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https://www.readbyqxmd.com/read/28710964/design-synthesis-and-biological-studies-of-a-library-of-nk1-receptor-ligands-based-on-a-5-arylthiosubstituted-2-amino-4-6-diaryl-3-cyano-4h-pyran-core-switch-from-antagonist-to-agonist-effect-by-chemical-modification
#1
Rocío Recio, Empar Vengut-Climent, Bernard Mouillac, Hélène Orcel, Miguel López-Lázaro, José Manuel Calderón-Montaño, Eleuterio Álvarez, Noureddine Khiar, Inmaculada Fernández
A library of 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyrans has been synthesized as a new family of non-peptide NK1 receptor ligands by a one-pot cascade process. Their biological effects via interaction with the NK1 receptor were experimentally determined as percentage of inhibition (for antagonists) and percentage of activation (for agonists), compared to the substance P (SP) effect, in IPone assay. A set of these amino compounds was found to inhibit the action of SP, and therefore can be considered as a new family of SP-antagonists...
June 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28701994/the-role-of-substance-p-in-secondary-pathophysiology-after-traumatic-brain-injury
#2
REVIEW
Robert Vink, Levon Gabrielian, Emma Thornton
It has recently been shown that substance P (SP) plays a major role in the secondary injury process following traumatic brain injury (TBI), particularly with respect to neuroinflammation, increased blood-brain barrier (BBB) permeability, and edema formation. Edema formation is associated with the development of increased intracranial pressure (ICP) that has been widely associated with increased mortality and morbidity after neurotrauma. However, a pharmacological intervention to specifically reduce ICP is yet to be developed, with current interventions limited to osmotic therapy rather than addressing the cause of increased ICP...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28699350/analgesic-properties-of-opioid-nk1-multitarget-ligands-with-distinct-in-vitro-profiles-in-naive-and-chronic-constriction-injury-cci-mice
#3
Joanna Starnowska, Roberto Costante, Karel Guillemyn, Katarzyna Popiolek-Barczyk, Nga N Chung, Carole Lemieux, Attila Keresztes, Joost Van Duppen, Adriano Mollica, John M Streicher, Jozef Vanden Broeck, Peter W Schiller, Dirk Tourwé, Joanna Mika, Steven Ballet, Barbara Przewlocka
The lower efficacy of opioids in neuropathic pain may be due to the increased activity of pronociceptive systems such as substance P. We present evidence to support this hypothesis in this work from the spinal cord in a neuropathic pain model in mice. Biochemical analysis confirmed the elevated mRNA and protein level of pronociceptive substance P, the major endogenous ligand of the neurokinin-1 (NK1) receptor, in the lumbar spinal cord of chronic constriction injury (CCI)-mice. To improve opioid efficacy in neuropathic pain, novel compounds containing opioid agonist and neurokinin 1 (NK1) receptor antagonist pharmacophores were designed...
July 12, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28698251/trpa1-mechanoreceptors-mediate-the-il-6-response-to-a-single-pd-dwell-in-the-rat
#4
Daniel Nilsson, Eva Jennische, Nicola Cavallini, Magnus Braide
BACKGROUND: The development of modern, biocompatible peritoneal dialysis (PD) fluids has not entirely eliminated the local pro-inflammatory effects of PD fluid administration. The present study was performed in order to establish the importance of known signaling pathways connected to mechano-, osmo- and chemo-sensors of the transient receptor potential (TRP) family for the acute inflammatory response to PD. METHODS: Rats were exposed to a single 4-hour dwell of lactate-buffered, 2...
July 11, 2017: Peritoneal Dialysis International: Journal of the International Society for Peritoneal Dialysis
https://www.readbyqxmd.com/read/28669862/spontaneous-and-bite-evoked-muscle-pain-are-mediated-by-a-common-nociceptive-pathway-with-differential-contribution-by-trpv1
#5
Sheng Wang, Jongseuk Lim, John Joseph, Sen Wang, Feng Wei, Jin Y Ro, Man-Kyo Chung
Spontaneous pain and function-associated pain are prevalent symptoms of multiple acute and chronic muscle pathologies. We established mouse models for evaluating spontaneous pain and bite-evoked pain from masseter muscle, and determined the roles of TRPV1 and the contribution of TRPV1- or NK1-dependent nociceptive pathways. Masseter muscle inflammation increased mouse grimace scale (MGS) scores and face wiping behavior which were attenuated by pharmacological or genetic inhibition of TRPV1. Masseter inflammation led to a significant reduction in bite force...
June 29, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28638718/substance-p-nk1-receptor-in-the-rat-corpus-callosum-during-postnatal-development
#6
Paolo Barbaresi, Emanuela Mensà, Guendalina Bastioli, Salvatore Amoroso
INTRODUCTION: The expression of substance P (SP) receptor (neurokinin 1, NK1) was studied in the rat corpus callosum (cc) from postnatal day 0 (the first 24 hr from birth, P0) to P30. METHODS: We used immunocytochemistry to study the presence of intracallosal NK1-immunopositive neurons (NK1IP-n) during cc development. RESULTS: NK1IP-n first appeared on P5. Their number increased significantly between P5 and P10, it remained almost constant between P10 and P15, then declined slightly until P30...
June 2017: Brain and Behavior
https://www.readbyqxmd.com/read/28620197/interleukin-28b-dampens-airway-inflammation-through-up-regulation-of-natural-killer-cell-derived-ifn-%C3%AE
#7
Bailing Yan, Feng Chen, Lijun Xu, Yanshi Wang, Xuefu Wang
Interleukin-28A (IL-28A) modulates CD11c+ dendritic cell (DC) function and promotes type 1T helper (Th1) differentiation, thus suppressing allergic airway diseases. However, the function of the IL-28A isoform IL-28B in these diseases remains largely unknown. In this study, we revealed a novel role of IL-28B in inducing type 1 immunity and protecting against ovalbumin (OVA)-induced allergic asthma in mice. IL-28B overexpression in wild-type mice promoted natural killer (NK) cell polarization in the lung, leading to the increased number of interferon (IFN)-γ-producing NK1 cells as well as Th1 differentiation...
June 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28606851/cardiorespiratory-action-of-opioid-tachykinin-agonist-peptide-hybrid-in-anaesthetized-rats-transduction-pathways
#8
Piotr Wojciechowski, Małgorzata Szereda-Przestaszewska, Andrzej Wojciech Lipkowski
AWL3106 composed of opioid (dermorphin) and tachykinin (substance P7-11) pharmacophores is a new compound with high analgesic potency and markedly reduced ability to induce tolerance and dependence. The present study aimed to determine the respiratory and cardiovascular responses evoked by this peptide in urethane-chloralose anaesthetized, spontaneously breathing rats in the presence or absence of vagal connection. Intravenous injection of AWL3106 at a dose of 0.3μmol/kg in intact rats resulted in apnoea lasting 5...
June 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28530714/cd8%C3%AE-%C3%AE-intraepithelial-lymphocytes-arise-from-two-main-thymic-precursors
#9
Roland Ruscher, Rebecca L Kummer, You Jeong Lee, Stephen C Jameson, Kristin A Hogquist
TCRαβ(+)CD4(-)CD8α(+)CD8β(-) intestinal intraepithelial lymphocytes (CD8αα IELs) are an abundant population of thymus-derived T cells that protect the gut barrier surface. We sought to better define the thymic IEL precursor (IELp) through analysis of its maturation, localization and emigration. We defined two precursor populations among TCRβ(+)CD4(-)CD8(-) thymocytes by dependence on the kinase TAK1 and rigorous lineage-exclusion criteria. Those IELp populations included a nascent PD-1(+) population and a T-bet(+) population that accumulated with age...
July 2017: Nature Immunology
https://www.readbyqxmd.com/read/28515228/nk1-1-cells-promote-sustained-tissue-injury-and-inflammation-after-trauma-with-hemorrhagic-shock
#10
Shuhua Chen, Rosemary A Hoffman, Melanie Scott, Joanna Manson, Patricia Loughran, Mostafa Ramadan, Anthony J Demetris, Timothy R Billiar
Various cell populations expressing NK1.1 contribute to innate host defense and systemic inflammatory responses, but their role in hemorrhagic shock and trauma remains uncertain. NK1.1(+) cells were depleted by i.p. administration of anti-NK1.1 (or isotype control) on two consecutive days, followed by hemorrhagic shock with resuscitation and peripheral tissue trauma (HS/T). The plasma levels of IL-6, MCP-1, alanine transaminase (ALT), and aspartate aminotransferase (AST) were measured at 6 and 24 h. Histology in liver and gut were examined at 6 and 24 h...
May 17, 2017: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/28501575/the-anti-asthmatic-drug-pranlukast-suppresses-the-delayed-phase-vomiting-and-reverses-intracellular-indices-of-emesis-evoked-by-cisplatin-in-the-least-shrew-cryptotis-parva
#11
Nissar A Darmani, Seetha Chebolu, Weixia Zhong, William D Kim, Matthew Narlesky, Joia Adams, Fanglong Dong
The introduction of second generation serotonin 5-HT3 receptor (5-HT3) antagonist palonosetron combined with long-acting substance P neurokinin NK1 receptor (NK1) antagonists (e.g. netupitant) has substantially improved antiemetic therapy against early- and delayed-phases of emesis caused by highly emetogenic chemotherapeutics such as cisplatin. However, the improved efficacy comes at a cost that many patients cannot afford. We introduce a new class of antiemetic, the antiasthmatic leukotriene CysLT1 receptor antagonist pranlukast for the suppression of cisplatin-evoked vomiting...
May 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28496413/cholera-toxin-induces-sustained-hyperexcitability-in-myenteric-but-not-submucosal-ah-neurons-in-guinea-pig-jejunum
#12
Katerina Koussoulas, Rachel M Gwynne, Jaime P P Foong, Joel C Bornstein
Background and Aims: Cholera toxin (CT)-induced hypersecretion requires activation of secretomotor pathways in the enteric nervous system (ENS). AH neurons, which have been identified as a population of intrinsic sensory neurons (ISNs), are a source of excitatory input to the secretomotor pathways. We therefore examined effects of CT in the intestinal lumen on myenteric and submucosal AH neurons. Methods: Isolated segments of guinea pig jejunum were incubated for 90 min with saline plus CT (12.5 μg/ml) or CT + neurotransmitter antagonist, or CT + tetrodotoxin (TTX) in their lumen...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28493529/pain-in-knee-osteoarthritis-is-associated-with-variation-in-the-neurokinin-1-substance-p-receptor-tacr1-gene
#13
S C Warner, D A Walsh, L L Laslett, R A Maciewicz, A Soni, D J Hart, W Zhang, K R Muir, E M Dennison, P Leaverton, E Rampersaud, C Cooper, T D Spector, F M Cicuttini, N K Arden, G Jones, M Doherty, A M Valdes
BACKGROUND: Substance P (SP) is a pain- and inflammation-related neuropeptide which preferentially binds to the neurokinin receptor 1 (NK1 ). SP and NK1 receptors have been implicated in joint pain, inflammation and damage in animal models and human studies of osteoarthritis (OA). The aim of this study was to test if genetic variation at the neurokinin 1 receptor gene (TACR1) is associated with pain in individuals with radiographic knee OA. METHODS: Participants from the Genetics of OA and Lifestyle study were used for the discovery group (n = 1615)...
August 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28485408/genetic-and-pharmacological-antagonism-of-nk1-receptor-prevents-opiate-abuse-potential
#14
A J Sandweiss, M I McIntosh, A Moutal, R Davidson-Knapp, J Hu, A K Giri, T Yamamoto, V J Hruby, R Khanna, T M Largent-Milnes, T W Vanderah
Development of an efficacious, non-addicting analgesic has been challenging. Discovery of novel mechanisms underlying addiction may present a solution. Here we target the neurokinin system, which is involved in both pain and addiction. Morphine exerts its rewarding actions, at least in part, by inhibiting GABAergic input onto substance P (SP) neurons in the ventral tegmental area (VTA), subsequently increasing SP release onto dopaminergic neurons. Genome editing of the neurokinin 1 receptor (NK1R) in the VTA renders morphine non-rewarding...
May 9, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28482051/biomarkers-of-chronic-acrolein-inhalation-exposure-in-mice-implications-for-tobacco-product-induced-toxicity
#15
Daniel J Conklin, Marina V Malovichko, Iris Zeller, Trinath P Das, Tatiana V Krivokhizhina, Blake H Lynch, Pawel Lorkiewicz, Abhinav Agarwal, Nalinie Wickramasinghe, Petra Haberzettl, Srinivas D Sithu, Jasmit Shah, Timothy E O'Toole, Shesh N Rai, Aruni Bhatnagar, Sanjay Srivastava
Exposure to tobacco smoke, which contains several harmful and potentially harmful constituents such as acrolein increases cardiovascular disease (CVD) risk. Although high acrolein levels induce pervasive cardiovascular injury, the effects of low-level exposure remain unknown and sensitive biomarkers of acrolein toxicity have not been identified. Identification of such biomarkers is essential to assess the toxicity of acrolein present at low levels in the ambient air or in new tobacco products such as e-cigarettes...
May 8, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28472227/cortical-nnos-nk1-receptor-neurons-are-regulated-by-cholinergic-projections-from-the-basal-forebrain
#16
Rhîannan H Williams, Jacqueline Vazquez-DeRose, Alexia M Thomas, Juliette Piquet, Bruno Cauli, Thomas S Kilduff
Cholinergic (ACh) basal forebrain (BF) neurons are active during wakefulness and rapid eye movement (REM) sleep and are involved in sleep homeostasis. We have previously shown in adult animals that cortical neurons that express neuronal nitric oxide synthase (nNOS) and the receptor for Substance P (NK1R) are activated during non-REM (NREM) sleep in proportion to homeostatic sleep drive. Here, we show that BF neurons modulate cortical nNOS/NK1R cells. In vitro optogenetic stimulation of BF terminals both activated and inhibited nNOS/NK1R neurons...
May 2, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28464353/neurokinin-1-receptor-blocker-cp-99%C3%A2-994-improved-emesis-induced-by-cisplatin-via-regulating-the-activity-of-gastric-distention-responsive-neurons-in-the-dorsal-motor-nucleus-of-vagus-and-enhancing-gastric-motility-in-rats
#17
X Sun, L Xu, F Guo, W Luo, S Gao, X Luan
BACKGROUND: Nowadays, chemotherapy induced nausea and vomiting (CINV) is still common in patients with cancer. It was reported that substance P mediated CINV via neurokinin-1 (NK1 ) receptor and antagonists of NK1 receptor has been proved useful for treating CINV but the mechanism are not fully understood. This study aimed to examine the role of NK1 receptor blocker, CP-99 994, when administrated into dorsal motor nucleus of vagus (DMNV), on the cisplatin-induced emesis in rats and the possible mechanism...
May 2, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28447301/management-of-chemotherapy-induced-nausea-and-vomiting-in-pediatric-patients
#18
REVIEW
Rudolph M Navari
Chemotherapy-induced nausea and vomiting (CINV) is associated with a significant deterioration in quality of life and is perceived by patients as a major adverse effect of the treatment. This review summarizes the safety and efficacy of current antiemetic agents for the prevention of CINV in children. Information on antiemetic prophylaxis for CINV in children was obtained from a literature review of current peer-reviewed articles and recent international guidelines. The literature review and the international antiemetic guidelines provide recommendations for use of specific antiemetics in children based on the emetogenicity of the chemotherapy...
June 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/28423730/the-sclttaxbcr-abl-transgenic-mouse-model-closely-reflects-the-differential-effects-of-dasatinib-on-normal-and-malignant-hematopoiesis-in-chronic-phase-cml-patients
#19
Claudia Schubert, Nicolas Chatain, Till Braunschweig, Mirle Schemionek, Kristina Feldberg, Melanie Hoffmann, Olli Dufva, Satu Mustjoki, Tim H Brümmendorf, Steffen Koschmieder
The second generation tyrosine kinase inhibitor (TKI) dasatinib is a clinically approved drug for chronic myeloid leukemia (CML) as well as Ph+ acute lymphoblastic leukemia. In addition to its antileukemic effects, dasatinib was shown to impact on normal hematopoiesis and cells of the immune system.Due to the fact that the murine in vivo studies so far have not been performed in a chronic-phase CML model under steady-state conditions, our aim was to study the hematopoietic effects of dasatinib (20 mg/kg p.o...
May 23, 2017: Oncotarget
https://www.readbyqxmd.com/read/28404628/simultaneous-detection-of-decidual-th1-th2-and-nk1-nk2-immunophenotyping-in-unknown-recurrent-miscarriage-using-8-color-flow-cytometry-with-fsc-vt-extended-strategy
#20
Peng Dong, Xi Wen, Jia Liu, Cui-Yan Yan, Jing Yuan, Lan-Rong Luo, Qiao-Fei Hu, Jian Li
Th1/Th2 imbalance is considered as a mechanism for recurrent miscarriage. The NK1/NK2 paradigm is hypothesised to play an important role in pregnancy. However, few results showed simultaneous changes of these subsets in vivo in decidual tissues. The present study aimed to detect the decidual mononuclear cells (dMo), and the Th1/Th2, and NK1/NK2 paradigm simultaneously using multiparametric flow cytometry (MFC) in unexplained recurrent miscarriages (URM). Mononuclear cells were isolated from the decidual tissues of URM cases and early pregnant women...
June 30, 2017: Bioscience Reports
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