allosterically modulate the binding of orthosteric agonists and antagonists to many class A G protein-coupled receptors, including the dopamine D2 receptor (D2R). Experimental and computational evidences have revealed that this effect is mediated by the binding of Na+ to a conserved site located beneath the orthosteric binding site (OBS). SB269652 acts as a negative allosteric modulator (NAM) of the D2R that adopts an extended bitopic pose, in which the tetrahydroisoquinoline moiety interacts with the OBS and the indole-2-carboxamide moiety occupies a secondary binding pocket (SBP)...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29352128/phosphorylation-of-the-transient-receptor-potential-ankyrin-1-by-cyclin-dependent-kinase-5-affects-chemo-nociception
#9
Bradford E Hall, Michaela Prochazkova, Matthew R Sapio, Paul Minetos, Natalya Kurochkina, B K Binukumar, Niranjana D Amin, Anita Terse, John Joseph, Stephen J Raithel, Andrew J Mannes, Harish C Pant, Man-Kyo Chung, Michael J Iadarola, Ashok B Kulkarni
Cyclin-dependent kinase 5 (Cdk5) is a key neuronal kinase that is upregulated during inflammation, and can subsequently modulate sensitivity to nociceptive stimuli. We conducted an in silico screen for Cdk5 phosphorylation sites within proteins whose expression was enriched in nociceptors and identified the chemo-responsive ion channel Transient Receptor Potential Ankyrin 1 (TRPA1) as a possible Cdk5 substrate. Immunoprecipitated full length TRPA1 was shown to be phosphorylated by Cdk5 and this interaction was blocked by TFP5, an inhibitor that prevents activation of Cdk5...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29352049/rev-erb-agonists-block-autophagy-in-cancer-cells
#10
(no author information available yet)
Disruption of the circadian clock components reduces cancer cell viability in vitro and in vivo.
January 19, 2018: Cancer Discovery
https://www.readbyqxmd.com/read/29352025/state-of-the-art-and-future-directions-for-extinction-as-a-translational-model-for-fear-and-anxiety
#11
REVIEW
Michelle G Craske, Dirk Hermans, Bram Vervliet
Through advances in both basic and clinical scientific research, Pavlovian fear conditioning and extinction have become an exemplary translational model for understanding and treating anxiety disorders. Discoveries in associative and neurobiological mechanisms underlying extinction have informed techniques for optimizing exposure therapy that enhance the formation of inhibitory associations and their consolidation and retrieval over time and context. Strategies that enhance formation include maximizing prediction-error correction by violating expectancies, deepened extinction, occasional reinforced extinction, attentional control and removal of safety signals/behaviours...
March 19, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29351922/activation-of-constitutive-androstane-receptor-ameliorates-renal-ischemia-reperfusion-induced-liver-and-kidney-injury
#12
You-Jin Choi, Dong Zhou, Anne Barbosa, Yongdong Niu, Xiudong Guan, Meishu Xu, Songrong Ren, Thomas Nolin, Yiuhua Liu, Wen Xie
Acute kidney injury (AKI) is associate with high mortality. Despite the evidence of AKI-induced distant organ injury, a relationship between AKI and liver injury has not been clearly established. The goal of this study is to investigate whether renal ischemia-reperfusion (IR) can affect liver pathophysiology. We showed that renal IR in mice induced fatty liver and compromised liver function through the down-regulation of constitutive androstane receptor (CAR; -90.4%) and inhibition of hepatic very low-density lipoprotein-triglyceride (VLDL-TG) secretion (-28...
January 19, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29351847/phosphorylation-of-ezh2-by-ampk-suppresses-prc2-methyltransferase-activity-and-oncogenic-function
#13
Lixin Wan, Kexin Xu, Yongkun Wei, Jinfang Zhang, Tao Han, Christopher Fry, Zhao Zhang, Yao Vickie Wang, Liyu Huang, Min Yuan, Weiya Xia, Wei-Chao Chang, Wen-Chien Huang, Chien-Liang Liu, Yuan-Ching Chang, Jinsong Liu, Yun Wu, Victor X Jin, Xiangpeng Dai, Jianfeng Guo, Jia Liu, Shulong Jiang, Jin Li, John M Asara, Myles Brown, Mien-Chie Hung, Wenyi Wei
Sustained energy starvation leads to activation of AMP-activated protein kinase (AMPK), which coordinates energy status with numerous cellular processes including metabolism, protein synthesis, and autophagy. Here, we report that AMPK phosphorylates the histone methyltransferase EZH2 at T311 to disrupt the interaction between EZH2 and SUZ12, another core component of the polycomb repressive complex 2 (PRC2), leading to attenuated PRC2-dependent methylation of histone H3 at Lys27. As such, PRC2 target genes, many of which are known tumor suppressors, were upregulated upon T311-EZH2 phosphorylation, which suppressed tumor cell growth both in cell culture and mouse xenografts...
January 18, 2018: Molecular Cell
https://www.readbyqxmd.com/read/29351550/differential-actions-of-ppar-%C3%AE-and-ppar-%C3%AE-%C3%AE-on-beige-adipocyte-formation-a-study-in-the-subcutaneous-white-adipose-tissue-of-obese-male-mice
#14
Tamiris Lima Rachid, Flavia Maria Silva-Veiga, Francielle Graus-Nunes, Isabele Bringhenti, Carlos Alberto Mandarim-de-Lacerda, Vanessa Souza-Mello
BACKGROUND AND AIMS: Obesity compromises adipocyte physiology. PPARs are essential to adipocyte plasticity, but its isolated role in the browning phenomenon is not clear. This study aimed to examine whether activation of PPAR-α or PPAR-β/δ could induce beige cell depots in the subcutaneous white adipose tissue of diet-induced obese mice. MATERIAL AND METHODS: Sixty animals were randomly assigned to receive a control diet (C, 10% lipids) or a high-fat diet (HF, 50% lipids) for ten weeks...
2018: PloS One
https://www.readbyqxmd.com/read/29351458/differences-in-l-type-calcium-channel-activity-partially-underlie-the-regional-dichotomy-in-pumping-behavior-by-murine-peripheral-and-visceral-lymphatic-vessels
#15
Scott D Zawieja, Jorge A Castorena-Gonzalez, Joshua Scallan, Michael J Davis
We identified a regional dichotomy in murine lymphatic contractile function with regard to vessel location within either the periphery or visceral cavity. All vessels isolated from peripheral regions; cervical, popliteal, inguinal, axillary, and inter-nodal inguinal axillary (Ing-Ax) developed robust contractions with maximal ejection fractions (EFs) of 50-80% in our ex vivo isobaric myograph experiments. Conversely, vessels isolated from the visceral cavity (mesenteric, TD, and iliac) demonstrated maximal EFs below 15%...
January 5, 2018: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/29351428/control-of-appetite-blood-glucose-and-blood-pressure-during-melanocortin-4-receptor-activation-in-normoglycemic-and-diabetic-npy-deficient-mice
#16
Alexandre A da Silva, John Nathan Freeman, John E Hall, Jussara M do Carmo
Although central melanocortin 4 receptor (MC4R) blockade abolishes the CNS-mediated anorexogenic, antidiabetic and cardiovascular actions of leptin, chronic MC4R stimulation fails to completely mimic leptin's effects. Because neuropeptide Y (NPY) and MC4R exert opposite effects on cardiovascular and metabolic functions, we tested its role in offsetting the long-term actions of MC4R activation. Wild-type (WT) and NPY-deficient (NPY-/-) mice were implanted with telemetry probes for measuring mean arterial pressure (MAP) and heart rate (HR) 24-h/d...
December 20, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/29351409/pharmacological-activation-of-ppar%C3%AE-inhibits-hypoxia-induced-proliferation-through-a-caveolin-1-targeted-and-dependent-mechanism-in-pasmcs
#17
Kai Yang, Mingming Zhao, Junyi Huang, Chenting Zhang, Qiu Yu Zheng, Yuqin Chen, Haiyang Jiang, Wenju Lu, Jian Wang
Previously, we and others have demonstrated that activation of peroxisome proliferator- activated receptor γ (PPARγ) by specific pharmacological agonists inhibits the pathogenesis of chronic hypoxia-induced pulmonary hypertension (CHPH) by suppressing the proliferation and migration in distal pulmonary arterial smooth muscle cells (PASMCs). Moreover, these beneficial effects of PPARγ are mediated by targeting the intracellular calcium homeostasis and store-operated calcium channel (SOCC) proteins, including the main caveolae component caveolin-1...
January 3, 2018: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/29351391/the-bile-acids-deoxycholic-acid-and-ursodeoxycholic-acid-regulate-colonic-epithelial-wound-healing
#18
Magdalena S Mroz, Natalia K Lajczak, Bridie J Goggins, Simon Keely, Stephen Joseph Keely
The intestinal epithelium constitutes an innate barrier which, upon injury, undergoes self-repair processes known as restitution. Although, bile acids are known as important regulators of epithelial function in health and disease, their effects on wound healing processes are not yet clear. Here we set out to investigate the effects of the colonic bile acids, deoxycholic acid (DCA) and ursodeoxycholic acid (UDCA) on epithelial restitution. Wound healing in T84 cell monolayers grown on transparent, permeable, supports was assessed over 48 hrs {plus minus} bile acids...
January 11, 2018: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/29351390/vagally-mediated-gastric-effects-of-brainstem-%C3%AE-2-adrenoceptor-activation-in-stressed-rats
#19
Yanyan Jiang, Kirsteen N Browning, Luca Toti, R Alberto Travagli
Chronic stress exerts vagally-dependent effects to disrupt gastric motility; previous studies have shown that, among other nuclei, A2 neurons are involved in mediating these effects. Several studies have also shown robust in vitro and in vivo effects of α2 adrenoceptor agonists on vagal motoneurons. We have demonstrated previously that brainstem vagal neurocircuits undergo remodeling following acute stress, however, the effects following brief periods of chronic stress have not been investigated. Our aim, therefore, was to test the hypothesis that different types of chronic stress influence gastric tone and motility by inducing plasticity in the response of vagal neurocircuits to α2 adrenoreceptor agonists...
January 11, 2018: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/29351171/spinal-pkc-erk-signal-pathway-mediates-hyperalgesia-priming
#20
Wei-Hsin Chen, Ya-Ting Chang, Yong-Cyuan Chen, Sin-Jhong Cheng, Chien-Chang Chen
Chronic pain can be initiated by one or more acute stimulations to sensitize neurons into the primed state. In the primed state, the basal nociceptive thresholds of the animal are normal, but in response to another hyperalgesic stimulus, the animal develops enhanced and prolonged hyperalgesia. The exact mechanism of how primed state is formed is not completely understood. Here we showed that spinal PKC/ERK signal pathway is required for neuronal plasticity change, hyperalgesic priming formation and the development of chronic hyperalgesia using acid-induced muscle pain (AIMP) model in mice...
January 18, 2018: Pain
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