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https://www.readbyqxmd.com/read/28213524/g-protein-coupled-receptor-kinase-2-grk-2-regulates-serotonin-metabolism-through-the-monoamine-oxidase-amx-2-in-caenorhabditis-elegans
#1
Jianjun Wang, Jiansong Luo, Dipendra K Aryal, William C Wetzel, Richard Nass, Jeffrey L Benovic
G protein-coupled receptors (GPCRs) regulate many animal behaviors. GPCR signaling is mediated by agonist-promoted interactions of GPCRs with heterotrimeric G proteins, GPCR kinases (GRKs) and arrestins. To further elucidate the role of GRKs in regulating GPCR-mediated behaviors, we utilized the genetic model system Caenorhabditis elegans. Our studies demonstrate that grk-2 loss-of-function strains are egg-laying defective and contain low levels of serotonin (5-HT) and high levels of the 5-HT metabolite 5-hydroxyindole acetic acid (5-HIAA)...
February 17, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28213183/a-role-for-the-serotonin-reuptake-transporter-in-the-brain-and-intestinal-features-of-autism-spectrum-disorders-and-developmental-antidepressant-exposure
#2
REVIEW
Kara Gross Margolis
Many disease conditions considered CNS-predominant harbor significant intestinal comorbidities. Serotonin (5-HT) and the serotonin reuptake transporter (SERT) have increasingly been shown to play important roles in both brain and intestinal development and long-term function. 5-HT and SERT may thus modulate critical functions in the development and perpetuation of brain-gut axis disease. We discuss the potential roles of 5-HT and SERT in the brain and intestinal manifestations of autism spectrum disorders and developmental antidepressant exposure...
February 14, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28212943/effects-of-acute-dopaminergic-and-serotonergic-manipulations-in-the-aci-paradigm-depend-on-the-basal-valence-of-cognitive-judgement-bias-in-rats
#3
Joanna Golebiowska, Rafal Rygula
Recent findings have revealed that pharmacological enhancement of dopaminergic (DA) function by the administration of a DA precursor (dihydroxy-L-phenylalanine; L-DOPA), but not the selective serotonin reuptake inhibitor (SSRI) citalopram, increases an optimism bias in humans. To test whether dopamine might play a similar role in non-human animals, in the present study, we evaluated the effects of acute injections of L-DOPA, the D2 receptor antagonist haloperidol, and the SSRI escitalopram on cognitive judgement bias of rats in the ambiguous-cue interpretation (ACI) paradigm...
February 14, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28212884/desipramine-decreases-expression-of-human-and-murine-indoleamine-2-3-dioxygenases
#4
Alexandra K Brooks, Tiffany M Janda, Marcus A Lawson, Jennifer L Rytych, Robin A Smith, Cecilia Ocampo-Solis, Robert H McCusker
Abundant evidence connects depression symptomology with immune system activation, stress and subsequently elevated levels of kynurenine. Anti-depressants, such as the tricyclic norepinephrine/serotonin reuptake inhibitor desipramine (Desip), were developed under the premise that increasing extracellular neurotransmitter level was the sole mechanism by which they alleviate depressive symptomologies. However, evidence suggests that anti-depressants have additional actions that contribute to their therapeutic potential...
February 14, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28212021/discovery-and-development-of-1-2-bromophenyl-sulfonyl-5-methoxy-3-4-methyl-1-piperazinyl-methyl-1h-indole-dimesylate-monohydrate-suvn-502-a-novel-potent-selective-and-orally-active-serotonin-6-5-ht6-receptor-antagonist-for-potential-treatment-of-alzheimer-s
#5
Ramakrishna Nirogi, Anil Shinde, Rama Sastry Kambhampati, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Rajesh Kumar Badange, Thrinath Reddy Bandyala, Venugopalarao Bhatta, Kumar Bojja, Veena Reballi, Ramkumar Subramanian, Vijay Benade, Raghava Choudary Palacharla, Gopinadh Bhyrapuneni, Pradeep Jayarajan, Vinod Goyal, Venkat Jasti
Optimization of a novel series of 3-(piperazinylmethyl) indole derivatives as 5-hydroxytryptamine-6 receptor (5-HT6R) antagonists resulted in identification of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate (5al, SUVN-502) as a clinical candidate for potential treatment of cognitive disorders. It has high affinity at human 5-HT6R (Ki = 2.04 nM) and selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins...
February 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28211304/granisetron-and-carvedilol-can-protect-experimental-rats-againstadjuvant-induced-arthritis
#6
Yasmin Moustafa Ahmed, Basim Anwar Shehata Messiha, Ali Ahmed Abo-Saif
CONTEXT: Rheumatoid arthritis (RA), a disabling autoimmune disorder of the joints as well as other organs, affects about 1% of population. Unfortunately, all current treatments of RA cause severe gastrointestinal, renal and other complications. OBJECTIVE: We aimed to evaluate the possible antiarthritic effects of a serotonin 5-HT3 receptor blocker, granisetron, and a nonselective adrenergic receptor blocker, carvedilol, on complete Freund's adjuvant-induced RA in adult female albino rats...
April 2017: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/28210931/serotonin-syndrome-from-5-hydroxytryptophan-supplement-ingestion-in-a-9-month-old-labrador-retriever
#7
Hopkins Jennifer, Pardo Mariana, Bischoff Karyn
INTRODUCTION: 5-Hydroxytryptophan (5-HTP) supplements are available over the counter and labeled as sleeping aids and anxiolytics for human use. 5-HTP is a serotonin precursor and overdose can lead to serotonin syndrome. CASE REPORT: A 9-month-old female Labrador retriever was evaluated after ingestion of a 5-HTP supplement. Signs of agitation developed within 1 h of ingestion, and emesis was attempted by the owner with  3% hydrogen peroxide (H2O2) orally. On presentation, the dog was obtunded, bilaterally mydriatic and salivating...
February 16, 2017: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
https://www.readbyqxmd.com/read/28210777/effects-of-biperiden-and-acute-tryptophan-depletion-and-their-combination-on-verbal-word-memory-and-eeg
#8
Laura G J M Borghans, Arjan Blokland, Anke Sambeth
BACKGROUND: Research on the neurobiological foundations of memory has shown that multiple neurotransmitters play an important role in memory processing. To study the interaction between neurotransmitters such as acetylcholine and serotonin, pharmacological models can be used. In this study, we tested the effects of the muscarinic M1 antagonist biperiden, acute tryptophan depletion (ATD), and the interaction between the two on episodic memory using the verbal learning task. METHODS: The study was conducted according to a double-blind, placebo-controlled, four-way crossover design...
February 16, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28209599/role-of-shp2-protein-tyrosine-phosphatase-in-sert-inhibition-by-enteropathogenic-e-coli-epec
#9
Megha Singhal, Christopher Manzella, Vinay Soni, Waddah A Alrefai, Seema Saksena, Gail A Hecht, Pradeep K Dudeja, Ravinder K Gill
Enteropathogenic E. coli (EPEC), one of the diarrheagenic E. coli pathotypes, is among the most important food-borne pathogens infecting children worldwide. Inhibition of serotonin transporter (SERT), that regulates extracellular availability of serotonin (5-HT), has been previously implicated in EPEC-associated diarrhea. EPEC was shown to inhibit SERT via activation of protein tyrosine phosphatases (PTPase), albeit the specific PTPase involved is not known. Current studies aimed to identify EPEC activated PTPase and its role in SERT inhibition...
February 16, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28209485/effects-of-clozapine-on-adipokine-secretions-productions-and-lipid-droplets-in-3t3-l1-adipocytes
#10
Tomomi Tsubai, Akira Yoshimi, Yoji Hamada, Makoto Nakao, Hiroshi Arima, Yutaka Oiso, Yukihiro Noda
Clozapine, a second-generation antipsychotic (SGA), is a cause of side effects related to metabolic syndrome. The participation of serotonin 5-HT2C and histamine H1 receptors in the central nervous system has been reported as a mechanism of the weight gain caused by clozapine. In the present study, we investigated the direct pharmacological action of clozapine on the 3T3-L1 adipocytes and compared it to that of blonanserin, an SGA with low affinity for both receptors. Short-term exposure to clozapine decreased secretion and mRNA expression of leptin...
January 28, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28208023/transcriptomic-profiling-of-human-hippocampal-progenitor-cells-treated-with-antidepressants-and-its-application-in-drug-repositioning
#11
Timothy R Powell, Tytus Murphy, Sang H Lee, Jack Price, Sandrine Thuret, Gerome Breen
Current pharmacological treatments for major depressive disorder (MDD) are ineffective in a significant proportion of patients, and the identification of new antidepressant compounds has been difficult. 'Connectivity mapping' is a method that can be used to identify drugs that elicit similar downstream effects on mRNA levels when compared to current treatments, and thus may point towards possible repositioning opportunities. We investigated genome-wide transcriptomic changes to human hippocampal progenitor cells treated with therapeutically relevant concentrations of a tricyclic antidepressant (nortriptyline) and a selective serotonin reuptake inhibitor (escitalopram)...
January 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28208011/glucosylsphingosine-activates-serotonin-receptor-2a-and-2b-implication-of-a-novel-itch-signaling-pathway
#12
Ramsha Afzal, Won-Sik Shim
Recent reports claimed that glucosylsphingosine (GS) is highly accumulated and specifically evoking itch-scratch responses in the skins of atopic dermatitis (AD) patients. However, it was unclear how GS can trigger itch-scratch responses, since there were no known molecular singling pathways revealed yet. In the present study, it was verified for the first time that GS can activate mouse serotonin receptor 2a (mHtr2a) and 2b (mHtr2b), but not 2c (mHtr2c) that are expressed in HEK293T cells. Specifically, effects of GS on all mouse serotonin receptor 2 subfamily were evaluated by calcium imaging techniques...
February 17, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28207733/beyond-negative-valence-2-week-administration-of-a-serotonergic-antidepressant-enhances-both-reward-and-effort-learning-signals
#13
Jacqueline Scholl, Nils Kolling, Natalie Nelissen, Michael Browning, Matthew F S Rushworth, Catherine J Harmer
To make good decisions, humans need to learn about and integrate different sources of appetitive and aversive information. While serotonin has been linked to value-based decision-making, its role in learning is less clear, with acute manipulations often producing inconsistent results. Here, we show that when the effects of a selective serotonin reuptake inhibitor (SSRI, citalopram) are studied over longer timescales, learning is robustly improved. We measured brain activity with functional magnetic resonance imaging (fMRI) in volunteers as they performed a concurrent appetitive (money) and aversive (effort) learning task...
February 2017: PLoS Biology
https://www.readbyqxmd.com/read/28205278/optimal-dose-of-ramosetron-in-female-patients-with-irritable%C3%A2-bowel-syndrome-with-diarrhea-a-randomized-placebo-controlled-phase-ii-study
#14
S Fukudo, K Matsueda, K Haruma, M Ida, H Hayase, H Akiho, Y Nakashima, M Hongo
BACKGROUND: Previous studies showed that 5 μg of ramosetron, a serotonin (5-hydroxytryptamine: 5-HT)-3 receptor antagonist, is only effective in male patients with irritable bowel syndrome (IBS) with diarrhea (IBS-D). We hypothesized that either dose 1.25, 2.5, or 5 μg of ramosetron would be effective in female patients with IBS-D. METHODS: This randomized, double-blind, placebo-controlled, phase II dose-finding exploratory trial included 409 female outpatients with IBS-D treated in Japan...
February 16, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28203264/a-pilot-study-exploring-the-association-of-morphological-changes-with-5-httlpr-polymorphism-in-ocd-patients
#15
Shinichi Honda, Tomohiro Nakao, Hiroshi Mitsuyasu, Kayo Okada, Leo Gotoh, Mayumi Tomita, Hirokuni Sanematsu, Keitaro Murayama, Keisuke Ikari, Masumi Kuwano, Takashi Yoshiura, Hiroaki Kawasaki, Shigenobu Kanba
BACKGROUND: Clinical and pharmacological studies of obsessive-compulsive disorder (OCD) have suggested that the serotonergic systems are involved in the pathogenesis, while structural imaging studies have found some neuroanatomical abnormalities in OCD patients. In the etiopathogenesis of OCD, few studies have performed concurrent assessment of genetic and neuroanatomical variables. METHODS: We carried out a two-way ANOVA between a variable number of tandem repeat polymorphisms (5-HTTLPR) in the serotonin transporter gene and gray matter (GM) volumes in 40 OCD patients and 40 healthy controls (HCs)...
2017: Annals of General Psychiatry
https://www.readbyqxmd.com/read/28203201/modulation-of-synaptic-plasticity-in-the-cortex-needs-to-understand-all-the-players
#16
REVIEW
Claire N J Meunier, Pascal Chameau, Philippe M Fossier
The prefrontal cortex (PFC) is involved in cognitive tasks such as working memory, decision making, risk assessment and regulation of attention. These functions performed by the PFC are supposed to rely on rhythmic electrical activity generated by neuronal network oscillations determined by a precise balance between excitation and inhibition balance (E/I balance) resulting from the coordinated activities of recurrent excitation and feedback and feedforward inhibition. Functional alterations in PFC functions have been associated with cognitive deficits in several pathologies such as major depression, anxiety and schizophrenia...
2017: Frontiers in Synaptic Neuroscience
https://www.readbyqxmd.com/read/28203149/gene-gene-environment-interactions-of-serotonin-transporter-monoamine-oxidase-a-and-childhood-maltreatment-predict-aggressive-behavior-in-chinese-adolescents
#17
Yun Zhang, Qing-Sen Ming, Jin-Yao Yi, Xiang Wang, Qiao-Lian Chai, Shu-Qiao Yao
Gene-environment interactions that moderate aggressive behavior have been identified independently in the serotonin transporter (5-HTT) gene and monoamine oxidase A gene (MAOA). The aim of the present study was to investigate epistasis interactions between MAOA-variable number tandem repeat (VNTR), 5-HTTlinked polymorphism (LPR) and child abuse and the effects of these on aggressive tendencies in a group of otherwise healthy adolescents. A group of 546 Chinese male adolescents completed the Child Trauma Questionnaire and Youth self-report of the Child Behavior Checklist...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28202410/atypical-antipsychotic-clozapine-reversed-deficit-on-prepulse-inhibition-of-the-acoustic-startle-reflex-produced-by-microinjection-of-doi-into-the-inferior-colliculus-in-rats
#18
Rodolpho Pereira de Oliveira, Karen Yuriko Nagaishi, Regina Cláudia Barbosa Silva
Dysfunctions of the serotonergic system have been suggested to be important in the neurobiology of schizophrenia. Patients with schizophrenia exhibit deficits in an operational measure of sensorimotor gating: prepulse inhibition (PPI) of startle. PPI is the normal reduction in the startle response caused by a low intensity non-startling stimulus (prepulse) which is presented shortly before the startle stimulus (pulse). The hallucinogen 2,5-dimethoxy-4-iodoamphetamine (DOI), a 5-hydroxytryptamine(HT)2 receptor agonist disrupted PPI in rats...
February 12, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28199430/-posttraumatic-stress-disorder-conceptualization-and-psychopharmacological-treatment-update
#19
Leandro N Grendas
Posttraumatic stress disorder (PTSD) is characterized by four symptom complexes: the reexperience/intrusion of the traumatic event, a state of hyperarousal when exposed to traumatic events, emotional block and emotional/affective deregulation with negative cognitive and mood alterations. Its evolution tends to be chronic and its related with a significative morbidity, affecting the functionality of the individual in his interpresonal, social and employment areas. In 1980, the American Psychiatric Association includes PTSD in the third edition of the Diagnostic and Statistical Manual of Mental Disorders (DSM-III), and thereafter several research studies are developed to evaluate the effectiveness of drugs on its treatment...
March 2016: Vertex: Revista Argentina de Psiquiatriá
https://www.readbyqxmd.com/read/28198797/erratum-risk-of-prenatal-depression-and-stress-treatment-alteration-on-serotonin-system-of-offspring-through-exposure-to-fluoxetine
#20
Siran Pei, Li Liu, Zhaomin Zhong, Han Wang, Shuo Lin, Jing Shang
No abstract text is available yet for this article.
February 13, 2017: Scientific Reports
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