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https://www.readbyqxmd.com/read/28550249/avn-492-a-novel-highly-selective-5-ht6r-antagonist-preclinical-evaluation
#1
Alexandre V Ivachtchenko, Ilya Okun, Vladimir Aladinskiy, Yan Ivanenkov, Angela Koryakova, Ruben Karapetyan, Oleg Mitkin, Ramiz Salimov, Andrey Ivashchenko
Discovery of 5-HT6 receptor subtype and its exclusive localization within the central nervous system led to extensive investigations of its role in Alzheimer's disease, schizophrenia, and obesity. In the present study, we present preclinical evaluation of a novel highly-potent and highly-selective 5-HT6R antagonist, AVN-492. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM). Thus, the compound displayed great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc...
May 25, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28549897/daily-acute-intermittent-hypoxia-improves-breathing-function-with-acute-and-chronic-spinal-injury-via-distinct-mechanisms
#2
B J Dougherty, J Terada, S R Springborn, S Vinit, P M MacFarlane, G S Mitchell
Daily acute intermittent hypoxia (dAIH) elicits respiratory plasticity, enhancing respiratory motor output and restoring breathing capacity after incomplete cervical spinal injuries (cSCI). We hypothesized that dAIH-induced functional recovery of breathing capacity would occur after both acute (2 weeks) and chronic (8 weeks) cSCI, but through distinct cellular mechanisms. Specifically, we hypothesized that dAIH-induced breathing recovery would occur through serotonin-independent mechanisms 2wks post C2 cervical hemisection (C2Hs), versus serotonin-dependent mechanisms 8wks post C2Hs...
May 23, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28549887/fluvoxamine-maleate-effects-on-dopamine-signaling-in-the-prefrontal-cortex-of-stressed-parkinsonian-rats-implications-for-learning-and-memory
#3
Ernest Dallé, Willie M U Daniels, Musa V Mabandla
Parkinson's disease (PD) is also associated with cognitive impairment and reduced extrinsic supply of dopamine (DA) to the prefrontal cortex (PFC). In the present study, we looked at whether exposure to early life stress reduces DA and serotonin (5-HT) concentration in the PFC thus leading to enhanced cognitive impairment in a Parkinsonian rat model. Maternal separation was the stressor used to develop an animal model for early life stress that has chronic effects on brain and behavior. Sprague-Dawley rats were treated with the antidepressant Fluvoxamine maleate (FM) prior to a unilateral 6-hydroxydopamine (6-OHDA) lesion to model motor deficits in rats...
May 23, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28548869/neurotransmitter-receptor-availability-in-the-rat-brain-is-constant-in-a-24-hour-period
#4
A Oskamp, F Wedekind, T Kroll, D Elmenhorst, A Bauer
Wakefulness and sleep are fundamental characteristics of the brain. We, therefore, hypothesized that transmitter systems contribute to their regulation and will exhibit circadian alterations. We assessed the concentration of various neurotransmitter receptors and transporters including adenosinergic (A1AR, A2AAR, and ENT1), dopaminergic (D1R, D2R, and DAT), and serotonergic (5-HT2AR) target proteins. Adult male Sprague Dawley rats were used and maintained in a 12 h light: 12 h dark cycle (lights on from 07:00 h to 19:00 h)...
May 26, 2017: Chronobiology International
https://www.readbyqxmd.com/read/28546851/monoamine-oxidases-oxidative-stress-and-altered-mitochondrial-dynamics-in-cardiac-ageing
#5
REVIEW
Damien Maggiorani, Nicola Manzella, Dale E Edmondson, Andrea Mattevi, Angelo Parini, Claudia Binda, Jeanne Mialet-Perez
The advances in healthcare over the past several decades have resulted in populations now living longer. With this increase in longevity, a wider prevalence of cardiovascular diseases is more common and known to be a major factor in rising healthcare costs. A wealth of scientific evidence has implicated cell senescence as an important component in the etiology of these age-dependent pathologies. A number of studies indicate that an excess of reactive oxygen species (ROS) contributes to trigger and accelerate the cardiac senescence processes, and a new role of monoamine oxidases, MAO-A and MAO-B, is emerging in this context...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28546460/common-toxidromes-in-movement-disorder-neurology
#6
N Malek, M R Baker
BACKGROUND: Physicians can come across patients who are exposed to certain prescription drugs or toxins that can result in adverse effects and complications which have high rates of morbidity and mortality. OBJECTIVE: To summarise the key clinical features and management of the common movement disorder toxidromes relevant to physicians (with an interest in neurology). METHODS: We searched PUBMED from 1946 to 2016 for papers relating to movement toxidromes and their treatment...
June 2017: Postgraduate Medical Journal
https://www.readbyqxmd.com/read/28546314/chronic-stress-induced-behavioral-changes-associated-with-subregion-selective-serotonin-cell-death-in-the-dorsal-raphe
#7
Reka Natarajan, Laura Forrester, Nicolas Chiaia, Bryan K Yamamoto
The current study examined the neurochemical mechanisms and neuroanatomical changes underlying co-existing behavioral effects associated with chronic stress-induced alterations in serotonin (5HT) neurons. Chronic unpredictable stress (CUS) to adult male rats produced depression-like changes with cognitive dysfunction and selective cell death in the interfascicular nucleus of the dorsal raphe (DRif) resulting in decreased 5HTergic innervation of medial prefrontal cortex (mPFC). Twenty-one days of CUS decreased basal plasma levels of corticosterone and produced a shorter latency to immobility and longer durations of immobility in the force-swim test that persisted for one month after CUS...
May 25, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28546284/a-new-role-for-microbiota-dulling-the-thrust-of-serotonin-and-5ht3-signaling-cascade
#8
Eugene B Chang, Mrinalini C Rao
N/A.
May 25, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28545527/what-intrinsic-factors-influence-responsiveness-to-acupuncture-in-pain-a-review-of-pre-clinical-studies-that-used-responder-analysis
#9
Yu-Kang Kim, Ji-Yeun Park, Seung-Nam Kim, Mijung Yeom, Seungmin Lee, Ju-Young Oh, Hyangsook Lee, Younbyoung Chae, Dae-Hyun Hahm, Hi-Joon Park
BACKGROUND: Not many studies have investigated individual sensitivity to acupuncture. To explore the intrinsic factors related to individual responses to acupuncture, we reviewed published pre-clinical studies using responder analysis on pain. METHODS: We searched the PubMed and EMBASE databases to June 2015. We included pre-clinical reports describing responders and non-responders to anti-nociceptive and analgesic effects of acupuncture in animal study. We identified the potential intrinsic factors which might be related with the response to acupuncture...
May 25, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28545126/pheromone-sensing-neurons-regulate-peripheral-lipid-metabolism-in-caenorhabditis-elegans
#10
Rosalind Hussey, Jon Stieglitz, Jaleh Mesgarzadeh, Tiffany T Locke, Ying K Zhang, Frank C Schroeder, Supriya Srinivasan
It is now established that the central nervous system plays an important role in regulating whole body metabolism and energy balance. However, the extent to which sensory systems relay environmental information to modulate metabolic events in peripheral tissues has remained poorly understood. In addition, it has been challenging to map the molecular mechanisms underlying discrete sensory modalities with respect to their role in lipid metabolism. In previous work our lab has identified instructive roles for serotonin signaling as a surrogate for food availability, as well as oxygen sensing, in the control of whole body metabolism...
May 18, 2017: PLoS Genetics
https://www.readbyqxmd.com/read/28545014/paracetamol-causes-endocrine-disruption-and-hepatotoxicity-in-male-fish-rhamdia-quelen-after-subchronic-exposure
#11
Izonete Cristina Guiloski, João Luiz Coelho Ribas, Laercio Dante Stein Piancini, Ana Carolina Dagostim, Silvana Maris Cirio, Luis Fernando Fávaro, Suelen Lúcio Boschen, Marta Margarete Cestari, Cláudio da Cunha, Helena Cristina Silva de Assis
Paracetamol is one of the most widely sold non-prescription drugs. This study aimed to evaluate the effects of the paracetamol on reproductive, biochemical, genetic, histopathological and hematogical biomarkers by waterborne exposure. Male fish of Rhamdia quelen were exposed to environmental concentrations of paracetamol (0, 0.25, 2.5μg/L) in a semi-static bioassay for 21days. Hemoglobin and hematocrit were reduced upon exposure to 0.25μg/L of paracetamol. Leukocytes and thrombocytes increased after paracetamol exposure...
May 8, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28544903/estrogen-receptor-%C3%AE-deficiency-impairs-bdnf-5-ht2a-signaling-in-the-hippocampus-of-female-brain-a-possible-mechanism-for-menopausal-depression
#12
Anindit Chhibber, Sarah K Woody, M A Karim Rumi, Michael J Soares, Liqin Zhao
Depression currently affects 350 million people worldwide and 19 million Americans each year. Women are 2.5 times more likely to experience major depression than men, with some women appearing to be at a heightened risk during the menopausal transition. Estrogen signaling has been implicated in the pathophysiology of mood disorders including depression; however, the underlying mechanisms are poorly understood. In this study, the role of estrogen receptor (ER) subtypes, ERα and ERβ, in the regulation of brain-derived neurotrophic factor (BDNF) and serotonin (5-HT) signaling was investigated; two pathways that have been hypothesized to be interrelated in the etiology of depression...
May 18, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28543924/plasma-serotonin-level-is-a-predictor-for-recurrence-and-poor-prognosis-in-colorectal-cancer-patients
#13
Yan Xia, Dawei Wang, Nan Zhang, Zhihao Wang, Li Pang
AIM: To investigate the prognostic value of plasma serotonin levels in colorectal cancer (CRC). PATIENTS AND METHODS: Preoperative plasma serotonin levels of 150 healthy control (HC) cases, 150 benign colorectal polyp (BCP) cases, and 176 CRC cases were determined using radioimmunoassay assay. Serotonin levels were compared between HC, BCP, and CRC cases, and those in CRC patients were related to 5-year outcome. RESULTS: Plasma serotonin levels were markedly higher in CRC patients than in either HCs or BCP cases...
May 22, 2017: Journal of Clinical Laboratory Analysis
https://www.readbyqxmd.com/read/28543786/immunohistochemical-colocalization-of-g-protein-alpha-subunits-and-5-ht-in-the-rectal-gland-of-the-cartilaginous-fish-scyliorhinus-canicula
#14
E R Lauriano, S Pergolizzi, J Gangemi, M Kuciel, G Capillo, M Aragona, C Faggio
Serotonin [5-hydroxytryptamine (5-HT)] is an important neuromodulator involved in a wide range of physiological functions. The effects of serotonin are mediated by an extended family of receptors coupled to multiple heterotrimeric G-proteins, associated with cellular membrane. G proteins connect receptors to effectors and thus trigger intracellular signaling pathways. These cellular processes several regulate systemic functions such as embryonic development, gonadal development, learning and memory, and organismal homeostasis...
May 22, 2017: Microscopy Research and Technique
https://www.readbyqxmd.com/read/28543334/the-use-of-selective-serotonin-receptor-inhibitors-ssris-is-not-associated-with-increased-risk-of-endoscopy-refractory-bleeding-rebleeding-or-mortality-in-peptic-ulcer-bleeding
#15
S B Laursen, G I Leontiadis, A J Stanley, J Hallas, O B Schaffalitzky de Muckadell
BACKGROUND: Observational studies have consistently shown an increased risk of upper gastrointestinal bleeding in users of selective serotonin receptor inhibitors (SSRIs), probably explained by their inhibition of platelet aggregation. Therefore, treatment with SSRIs is often temporarily withheld in patients with peptic ulcer bleeding. However, abrupt discontinuation of SSRIs is associated with development of withdrawal symptoms in one-third of patients. Further data are needed to clarify whether treatment with SSRIs is associated with poor outcomes, which would support temporary discontinuation of treatment...
May 23, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28540658/overexpression-of-the-dyrk1a-gene-dual-specificity-tyrosine-phosphorylation-regulated-kinase-1a-induces-alterations-of-the-serotoninergic-and-dopaminergic-processing-in-murine-brain-tissues
#16
Jacqueline London, Claude Rouch, Linh Chi Bui, Elodie Assayag, Benoit Souchet, Fabrice Daubigney, Hind Medjaoui, Serge Luquet, Christophe Magnan, Jean Maurice Delabar, Julien Dairou, Nathalie Janel
Trisomy 21 (T21) or Down syndrome (DS) is the most common genetic disorder associated with intellectual disability and affects around 5 million persons worldwide. Neuroanatomical phenotypes associated with T21 include slight reduction of brain size and weight, abnormalities in several brain areas including spines dysgenesis, dendritic morphogenesis, and early neuroanatomical characteristics of Alzheimer's disease. Monoamine neurotransmitters are involved in dendrites development, functioning of synapses, memory consolidation, and their levels measured in the cerebrospinal fluid, blood, or brain areas that are modified in individuals with T21...
May 25, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28540034/ayahuasca-dimethyltryptamine-and-psychosis-a-systematic-review-of-human-studies
#17
REVIEW
Rafael G Dos Santos, José Carlos Bouso, Jaime E C Hallak
Ayahuasca is a hallucinogen brew traditionally used for ritual and therapeutic purposes in Northwestern Amazon. It is rich in the tryptamine hallucinogens dimethyltryptamine (DMT), which acts as a serotonin 5-HT2A agonist. This mechanism of action is similar to other compounds such as lysergic acid diethylamide (LSD) and psilocybin. The controlled use of LSD and psilocybin in experimental settings is associated with a low incidence of psychotic episodes, and population studies corroborate these findings. Both the controlled use of DMT in experimental settings and the use of ayahuasca in experimental and ritual settings are not usually associated with psychotic episodes, but little is known regarding ayahuasca or DMT use outside these controlled contexts...
April 2017: Therapeutic Advances in Psychopharmacology
https://www.readbyqxmd.com/read/28539956/serum-prolactin-levels-in-patients-with-major-depressive-disorder-receiving-selective-serotonin-reuptake-inhibitor-monotherapy-for-3-months-a-prospective-study
#18
Young-Min Park
OBJECTIVE: It is unclear whether selective serotonin-reuptake inhibitors (SSRIs) can significantly increase the prolactin level. The purpose of this study was to identify the relationship between the prolactin level and the administration of SSRIs such as escitalopram and sertraline. An additional purpose was to determine whether the elevation of prolactin differs between escitalopram and sertraline treatment. METHODS: Serum prolactin levels were measured at baseline and after 3 months in 23 patients who received SSRI monotherapy with escitalopram (n=18) (ESC group) or sertraline (n=5) (SERT group) for 3 months...
May 2017: Psychiatry Investigation
https://www.readbyqxmd.com/read/28539670/simvastatin-and-bezafibrate-ameliorate-emotional-disorder-induced-by-high-fat-diet-in-c57bl-6-mice
#19
Hui Wang, Jia Zhou, Qiong Zhen Liu, Lu Lu Wang, Jing Shang
High fat diet (HFD)-induced metabolic disorders may lead to emotional disorders. This study aimed to explore the effect of simvastatin (SMV) and bezafibrate (BZ) on improving HFD-induced emotional changes, and tried to identify their different mechanisms. The intraperitoneal glucose tolerance test (IPGTT) was used to evaluate glucose control ability; and behavior tests including open field tests (OFT), forced swimming tests (FST), tail suspension tests (TST) and sucrose preference (SPT), were then performed to evaluate emotional changes...
May 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28538871/what-do-cochrane-systematic-reviews-say-about-interventions-for-autism-spectrum-disorders
#20
Larissa Lyra, Luiz Eduardo Rizzo, Camila Sá Sunahara, Daniela Vianna Pachito, Carolina de Oliveira Cruz Latorraca, Ana Luiza Cabrera Martimbianco, Rachel Riera
CONTEXT AND OBJECTIVE: Autism spectrum disorders (ASDs) include autistic disorder, Asperger's disorder and pervasive developmental disorder. The manifestations of ASDs can have an important impact on learning and social functioning that may persist during adulthood. The aim here was to summarize the evidence from Cochrane systematic reviews on interventions for ASDs. DESIGN AND SETTING: Review of systematic reviews, conducted within the Discipline of Evidence-Based Medicine, Escola Paulista de Medicina, Universidade Federal de São Paulo...
March 2017: São Paulo Medical Journal, Revista Paulista de Medicina
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