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https://www.readbyqxmd.com/read/28198447/the-tnf-%C3%AE-antagonist-etanercept-reverses-age-related-decreases-in-colonic-sert-expression-and-faecal-output-in-mice
#1
Bhavik Anil Patel, Sara Fidalgo, Chunfang Wang, Leena Parmar, Kasonde Mandona, Annabelle Panossian, Melanie S Flint, Richard N Ranson, M Jill Saffrey, Mark S Yeoman
Treatment for chronic constipation in older people is challenging and the condition has a major impact on quality of life. A lack of understanding about the causes of this condition has hampered the development of effective treatments. 5-HT is an important pro-kinetic agent in the colon. We examined whether alterations in colonic 5-HT signalling underlie age-related changes in faecal output in mice and whether these changes were due to an increase in TNF-α. Components of the 5-HT signalling system (5-HT, 5-HIAA, SERT) and TNF-α expression were examined in the distal colon of 3, 12, 18 and 24-month old mice and faecal output and water content monitored under control conditions and following the administration of etanercept (TNF-α inhibitor; 1 mg Kg(-1))...
February 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28182708/comparison-of-brain-serotonin-transporter-using-i-123-adam-between-obese-and-non-obese-young-adults-without-an-eating-disorder
#2
Chih-Hsing Wu, Chin-Sung Chang, Yen Kuang Yang, Lie-Hang Shen, Wei-Jen Yao
Cerebral serotonin metabolism has an important but controversial role in obesity. However, it is not given enough attention in morbidly obese young adults. We used single photon emission computed tomography (SPECT) with [I-123]-labeled 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine (ADAM) to investigate changes in serotonin transporter (SERT) availability in 10 morbidly obese young adults without an eating disorder (M/F = 5/5, body mass index (BMI): 40.3 ± 4.1 kg/m2, percentage of body fat (BF%): 46...
2017: PloS One
https://www.readbyqxmd.com/read/28132172/evaluation-of-benign-afebrile-convulsions-in-16-children-with-rotavirus-gastroenteritis
#3
Alaaddin Yorulmaz, Sadiye Sert, Fatma Hilal Yilmaz
In this study, we aimed to investigate the demographic, clinical, and laboratory findings of the patients hospitalized with rotavirus gastroenteritis-related afebrile seizure, retrospectively. The study population consisted of 16 patients (9 girls and 7 boys) with a mean age of 13.81 ± 5.98 months (age range 6-26). The male/female ratio was 0.77. None of the patients had any psychomotor developmental retardation. Neurological examinations of all the patients were normal. There were 7 patients with generalized tonic (43...
January 28, 2017: Acta Neurologica Belgica
https://www.readbyqxmd.com/read/28097008/preclinical-findings-predicting-efficacy-and-side-effect-profile-of-ly2940094-an-antagonist-of-nociceptin-receptors
#4
Jeffrey M Witkin, Linda M Rorick-Kehn, Mark J Benvenga, Benjamin L Adams, Scott D Gleason, Karen M Knitowski, Xia Li, Steven Chaney, Julie F Falcone, Janice W Smith, Julie Foss, Kirsti Lloyd, John T Catlow, David L McKinzie, Kjell A Svensson, Vanessa N Barth, Miguel A Toledo, Nuria Diaz, Celia Lafuente, Alma Jiménez, Alfonso Benito, Conception Pedregal, Maria A Martínez-Grau, Anke Post, Michael A Ansonoff, John E Pintar, Michael A Statnick
Nociceptin/Orphanin FQ (N/OFQ) is a 17 amino acid peptide whose receptor is designated ORL1 or nociceptin receptor (NOP). We utilized a potent, selective, and orally bioavailable antagonist with documented engagement with NOP receptors in vivo to assess antidepressant- and anxiolytic-related pharmacological effects of NOP receptor blockade along with measures of cognitive and motor impingement. LY2940094 ([2-[4-[(2-chloro-4,4-difluoro-spiro[5H-thieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)methyl]-3-methyl-pyrazol-1-yl]-3-pyridyl]methanol) displayed antidepressant-like behavioral effects in the forced-swim test in mice, an effect absent in NOP (-/-) mice...
December 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28094186/nardonaphthalenones-a-and-b-from-the-roots-and-rhizomes-of-nardostachys-chinensis-batal
#5
Xu Deng, Yi-Jing Wu, Ying-Peng Chen, Hong-Hong Zheng, Zhong-Ping Wang, Yan Zhu, Xiu-Mei Gao, Yan-Tong Xu, Hong-Hua Wu
Nardonaphthalenones A and B (1-2), one new apo-α-carotenone (3) and four new monoterpenoids (4, 8-9 and 11), along with six known compounds (5-7, 10, 12-13) were isolated from the dried roots and rhizomes of Nardostachys chinensis Batal. Their structures were elucidated by analysis of the spectroscopic data including NMR, HRESIMS and circular dichroism data. Furthermore, the serotonin transporter (SERT)-regulating activities of these isolates were evaluated, among them compound 3 showed the strongest enhancement activity while compound 12 showed a moderate inhibition activity on SERT...
January 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28068779/norepinephrine-transporter-gene-variants-and-remission-from-depression-with-venlafaxine-treatment-in-older-adults
#6
Victoria S Marshe, Malgorzata Maciukiewicz, Soham Rej, Arun K Tiwari, Etienne Sibille, Daniel M Blumberger, Jordan F Karp, Eric J Lenze, Charles F Reynolds, James L Kennedy, Benoit H Mulsant, Daniel J Müller
OBJECTIVE: The primary objective of this study was to investigate five putatively functional variants of the norepinephrine transporter (SLC6A2, NET) and serotonin transporter (SLC6A4, SERT) genes and remission in depressed older adults treated with venlafaxine. A secondary objective was to analyze 17 other variants in serotonergic system genes (HTR1A, HTR2A, HTR1B, HTR2C, TPH1, TPH2) potentially involved in the mechanism of action of venlafaxine. METHOD: The sample included 350 adults age 60 or older with DSM-IV-defined major depressive disorder and a score of at least 15 on the Montgomery-Åsberg Depression Rating Scale (MADRS)...
January 10, 2017: American Journal of Psychiatry
https://www.readbyqxmd.com/read/28066808/effect-of-mr-imaging-contrast-thresholds-on-prediction-of-neoadjuvant-chemotherapy-response-in-breast-cancer-subtypes-a-subgroup-analysis-of-the-acrin-6657-i-spy-1-trial
#7
Wen Li, Vignesh Arasu, David C Newitt, Ella F Jones, Lisa Wilmes, Jessica Gibbs, John Kornak, Bonnie N Joe, Laura J Esserman, Nola M Hylton
Functional tumor volume (FTV) measurements by dynamic contrast-enhanced magnetic resonance imaging can predict treatment outcomes for women receiving neoadjuvant chemotherapy for breast cancer. Here, we explore whether the contrast thresholds used to define FTV could be adjusted by breast cancer subtype to improve predictive performance. Absolute FTV and percent change in FTV (ΔFTV) at sequential time-points during treatment were calculated and investigated as predictors of pathologic complete response at surgery...
December 2016: Tomography: a Journal for Imaging Research
https://www.readbyqxmd.com/read/28043073/a-comparative-qsar-analysis-and-molecular-docking-studies-of-phenyl-piperidine-derivatives-as-potent-dual-nk1r-antagonists-serotonin-transporter-sert-inhibitors
#8
Somayeh Zare, Masood Fereidoonnezhad, Davoud Afshar, Zahra Ramezani
Depression is a critical mood disorder that affects millions of patients. Available therapeutic antidepressant agents are associated with several undesirable side effects. Recently, it has been shown that Neurokinin 1 receptor (NK1R) antagonists can potentiate the antidepressant effects of serotonin-selective reuptake inhibitors (SSRIs). In this study, a series of phenyl piperidine derivatives as potent dual NK1R antagonists/serotonin transporter (SERT) inhibitors were applied to quantitative structure-activity relationship (QSAR) analysis...
December 23, 2016: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28035393/fluoxetine-protects-against-methamphetamine%C3%A2-induced-lung-inflammation-by-suppressing-oxidative-stress-through-the-sert-p38-mapk-nrf2-pathway-in-rats
#9
Yun Wang, Yu-Han Gu, Ming Liu, Yang Bai, Huai-Liang Wang
Methamphetamine (MA) abuse is a major public health and safety concern throughout the world and a growing burden on healthcare costs. The purpose of the present study was to investigate the protective effect of fluoxetine against MA‑induced chronic pulmonary inflammation and to evaluate the potential role of nuclear factor erythroid 2-related factor 2 (Nrf2)-mediated antioxidative stress. Wistar rats were divided into control, MA and two fluoxetine‑treated groups. Rats in the MA and the two fluoxetine‑treated groups were treated daily with intraperitoneal injection of 10 mg/kg MA twice daily...
February 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27993209/enhanced-serotonin-signaling-stimulates-ordered-intestinal-mucosal-growth
#10
John J Tackett, Neeru Gandotra, Michaela C Bamdad, Eleanor D Muise, Robert A Cowles
BACKGROUND: Significant quantities of serotonin (5-hydroxytryptamine; 5-HT) are found in the intestine, and studies have demonstrated that 5-HT can stimulate enterocyte cell division, suggesting regulatory roles in mucosal homeostasis and intestinal adaptation. We hypothesized that excess enteric 5-HT signaling enhances mucosal growth without changing intestinal villous cellular makeup. METHODS: Mice lacking the serotonin reuptake transporter (SERT) and wild-type littermates (WTLM) were euthanized and their ileum analyzed...
February 2017: Journal of Surgical Research
https://www.readbyqxmd.com/read/27981188/maternal-immune-activation-epigenetically-regulates-hippocampal-serotonin-transporter-levels
#11
Sonali N Reisinger, Eryan Kong, Deeba Khan, Stefan Schulz, Marianne Ronovsky, Stefanie Berger, Orsolya Horvath, Maureen Cabatic, Angelika Berger, Daniela D Pollak
Major depressive disorder (MDD) is one of the most debilitating psychiatric diseases, affecting a large percentage of the population worldwide. Currently, the underlying pathomechanisms remain incompletely understood, hampering the development of critically needed alternative therapeutic strategies, which further largely depends on the availability of suitable model systems. Here we used a mouse model of early life stress - a precipitating factor for the development of MDD - featuring infectious stress through maternal immune activation (MIA) by polyinosinic:polycytidilic acid (Poly(I:C)) to examine epigenetic modulations as potential molecular correlates of the alterations in brain structure, function and behavior...
October 2016: Neurobiology of Stress
https://www.readbyqxmd.com/read/27927740/chronic-vortioxetine-treatment-reduces-exaggerated-expression-of-conditioned-fear-memory-and-restores-active-coping-behavior-in-chronically-stressed-rats
#12
Lauren Hatherall, Connie Sánchez, David A Morilak
BACKGROUND: Stress is a risk factor for depression and anxiety disorders, disrupting neuronal processes leading to exaggerated fear and compromised coping behaviors. Current antidepressants are only partially effective. Vortioxetine, a novel multimodal antidepressant, is a serotonin transporter inhibitor; 5-HT3, 5-HT7, and 5-HT1D receptor antagonist; 5-HT1B partial agonist; and 5-HT1A agonist. We have shown that chronic dietary vortioxetine administration reversed stress-induced deficits in cognitive flexibility...
December 29, 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27917802/transient-neurological-symptoms-after-spinal-anesthesia
#13
Muhammet Gozdemir, Bunyamin Muslu, Huseyin Sert, Burhanettin Usta, Ruveyda Irem Demircioglu, Hulya Kasikara
PURPOSE: The aim of this study was to investigate the incidence of transient neurological symptoms (TNS) after spinal anesthesia with levobupivacaine, bupivacaine, articaine or lidocaine. METHODS: The patients (n=400) were randomly assigned to receive spinal anesthesia with levobupivacaine, bupivacaine, articaine or isobaric lidocaine. Onsets of sensory and motor block were recorded. On postoperative days 1, 2 and 3, patients were interviewed by an investigator blinded to the spinal anaesthetic agent used...
December 1, 2016: Clinical and Investigative Medicine. Médecine Clinique et Experimentale
https://www.readbyqxmd.com/read/27908600/adenoma-recurrence-after-piecemeal-colonic-emr-is-predictable-the-sydney-emr-recurrence-tool
#14
David J Tate, Lobke Desomer, Amir Klein, Gregor Brown, Luke F Hourigan, Eric Y T Lee, Alan Moss, Donald Ormonde, Spiro Raftopoulos, Rajvinder Singh, Stephen J Williams, Simon Zanati, Karen Byth, Michael J Bourke
BACKGROUND AND AIMS: EMR is the primary treatment of large laterally spreading lesions (LSLs) in the colon. Residual or recurrent adenoma (RRA) is a major limitation. We aimed to identify a robust method to stratify the risk of RRA. METHODS: Prospective multicenter data on consecutive LSLs ≥20 mm removed by piecemeal EMR from 8 Australian tertiary-care centers were included (September 2008 until May 2016). A logistic regression model for endoscopically determined recurrence (EDR) was created on a randomly selected half of the cohort to yield the Sydney EMR recurrence tool (SERT), a 4-point score to stratify the incidence of RRA based on characteristics of the index EMR...
November 28, 2016: Gastrointestinal Endoscopy
https://www.readbyqxmd.com/read/27897987/atmospheric-correction-of-satellite-gf-1-wfv-imagery-and-quantitative-estimation-of-suspended-particulate-matter-in-the-yangtze-estuary
#15
Pei Shang, Fang Shen
The Multispectral Wide Field of View (WFV) camera on the Chinese GF-1 satellite, launched in 2013, has advantages of high spatial resolution (16 m), short revisit period (4 days) and wide scene swath (800 km) compared to the Landsat-8/OLI, which make it an ideal means of monitoring spatial-temporal changes of Suspended Particulate Matter (SPM) in large estuaries like the Yangtze Estuary. However, a lack of proper atmospheric correction methods has limited its application in water quality assessment. We propose an atmospheric correction method based on a look up table coupled by the atmosphere radiative transfer model (6S) and the water semi-empirical radiative transfer (SERT) model for inversion of water-leaving reflectance from GF-1 top-of-atmosphere radiance, and then retrieving SPM concentration from water-leaving radiance reflectance of the Yangtze Estuary and its adjacent sea...
November 25, 2016: Sensors
https://www.readbyqxmd.com/read/27882537/neurochemical-and-behavioral-effects-of-hypidone-hydrochloride-yl-0919-a-novel-combined-selective-serotonin-reuptake-inhibitor-and-partial-5-ht1a-agonist
#16
Li-Ming Zhang, Xiao-Yun Wang, Nan Zhao, Yu-Lu Wang, Xiao-Xu Hu, Yu-Hua Ran, Yan-Qin Liu, You-Zhi Zhang, Ri-Fang Yang, Yun-Feng Li
The purpose of the present study was to investigate the pharmacology of hypidone hydrochloride (YL-0919), a novel selective serotonin reuptake inhibitor (SSRI) and 5-hydroxytryptamine (5-HT)1A receptor agonist with high affinity for serotonin transporter (SERT) and 5-HT1A receptors. YL-0919 promoted [(35) S]GTPγ S binding at 85% of the magnitude of the full 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), suggesting that YL-0919 is a high-efficacy partial agonist of 5-HT1A receptors...
November 24, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27874199/glucose-and-lipid-levels-with-lanreotide-autogel-120-mg-in-treatment-na%C3%A3-ve-patients-with-acromegaly-data-from-the-primarys-study
#17
Philippe J Caron, Stephan Petersenn, Aude Houchard, Caroline Sert, John S Bevan
OBJECTIVE: Impaired glycaemic control, characteristic of acromegaly, can be exacerbated by treatment with somatostatin analogues (SSAs), particularly those with multireceptor activity. We present data from the PRIMARYS study on the impact of the SSA lanreotide, associated with tumour volume and hormonal improvements, on glucose and other metabolic parameters in acromegaly. DESIGN: PRIMARYS was a 48-week open-label single-arm phase 3b study of lanreotide autogel 120 mg/4 weeks...
November 22, 2016: Clinical Endocrinology
https://www.readbyqxmd.com/read/27865645/discovery-of-smp-304-a-novel-benzylpiperidine-derivative-with-serotonin-transporter-inhibitory-activity-and-5-ht1a-weak-partial-agonistic-activity-showing-the-antidepressant-like-effect
#18
Hidefumi Yoshinaga, Shuji Masumoto, Koji Koyama, Naoya Kinomura, Yuji Matsumoto, Taro Kato, Satoko Baba, Kenji Matsumoto, Tomoko Horisawa, Hitomi Oki, Kazuki Yabuuchi, Toru Kodo
We report the discovery of a novel benzylpiperidine derivative with serotonin transporter (SERT) inhibitory activity and 5-HT1A receptor weak partial agonistic activity showing the antidepressant-like effect. The 3-methoxyphenyl group and the phenethyl group of compound 1, which has weak SERT binding activity, but potent 5-HT1A binding activity, were optimized, leading to compound 35 with potent and balanced dual SERT and 5-HT1A binding activity, but also potent CYP2D6 inhibitory activity. Replacement of the methoxy group in the left part of compound 35 with a larger alkoxy group, such as ethoxy, isopropoxy or methoxy-ethoxy group ameliorated CYP2D6 inhibition, giving SMP-304 as a candidate...
January 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27826242/fluoxetine-prevents-a%C3%AE-1-42-induced-toxicity-via-a-paracrine-signaling-mediated-by-transforming-growth-factor-%C3%AE-1
#19
Filippo Caraci, Fabio Tascedda, Sara Merlo, Cristina Benatti, Simona F Spampinato, Antonio Munafò, Gian Marco Leggio, Ferdinando Nicoletti, Nicoletta Brunello, Filippo Drago, Maria Angela Sortino, Agata Copani
Selective reuptake inhibitors (SSRIs), such as fluoxetine and sertraline, increase circulating Transforming-Growth-Factor-β1 (TGF-β1) levels in depressed patients, and are currently studied for their neuroprotective properties in Alzheimer's disease. TGF-β1 is an anti-inflammatory cytokine that exerts neuroprotective effects against β-amyloid (Aβ)-induced neurodegeneration. In the present work, the SSRI, fluoxetine, was tested for the ability to protect cortical neurons against 1 μM oligomeric Aβ1-42-induced toxicity...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27782890/pediatric-small-bowel-transplantation-a-single-center-experience-from-turkey
#20
Cem Tuğmen, Maşallah Baran, İsmail Sert, Ayşe Berna Anıl, Eyüp Kebapçı, Sait Murat Doğan, Selçuk Kılınç, Gaye Aydın, Ayşe Gülden Diniz, Mustafa Ölmez, İbrahim Pirim, Cezmi Karaca
BACKGROUND/AIMS: Small bowel transplantation (SBTx) is a treatment option for patients with serious parenteral nutrition-related problems in intestinal failure. İzmir Tepecik Training Research Hospital Organ Transplantation Center is still the only pediatric intestinal transplant center in Turkey. MATERIAL AND METHODS: This study was approved by the local ethics committee. Patients' data were analyzed from the medical charts and the hospital digital database. Seven isolated SBTxs were performed in six children between 2010 and 2016...
September 2016: Turkish Journal of Gastroenterology: the Official Journal of Turkish Society of Gastroenterology
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