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https://www.readbyqxmd.com/read/28088578/the-effect-of-long-term-hindlimb-unloading-on-the-expression-of-risk-neurogenes-encoding-elements-of-serotonin-dopaminergic-systems-and-apoptosis-comparison-with-the-effect-of-actual-spaceflight-on-mouse-brain
#1
E A Kulikova, V A Kulikov, N A Sinyakova, A V Kulikov, N K Popova
The study of spaceflight effects on the brain is technically complex concern; complicated by the problem of applying an adequate ground model. The most-widely used experimental model to study the effect of microgravity is the tail-suspension hindlimb unloading model; however, its compliance with the effect of actual spaceflight on the brain is still unclear. We evaluated the effect of one month hindlimb unloading on the expression of genes related to the brain neuroplasticity - brain neutotrophic factors (Gdnf, Cdnf), apoptotic factors (Bcl-xl, Bax), serotonin- and dopaminergic systems (5-HT2A, Maoa, Maob, Th, D1r, Comt), and compared the results with the data obtained on mice that spent one month in spaceflight on Russian biosatellite Bion-M1...
January 11, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28087766/control-of-amygdala-circuits-by-5-ht-neurons-via-5-ht-and-glutamate-co-transmission
#2
Ayesha Sengupta, Marco Bocchio, David M Bannerman, Trevor Sharp, Marco Capogna
: The serotonin (5-HT) system and the amygdala are key regulators of emotional behavior. Several lines of evidence suggest that 5-HT transmission in the amygdala is implicated in the susceptibility and drug treatment of mood disorders. Thus, elucidating the physiological mechanisms through which midbrain 5-HT neurons modulate amygdala circuits could be pivotal in understanding emotional regulation in health and disease. To shed light on these mechanisms, we performed patch-clamp recordings from basal amygdala (BA) neurons in brain slices from mice with channelrhodopsin (ChR2) genetically targeted to 5-HT neurons...
January 13, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28076854/open-angle-glaucoma-drug-development-pipeline-during-the-last-20-years-1995-2015
#3
André Vicente, Sylvie Prud'homme, Joana Ferreira, Luís Abegão Pinto, Ingeborg Stalmans
OBJECTIVES: To analyse drug development for open-angle glaucoma during the last 20 years. METHODS: Research was performed by referring to clinical trials registered at the International Clinical Trials Registry Platform (ICTRP). A search for the condition "open-angle glaucoma" with the intervention "drug" was performed. We included trials registered from 01/01/1995 to 01/01/2015, only involving studies in phases 1, 2, and 3. Only studies resorting to novel treatment strategies (either novel drugs or yet-untested fixed associations of approved medication) were considered...
January 12, 2017: Ophthalmic Research
https://www.readbyqxmd.com/read/28072812/is-kratom-the-new-legal-high-on-the-block-the-case-of-an-emerging-opioid-receptor-agonist-with-substance-abuse-potential
#4
George C Chang-Chien, Charles A Odonkor, Prin Amorapanth
Kratom is an unscheduled opioid receptor agonist that comes in the form of dietary supplements currently being abused by chronic pain patients on prescription opioids. Active alkaloids isolated from kratom such as mitragynine and 7-hydroxymitragynine are thought to act on mu- and delta-opioid receptors as well as alpha-2 adrenergic and 5-HT2A receptors. Animal studies suggest that kratom may be more potent than morphine. Consequently, kratom consumption produces analgesic and euphoric feelings among users. In particular, some chronic pain patients on opioids take kratom to counteract the effects of opioid withdrawal...
January 2017: Pain Physician
https://www.readbyqxmd.com/read/28068560/effect-of-sarpogrelate-a-selective-5-ht2a-receptor-antagonist-on-characteristics-of-coronary-artery-disease-in-patients-with-type-2-diabetes
#5
Dong-Hwa Lee, Eun Ju Chun, Jee Hye Hur, Se Hee Min, Jie-Eun Lee, Tae Jung Oh, Kyoung Min Kim, Hak Chul Jang, Seung Jin Han, Doo Kyoung Kang, Hae Jin Kim, Soo Lim
BACKGROUND AND AIMS: Sarpogrelate, a 5-hydroxytryptamine type 2A antagonist, is a potential antiplatelet agent. We performed a randomized study to evaluate the effect of sarpogrelate on vascular health in Korean patients with diabetes. METHODS: Forty diabetic patients aged 58.6 ± 6.8 years with 10-75% coronary artery stenosis, as assessed by coronary computed tomography angiography, were randomly assigned to sarpogrelate 300 mg/day plus aspirin 100 mg/day (SPG + ASA group) or aspirin 100 mg/day alone (ASA group) for 6 months...
December 10, 2016: Atherosclerosis
https://www.readbyqxmd.com/read/28063918/simultaneous-in-vivo-receptor-occupancy-assays-for-serotonin-1a-2a-and-dopamine-2-receptors-with-the-use-of-non-radiolabelled-tracers-proposed-method-in-screening-antipsychotics
#6
Jagadeesh Babu Thentu, Ramakrishna Nirogi, Gopinadh Bhyrapuneni, Devender Reddy Ajjala, Raghupathi Reddy Aleti, Veera Raghava Choudary Palacharla
INTRODUCTION: Conventionally, receptor occupancy assays employ radiolabelled tracer.However, recent advances with non-radiolabelled tracers brought a revolution in target engagement assays.Non-radiolabelled tracer based receptor occupancy uses LC-MS/MS based quantification.It offers simultaneous quantification of more than one tracer; thus, provides the feasibility of evaluating multiple targets in a single animal.In the present study, we demonstrated simultaneous measurement of serotonin 1A, serotonin 2A, and dopamine 2 receptor occupancy using non-radiolabelled tracers in rats...
January 4, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28059046/long-term-effects-of-aripiprazole-exposure-on-monoaminergic-and-glutamatergic-receptor-subtypes-comparison-with-cariprazine
#7
Yong Kee Choi, Nika Adham, Béla Kiss, István Gyertyán, Frank I Tarazi
OBJECTIVE: This study examined the chronic effects of aripiprazole and cariprazine on serotonin (5-HT1A and 5-HT2A) and glutamate (NMDA and AMPA) receptor subtypes. In addition, the effects of aripiprazole on D2 and D3 receptors were tested and compared with previously reported cariprazine data. METHODS: Rats received vehicle, aripiprazole (2, 5, or 15 mg/kg), or cariprazine (0.06, 0.2, or 0.6 mg/kg) for 28 days. Receptor levels were quantified using autoradiographic assays on brain sections from the medial prefrontal cortex (MPC), dorsolateral frontal cortex (DFC), nucleus accumbens (NAc), caudate-putamen medial (CPu-M), caudate-putamen lateral (CPu-L), hippocampal CA1 (HIPP-CA1) and CA3 (HIPP-CA3) regions, and the entorhinal cortex (EC)...
January 6, 2017: CNS Spectrums
https://www.readbyqxmd.com/read/28057524/involvement-of-presynaptic-5-ht1a-receptors-in-the-low-propensity-of-brexpiprazole-to-induce-extrapyramidal-side-effects-in-rats
#8
Cedric Mombereau, Jørn Arnt, Arne Mørk
Previous studies have shown that partial and full 5-HT1A receptor agonists reduce antipsychotic-induced catalepsy. Consequently, some antipsychotics combining balanced efficacy between dopamine (DA) D2 antagonism or partial agonism and 5-HT1A receptor agonism have a low propensity to induce extrapyramidal side effects (EPS), as reflected by low cataleptogenic activity in rodents. In the present experiments, we attempted to explore the importance of pre- and postsynaptic 5-HT1A agonistic properties of brexpiprazole and aripiprazole in the context of neurological side-effect liabilities...
January 3, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28057087/sleep-homeostatic-and-waking-behavioral-phenotypes-in-egr3-deficient-mice-associated-with-serotonin-receptor-5-ht2-deficits
#9
Janne Grønli, William C Clegern, Michelle A Schmidt, Rahmi S Nemri, Michael J Rempe, Amelia L Gallitano, Jonathan P Wisor
STUDY OBJECTIVE: The expression of the immediate early gene early growth response 3 (Egr3) is a functional marker of brain activity including responses to novelty, sustained wakefulness, and sleep. We examined the role of this gene in regulating wakefulness and sleep. METHODS: Electroencephalogram/electromyogram (EEG/EMG) were recorded in Egr3-/- and wild-type (WT) mice during 24 h baseline, 6 h sleep disruption and 6 h recovery. Serotonergic signaling was assessed with 6 h EEG/EMG recordings after injections of nonselective 5-HT2 antagonist (clozapine), selective 5-HT2 antagonists (5-HT2A; MDL100907 and 5-HT2BC; SB206553) and a cocktail of both selective antagonists, administered in a randomized order to each animal...
December 1, 2016: Sleep
https://www.readbyqxmd.com/read/28053817/pretreatment-with-ginseng-fruit-saponins-affects-serotonin-expression-in-an-experimental-comorbidity-model-of-myocardial-infarction-and-depression
#10
Mei-Yan Liu, Yan-Ping Ren, Li-Jun Zhang, Jamie Y Ding
We previously demonstrated that serotonin (5-HT) and 5-HT2A receptor (5-HT2AR) levels in platelets were up- or down-regulated after myocardial infarction (MI) associated with depression. In this study, we further evaluated the effects of pretreatment with ginseng fruit saponins (GFS) on the expression of 5-HT and 5-HT2AR in MI with or without depression. Eighty Sprague-Dawley (SD) rats were treated with saline and GFS (n=40 per group). The animals were then randomly divided into four subgroups: sham, MI, depression, and MI + depression (n=10 per subgroup)...
December 2016: Aging and Disease
https://www.readbyqxmd.com/read/28053035/a-high-resolution-in-vivo-atlas-of-the-human-brain-s-serotonin-system
#11
Vincent Beliveau, Melanie Ganz, Ling Feng, Brice Ozenne, Liselotte Højgaard, Patrick M Fisher, Claus Svarer, Douglas N Greve, Gitte M Knudsen
: The serotonin (5-hydroxytryptamine, 5-HT) system modulates many important brain functions and is critically involved in many neuropsychiatric disorders. Here, we present a high-resolution, multidimensional, in vivo atlas of four of the human brain's 5-HT receptors (5-HT1A, 5-HT1B, 5-HT2A, and 5-HT4) and the 5-HT transporter (5-HTT). The atlas is created from molecular and structural high-resolution neuroimaging data consisting of positron emission tomography (PET) and magnetic resonance imaging (MRI) scans acquired in a total of 210 healthy individuals...
January 4, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28043245/-association-between-5-hydroxytryptamine-2a-receptor-gene-polymorphisms-and-susceptibility-to-occupational-stress-in-oilfield-workers
#12
Y Jiang, Abudoureyimu Palizhati, X Y Gao, S Z Guan, J W Liu
Objective: To investigate the association between 5-hydroxytryptamine 2A (5-HT2A) receptor gene polymorphisms and occupational stress in oilfield workers. Methods: Cluster sampling was used to select 826 oilfield workers from January to August, 2013. The SNaPshot single nucleotide polymorphism (SNP) genotyping method was used to determine the genotypes of rs6313, rs1923884, and rs2070040 in 5-HT2A receptor gene, and the Occupational Stress Inventory-Revised Edition was used to analyze occupational stress in these workers...
October 20, 2016: Chinese Journal of Industrial Hygiene and Occupational Diseases
https://www.readbyqxmd.com/read/28043241/-influence-of-occupational-stress-and-5-hydroxytryptamine-2a-receptor-gene-polymorphisms-on-depression-in-workers-in-a-thermal-power-plant
#13
H Wu, F F Wang, W H Zhou, G Z Gu, S F Yu
Objective: To investigate the association of occupational stress and 5-hydroxytryptamine 2A (5-HT2A) receptor gene polymorphisms with depression. Methods: In November 2010, cluster sampling was used to select 589 workers in a thermal power plant as study subjects. Questionnaires were used to investigate demographic features and occupational stressors. Polymerase chain reaction-restriction fragment length polymorphism was used to detect the genotypes of T102C and A-1438G in 5-HT2A receptor gene in 589 workers...
October 20, 2016: Chinese Journal of Industrial Hygiene and Occupational Diseases
https://www.readbyqxmd.com/read/28034961/role-of-prefrontal-serotonergic-and-dopaminergic-systems-in-encounter-induced-hyperactivity-in-methamphetamine-sensitized-mice
#14
Tatsunori Tanaka, Yukio Ago, Chiaki Umehara, Emina Imoto, Shigeru Hasebe, Hitoshi Hashimoto, Kazuhiro Takuma, Toshio Matsuda
BACKGROUND: Isolation-reared mice show social encounter-induced hyperactivity with activation of prefrontal serotonergic and dopaminergic systems, but it is not known whether this stress response is observed in other pathological conditions. Here we examined whether the social encounter stimulation induces abnormal behavior during withdrawal in chronic methamphetamine (METH)-treated mice. METHODS: To induce METH-induced behavioral sensitization, male mice were injected with METH (1 mg/kg) once daily for 7 days...
December 29, 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28029458/design-and-synthesis-of-novel-n-sulfonyl-2-indoles-that-behave-as-5-ht6-receptor-ligands-with-significant-selectivity-for-d3-over-d2-receptors
#15
Oscar M Saavedra, Delphine Karila, Dominique Brossard, Anne Rojas, Delphine Dupuis, Arnaud Gohier, Clotilde Mannoury la Cour, Mark J Millan, Jean-Claude Ortuno, Stephen Hanessian
All clinically-used antipsychotics display similar affinity for both D2 (D2R) and D3 (D3R) receptors, and they likewise act as 5-HT2A receptor antagonists. They provide therapeutic benefit for positive symptoms, but no marked or consistent improvement in neurocognitive, social cognitive or negative symptoms. Since blockade of D3 and 5-HT6 (5-HT6R) receptors enhances neurocognition and social cognition, and potentially improves negative symptoms, a promising approach for improved treatment for schizophrenia would be to develop drugs that preferentially act at D3R versus D2R and likewise recognize 5-HT6R...
October 12, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28019026/psychedelics-as-medicines-an-emerging-new-paradigm
#16
D E Nichols, M W Johnson, C D Nichols
Scientific interest in serotonergic psychedelics (e.g., psilocybin and LSD; 5-HT2A receptor agonists) has dramatically increased within the last decade. Clinical studies administering psychedelics with psychotherapy have shown preliminary evidence of robust efficacy in treating anxiety and depression, as well as addiction to tobacco and alcohol. Moreover, recent research has suggested that these compounds have potential efficacy against inflammatory diseases through novel mechanisms, with potential advantages over existing antiinflammatory agents...
November 4, 2016: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28017279/cardiovascular-remodeling-and-the-peripheral-serotonergic-system
#17
REVIEW
Estelle Ayme-Dietrich, Gaëlle Aubertin-Kirch, Luc Maroteaux, Laurent Monassier
Plasma 5-hydroxytryptamine (5-HT; serotonin), released from blood platelets, plays a major role in the human cardiovascular system. Besides the effect of endogenous serotonin, many drugs targeting serotonergic receptors are widely used in the general population (antiobesity agents, antidepressants, antipsychotics, antimigraine agents), and may enhance the cardiovascular risk. Depending on the type of serotonin receptor activated and its location, the use of these compounds triggers acute and chronic effects...
December 21, 2016: Archives of Cardiovascular Diseases
https://www.readbyqxmd.com/read/28004950/stimulation-of-5-ht2a-receptors-recovers-sensory-responsiveness-in-acute-spinal-neonatal-rats
#18
Hillary E Swann, Sierra D Kauer, Jacob T Allmond, Michele R Brumley
Quipazine is a 5-HT2A-receptor agonist that has been used to induce motor activity and promote recovery of function after spinal cord injury in neonatal and adult rodents. Sensory stimulation also activates sensory and motor circuits and promotes recovery after spinal cord injury. In rats, tail pinching is an effective and robust method of sacrocaudal sensory afferent stimulation that induces motor activity, including alternating stepping. In this study, responsiveness to a tail pinch following treatment with quipazine (or saline vehicle control) was examined in spinal cord transected (at midthoracic level) and intact neonatal rats...
December 22, 2016: Behavioral Neuroscience
https://www.readbyqxmd.com/read/27999378/effect-of-5-ht2a-receptor-polymorphisms-work-stressors-and-social-support-on-job-strain-among-petroleum-workers-in-xinjiang-china
#19
Yu Jiang, Jinhua Tang, Rong Li, Junling Zhao, Zhixin Song, Hua Ge, Yulong Lian, Jiwen Liu
Previous studies have shown that work stressors and social support influence job strain. However, few studies have examined the impact of individual differences on job strain. In Xinjiang, there are a large number of petroleum workers in arid deserts. The present study investigated the effects of work stressors, social support, and 5-hydroxytryptamine receptor (5-HTR2A) genotype on the etiology of job strain among petroleum workers in Xinjiang. A cross-sectional study was carried out between January and August 2013...
December 19, 2016: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/27994633/electroacupuncture-restores-5-ht-system-deficit-in-chronic-mild-stress-induced-depressed-rats
#20
Dongmei Duan, Ya Tu, Xiuyan Yang, Ping Liu
Objective. The current study is designed to investigate the antidepressant efficacy of electroacupuncture (EA) treatment by evaluating its effect on the synthesis, metabolism, reuptake, and receptors of 5-hydroxytryptamine (5-HT), so as to clarify the molecular mechanisms of EA for antidepression. Materials and Methods. Solitary combined with the chronic unpredictable mild stress (CUMS) was used to establish the rat model with depression. The depressed rats were supplied with EA treatment for 4 weeks, and the behavior change and the following indices including 5-HT, 5-hydroxyindoleacetic acid (5-HIAA), monoamine oxidase A (MAO-A), tryptophan hydroxylase (TPH), 5-HT transporter (SERT), 5-HT1A, and 5-HT2A in hippocampus and prefrontal cortex were examined...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
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