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Sert 1

Umit Kervan, Sinan Sabit Kocabeyoglu, Dogan Emre Sert, Emre Aygün, Kemal Kavasoglu, Mehmet Karahan, Ertekin Utku Unal, Mustafa Pac
OBJECTIVES: The common femoral artery is the standard site for immediate vascular access when initiating adult venoarterial extracorporeal membrane oxygenation. However, this approach is fraught with problems such as femoral artery occlusion, distal limb ischemia, reperfusion injury resulting in compartment syndrome, retroperitoneal hemorrhage, thrombosis, embolization, and most importantly, pulmonary edema. Here, we show our preference of using the subclavian artery with a side graft as a different cannulation technique for outflow of extracorporeal membrane oxygenation, which can avoid complications associated with different access techniques...
October 14, 2016: Experimental and Clinical Transplantation
Andrew P Degnan, George O Tora, Hong Huang, David A Conlon, Carl D Davis, Umesh M Hanumegowda, Xiaoping Hou, Yi Hsiao, Joanna Hu, Rudolph Krause, Yu-Wen Li, Amy E Newton, Rick L Pieschl, Joseph Raybon, Thorsten Rosner, Jung-Hui Sun, Matthew T Taber, Sarah J Taylor, Michael K Wong, Huiping Zhang, Nicholas J Lodge, Joanne J Bronson, John E Macor, Kevin W Gillman
Combination studies of neurokinin 1 (NK1) receptor antagonists and serotonin-selective reuptake inhibitors (SSRIs) have shown promise in preclinical models of depression. Such a combination may offer important advantages over the current standard of care. Herein we describe the discovery and optimization of an indazole-based chemotype to provide a series of potent dual NK1 receptor antagonists/serotonin transporter (SERT) inhibitors to overcome issues of ion channel blockade. This effort culminated in the identification of compound 9, an analog that demonstrated favorable oral bioavailability, excellent brain uptake, and robust in vivo efficacy in a validated depression model...
October 17, 2016: ACS Chemical Neuroscience
Fatih Akın, Ahmet Sert, Şükrü Arslan
BACKGROUND: Mean platelet volume (MPV), which is commonly used as a measure of platelet size, indicates the rate of platelet production and platelet activation. We aimed to evaluate the mean platelet volume in children with hepatitis A. METHODS: In this retrospective case-controlled study, the study population consisted of 62 children with hepatitis A and 62 healthy control subjects. RESULTS: MPV values, aspartate transaminase (AST), and alanine transaminase (ALT) levels on admission were significantly increased in patients with hepatitis A when compared to controls whereas white blood cell (WBC) counts were significantly lower...
October 6, 2016: Journal of Health, Population, and Nutrition
Friederike Matthäus, Nasser Haddjeri, Connie Sánchez, Yasmina Martí, Senda Bahri, Renaud Rovera, Patrick Schloss, Thorsten Lau
Citalopram is a clinically applied selective serotonin re-uptake inhibitor for antidepressant pharmacotherapy. It consists of two enantiomers, S-citalopram (escitalopram) and R-citalopram, of which escitalopram exerts the antidepressant therapeutic effect and has been shown to be one of the most efficient antidepressants, while R-citalopram antagonizes escitalopram via an unknown molecular mechanism that may depend on binding to a low-affinity allosteric binding site of the serotonin transporter. However, the precise mechanism of antidepressant regulation of the serotonin transporter by citalopram enantiomers still remains elusive...
September 21, 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
Jessica ChenFeng, Lana Kim, Yuwei Wu, Carmen Knudson-Martin
Asian Americans juggle the intersections of multiple social identities and societal discourses as they respond to experiences of immigration, marginalization, and patriarchy, integrate collectivist and individualistic family values, and form families and intimate relationships. In this study we examine what we have learned as we apply Socio-Emotional Relationship Therapy (SERT) with heterosexual couples of Asian heritage. SERT begins with sociocultural attunement and the assumption that relationships should mutually support each partner...
September 24, 2016: Family Process
Jenna L N Sprowles, Jillian R Hufgard, Arnold Gutierrez, Rebecca A Bailey, Sarah A Jablonski, Michael T Williams, Charles V Vorhees
Selective serotonin reuptake inhibitors (SSRIs) block the serotonin (5-HT) reuptake transporter (SERT) and increase synaptic 5-HT. 5-HT is also important in brain development; hence when SSRIs are taken during pregnancy there exists the potential for these drugs to affect CNS ontogeny. Prenatal SSRI exposure has been associated with an increased prevalence of autism spectrum disorder (ASD), and peripheral 5-HT is elevated in some ASD patients. Perinatal SSRI exposure in rodents has been associated with increased depression and anxiety-like behavior, decreased sociability, and impaired learning in the offspring, behaviors often seen in ASD...
November 2016: International Journal of Developmental Neuroscience
M Y Liu, L J Zhang, M C Liu
OBJECTIVE: To evaluate the effect of ginsenoside pre-treatment on serotonin (5-hydroxytryptamine, 5-HT), 5-HT2A receptor (5-HT2AR), and 5-HT transporter (serotonin transporter, SERT) in serum, platelet lysate and brain tissue homogenates in SD rats with myocardial infarction (MI) or depression. METHODS: Eighty SD rats were randomized treated with ginsenoside or normal saline(NS). After 4 weeks, the rats were, then, randomized to four subgroups: the MI, the depression, the MI in combination with depression and sham subgroups...
September 1, 2016: Zhonghua Nei Ke za Zhi [Chinese Journal of Internal Medicine]
Gavin McLaughlin, Noreen Morris, Pierce V Kavanagh, John D Power, Geraldine Dowling, Brendan Twamley, John O'Brien, Brian Talbot, Donna Walther, John S Partilla, Michael H Baumann, Simon D Brandt
3-Methoxy-2-(methylamino)-1-(4-methylphenyl)propan-1-one (mexedrone) appeared in 2015 and was advertised by UK Internet retailers as a non-controlled mephedrone derivative (2-(methylamino)-1-(4-methylphenyl)propan-1-one), which was of particular interest to countries who operate generic drugs legislation. This study describes the synthesis and analytical characterization of mexedrone and differentiation from its isomer, N-methoxymephedrone, which was predicted to be a suitable candidate before the identity of mexedrone was revealed...
August 15, 2016: Drug Testing and Analysis
Jennifer M Panlilio, Sara Marin, Marissa B Lobl, M Danielle McDonald
The selective serotonin reuptake inhibitor (SSRI) fluoxetine (FLX), the active ingredient of the antidepressant drug Prozac, inhibits reuptake of the neurotransmitter, serotonin (5-HT; 5-hydroxytryptamine), into cells by the 5-HT transporter (SERT). Given the role of 5-HT in oxygen detection and the cardiovascular and ventilatory responses of fish to hypoxia, we hypothesized that treatment of the Gulf toadfish, Opsanus beta, with FLX would interfere with their response to hypoxia. Toadfish treated intra-arterially with 3...
2016: Scientific Reports
Tanja Dujic, Kaixin Zhou, Roger Tavendale, Colin N A Palmer, Ewan R Pearson
OBJECTIVE: The mechanism causing gastrointestinal intolerance to metformin treatment is unknown. We have previously shown that reduced-function alleles of organic cation transporter 1 (OCT1) are associated with increased intolerance to metformin. Considering recent findings that serotonin reuptake transporter (SERT) might also be involved in metformin intestinal absorption, and the role of serotonin in gastrointestinal physiology, in this study we investigated the association between a common polymorphism in the SERT gene and metformin gastrointestinal intolerance...
August 4, 2016: Diabetes Care
Mehtap Evran, Murat Sert, Tamer Tetiker, Gamze Akkuş, Ömer Sunkar Biçer
Spontaneous calcaneal fractures in diabetic patients without obvious trauma may occur, sometimes accompanying diabetic foot ulcers. In the current study we report four cases who were hospitalized for diabetic foot ulcer with concomitant calcaneal fractures. There were four diabetic patients (one type 1 and three type 2) who registered with diabetic foot ulcers with coexisting calcaneal fractures, all of which were classified as Type A according to Essex Lopresti Calcaneal Fracture Classification. Two of the patients with renal failure were in a routine dialysis program, as well as vascular compromise and osteomyelitis in all of the patients...
July 16, 2016: World Journal of Clinical Cases
F P Mayer, L Wimmer, O Dillon-Carter, J S Partilla, N V Burchardt, M D Mihovilovic, M H Baumann, H H Sitte
BACKGROUND AND PURPOSE: 4-Methyl-N-methylcathinone (mephedrone) is a synthetic stimulant that acts as a substrate-type releaser at transporters for dopamine (DAT), noradrenaline (NET) and 5-HT (SERT). Upon systemic administration, mephedrone is metabolized to several phase I compounds: the N-demethylated metabolite, 4-methylcathinone (nor-mephedrone); the ring-hydroxylated metabolite, 4-hydroxytolylmephedrone (4-OH-mephedrone); and the reduced keto-metabolite, dihydromephedrone. EXPERIMENTAL APPROACH: We used in vitro assays to compare the effects of mephedrone and synthetically prepared metabolites on transporter-mediated uptake and release in HEK293 cells expressing human monoamine transporters and in rat brain synaptosomes...
September 2016: British Journal of Pharmacology
Mehmet Hamurcu, Erdogan E Hakki, Tijen Demiral Sert, Canan Özdemir, Ersin Minareci, Zuhal Z Avsaroglu, Sait Gezgin, Seyit Ali Kayis, Richard W Bell
Recent studies indicate an extremely high level of tolerance to boron (B) toxicity in Puccinellia distans (Jacq.) Parl. but the mechanistic basis is not known. Puccinellia distans was exposed to B concentrations of up to 1000 mg B L-1 and root B uptake, growth parameters, B and N contents, H2O2 accumulation and ·OH-scavenging activity were measured. Antioxidant enzyme activities including superoxide dismutase (SOD), ascorbate peroxidase, catalase, peroxidase and glutathione reductase, and lipid peroxidation products were determined...
2016: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
Hao Sun, Min Shi, Wei Zhang, Yue-Ming Zheng, Ya-Zhou Xu, Jun-Jie Shi, Ting Liu, Hendra Gunosewoyo, Tao Pang, Zhao-Bing Gao, Fan Yang, Jie Tang, Li-Fang Yu
A novel series of sigma (σ) receptor ligands based on an alkoxyisoxazole scaffold has been designed and synthesized. Preliminary receptor binding assays identified highly potent (Ki < 1 nM) and selective σ1 ligands devoid of binding interactions with the monoamine transporters DAT, NET, and SERT. In particular, compound 53 was shown to possess significant antinociceptive activity in the mouse formalin-induced inflammation pain model when administered intraperitoneally at 40 and 80 mg/kg. Initial pharmacokinetics evaluation indicated an excellent brain exposure following oral dosing in mice, suggesting that further investigation into the use of alkoxyisoxazoles as σ1 ligands for antinociception is warranted...
July 14, 2016: Journal of Medicinal Chemistry
A A Terentev, A E Lychkova, A N Kazimirsky, A M Puzikov
The review describes the influence of serotonin (5-HT) and its receptor, transporter SERT and nuclear factor Nf-kB on the immune function of the body, particularly in the digestive tract. The mechanisms of the synthesis, metabolism and catab. olism of 5-HT are characterized. The targets for serotonin on cell level are immunoactive cells--neutrophils, eosinophils, leukocytes, monocytes and dendritic cells. Receptor and non-receptor described mechanisms of action of peripheral serotonin are described. immunoactive cells express on their membrane 5 HT1A-5-HT1E-5-HT2A-5-HT3-, 5-HT4- and 5-HT7-serotonin receptor subtypes...
2016: Experimental & Clinical Gastroenterology
Sivaprakasam R Saroja, Yogesh D Aher, Predrag Kalaba, Nilima Y Aher, Martin Zehl, Volker Korz, Saraswathi Subramaniyan, Andras G Miklosi, Lisa Zanon, Winfried Neuhaus, Harald Höger, Thierry Langer, Ernst Urban, Johann Leban, Gert Lubec
A series of compounds targeting the dopamine transporter (DAT) haS been shown to improve memory performance most probably by re-uptake inhibition. Although specific DAT inhibitors are available, there is limited information about specificity, mechanism and in particular the effect on dopamine receptors. It was therefore the aim of the study to test the DAT inhibitor 4-(diphenyl-methanesulfinylmethyl)-2-methyl-thiazole (code: CE-111), synthetized in our laboratory for the specificity to target DAT, for the effects upon spatial memory and for induced dopamine receptor modulation...
October 1, 2016: Behavioural Brain Research
Dilek Gogas Yavuz, Habip Bilen, Seda Sancak, Tayfun Garip, Zeliha Hekimsoy, Ibrahim Sahin, Murat Yilmaz, Hasan Aydin, Aysegul Atmaca, Murat Sert, Pinar Karakaya, Dilek Arpaci, Aytekin Oguz, Nilgun Guvener
OBJECTIVE: The objective of this study is to evaluate the impact of sequential telephonic interviews on treatment persistence and daily adherence to insulin injections among insulin-naïve type 2 diabetes patients initiated on different insulin regimens in a 3-month period. METHODS: A total of 1,456 insulin-naïve patients with type 2 diabetes (mean [standard deviation, SD] age: 56.0 [12.0] years, 49.1% were females) initiated on insulin therapy and consecutively randomized to sequential (n=733) and single (n=723) telephonic interview groups were included...
2016: Patient Preference and Adherence
M Julia García-Fuster, Jesús A García-Sevilla
RATIONALE: Fas-associated death domain (FADD) is an adaptor of death receptors that can also induce anti-apoptotic actions through its phosphorylated form (p-FADD). Activation of monoamine receptors, indirect targets of classic anti-depressant drugs (ADs), reduced FADD and increased p-FADD and p-FADD/FADD ratio in brain. OBJECTIVES: To ascertain whether ADs, which indirectly regulate monoamine receptors, modulate FADD protein forms to promote anti-apoptotic actions...
August 2016: Psychopharmacology
Stephanie B Linley, Francisco Olucha-Bordonau, Robert P Vertes
As well recognized, serotonergic (5-HT) fibers distribute widely throughout the forebrain, including the amygdala. Although a few reports have examined the 5-HT innervation of select nuclei of the amygdala in the rat, no previous report has described overall 5-HT projections to the amygdala in the rat. Using immunostaining for the serotonin transporter, SERT, we describe the complete pattern of distribution of 5-HT fibers to the amygdala (proper) and to the extended amygdala in the rat. Based on its ontogenetic origins, the amygdalar was subdivided into two major parts: pallial and subpallial components, with the pallial component further divided into superficial and deep nuclei (Olucha-Bordonau et al...
May 23, 2016: Journal of Comparative Neurology
Durmuş Sert, Emin Mercan, Serdar Aydemir, Mustafa Civelek
The aim of this work was to study the influence of milk somatic cell count (SCC) levels on spray-dried milk powders. For this reason, 3 cow milks with different SCC (<300,000, 300,000-700,000, >700,000 SCC/mL) were processed into skim (SMP) and whole milk powder (WMP). The effect of SCC on the physicochemical and functional characteristics of the milk powders and textural properties of set-type yogurts produced from reconstituted milk powders with different SCC was evaluated. A crucial difference was noted between milk powders depending on different SCC...
July 2016: Journal of Dairy Science
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