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5 HT receptors

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https://www.readbyqxmd.com/read/29778944/activation-and-blockade-of-basolateral-amygdala-5-ht-6-receptor-produce-anxiolytic-like-behaviors-in-an-experimental-model-of-parkinson-s-disease
#1
Yi-Na Sun, Lu Yao, Li-Bo Li, Yong Wang, Cheng-Xue Du, Yuan Guo, Jian Liu
Although the basolateral amygdala (BLA) and serotonin6 (5-HT6 ) receptor are involved in modulation of anxiety, their roles in Parkinson' disease (PD)-related anxiety are still unknown. Thus we perform this study to examine the involvement of BLA 5-HT6 receptor on anxiety in unilateral 6-hydroxydopamine-induced PD rats. The lesion of the medial forebrain bundle (MFB) induced anxiety-like behaviors, and decreased the basal firing rate of BLA glutamate neurons and dopamine (DA) levels in tissues of the medial prefrontal cortex (mPFC), amygdala and ventral part of hippocampus (vHip) in rats...
May 17, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29775777/antidepressant-potential-of-novel-flavonoids-derivatives-from-sweet-violet-viola-odorata-l-pharmacological-biochemical-and-computational-evidences-for-possible-involvement-of-serotonergic-mechanism
#2
Nasiara Karim, Imran Khan, Abeer Abdelhalim, Ajmal Khan, Sobia Ahsan Halim
Plant-derived natural constituents are of great interest in modern drug discovery due to their natural diversity. Viola odorata L has been traditionally used for the treatment of neuropsychiatric disorders. The present study was undertaken to isolate phytoconstituents including three flavonoids 5,7-Dihydroxy-3,6-dimethoxyflavone[1] 5,7,4'-trihydroxy-3',5'dimethoxyflavone [2] and 5,7,4'-trihydroxy-3'-methoxyflavone [3] from the whole plant of Viola odorata L and to investigate the antidepressant-like effects of these compounds and their possible mechanism of action using antagonists of the serotonergic, dopaminergic and adrenergic system...
May 15, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29775613/suppression-of-nlrp3-inflammasome-attenuates-stress-induced-depression-like-behavior-in-nlgn3-deficient-mice
#3
Ze-Qun Li, Zhi-Yuan Yan, Bo-Jun Lan, Yi-Qun Dong, Ye Xiong
Depression, regulated by central nervous system (CNS), is a significant inflammatory disorder. Neuroligin3 (NLGN3) has been implicated in brain functions. In the study, a chronic unpredictable mild stress (CUMS) model in wild type (WT) or NLGN3-knockout (KO) mice was established to explore the role of NLGN3 in regulating depression and to reveal the underlying molecular mechanism. The results indicated that NLGN3-knockout markedly reversed the loss of body weight, the reduction of sucrose consumption, the decrease of immobile time in the forced swimming tests (FST) and tail suspension tests (TST) induced by CUMS paradigm...
May 15, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29764208/de-esterified-tragacanth-chitosan-nano-hydrogel-for-methotrexate-delivery-optimization-of-the-formulation-by-taguchi-design
#4
Komail Sadrjavadi, Behzad Shahbazi, Ali Fattahi
The objective of the present study was to prepare and characterized de-esterified tragacanth-chitosan nanoparticles (DET-CS NPs) as a novel carrier for methotrexate, with a view to improve drug efficacy and target ability. The preparation process was optimized using Taguchi design. NPs were characterized for size, zeta potential, morphology, thermal stability, loading efficiency, cytotoxicity and cellular uptake. Taguchi design indicated that the molecular weight of chitosan possessed the most effect on the zeta potential, PDI, and zeta deviation, and the size of nanoparticles was significantly affected by the DET concentration...
May 15, 2018: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29762664/behavioral-and-serotonergic-changes-in-the-frontal-cortex-following-methamphetamine-self-administration
#5
Lisa M McFadden, Rebecca Cordie, Tamee Livermont, Andrew Johansen
Background: Methamphetamine (METH) use is associated with a variety of negative health outcomes including psychosis. The frontal cortex serotonin (5-HT)-2 receptors are thought to contribute to psychosis-like behaviors. This study investigated changes in serotonergic markers in the frontal cortex following METH self-administration and hallucinogenic drug-induced behavior. Methods: Consistent with previously published studies, freely-cycling male and female rats were allowed to self-administer METH (Males: 0...
May 14, 2018: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29754752/hippocampal-5-ht-input-regulates-memory-formation-and-schaffer-collateral-excitation
#6
Catia M Teixeira, Zev B Rosen, Deepika Suri, Qian Sun, Marc Hersh, Derya Sargin, Iva Dincheva, Ashlea A Morgan, Stephen Spivack, Anne C Krok, Tessa Hirschfeld-Stoler, Evelyn K Lambe, Steven A Siegelbaum, Mark S Ansorge
The efficacy and duration of memory storage is regulated by neuromodulatory transmitter actions. While the modulatory transmitter serotonin (5-HT) plays an important role in implicit forms of memory in the invertebrate Aplysia, its function in explicit memory mediated by the mammalian hippocampus is less clear. Specifically, the consequences elicited by the spatio-temporal gradient of endogenous 5-HT release are not known. Here we applied optogenetic techniques in mice to gain insight into this fundamental biological process...
May 8, 2018: Neuron
https://www.readbyqxmd.com/read/29752984/antinociceptive-effects-of-the-antidepressant-phenelzine-are-mediated-by-context-dependent-inhibition-of-neuronal-responses-in-the-dorsal-horn
#7
Liam E Potter, Suzanne Doolen, Katherine Mifflin, Gustavo Tenorio, Glen Baker, Bradley K Taylor, Bradley J Kerr
The putative strong anti-nociceptive properties of the antidepressant phenelzine (PLZ) have not been widely explored as a treatment for pain. Antinociceptive effects of PLZ were identified in the formalin model of tonic pain (Mifflin et al. 2016) and in allodynia associated with experimental autoimmune encephalomyelitis, (EAE) a mouse model of multiple sclerosis (Potter et al. 2016). Here, we further clarify the specific types of stimuli and contexts in which PLZ modulates nociceptive sensitivity. Our findings indicate that PLZ selectively inhibits ongoing inflammatory pain while sparing transient reflexive and acute nociception...
May 9, 2018: Neuroscience
https://www.readbyqxmd.com/read/29752624/g%C3%AE-%C3%AE-snare-interactions-and-their-behavioral-effects
#8
Simon Alford, Heidi Hamm, Shelagh Rodriguez, Zack Zurawski
Presynaptic terminals possess interlocking molecular mechanisms that control exocytosis. An example of such complexity is the modulation of release by presynaptic G Protein Coupled Receptors (GPCRs). GPCR ubiquity at synapses-GPCRs are present at every studied presynaptic terminal-underlies their critical importance in synaptic function. GPCRs mediate presynaptic modulation by mechanisms including via classical Gα effectors, but membrane-delimited actions of Gβγ can also alter probability of release by altering presynaptic ionic conductances...
May 11, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29751720/-association-rules-analysis-of-fufang-kushen-injection-in-combination-with-modern-medications-in-treating-lung-cancer-real-world-study-based-on-hospital-information
#9
Hui-Sheng Yang, Yan-Ming Xie, Cen Chen, Yan Zhuang, Yin Zhang
The present study was aimed to analyze the association rules of Fufang Kushen injection in combination with other modern medications in treating lung cancer based on the electrical medical records in real world clinical situations extracted from hospital information system in Institute of Basic Medical Sciences, China Academy of Chinese Medical Sciences, and provide reference for improving rationality of clinical drug use and exploring the prescription rules as well as subsequent in-depth analysis. The electrical medical records of the hospitalized patients using Fufang Kushen injection for lung cancer were extracted to analyze the frequency distribution characteristics in combined application with western medicine, and Apriori algorithm was used to analyze the specific association rules in combined drug use...
April 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29748774/structural-determinants-influencing-halogen-bonding-a-case-study-on-azinesulfonamide-analogs-of-aripiprazole-as-5-ht-1a-5-ht-7-and-d-2-receptor-ligands
#10
Krzysztof Marciniec, Rafał Kurczab, Maria Książek, Ewa Bębenek, Elwira Chrobak, Grzegorz Satała, Andrzej J Bojarski, Joachim Kusz, Paweł Zajdel
A series of azinesulfonamide derivatives of long-chain arylpiperazines with variable-length alkylene spacers between sulfonamide and 4-arylpiperazine moiety is designed, synthesized, and biologically evaluated. In vitro methods are used to determine their affinity for serotonin 5-HT1A , 5-HT6 , 5-HT7 , and dopamine D2 receptors. X-ray analysis, two-dimensional NMR conformational studies, and docking into the 5-HT1A and 5-HT7 receptor models are then conducted to investigate the conformational preferences of selected serotonin receptor ligands in different environments...
May 11, 2018: Chemistry Central Journal
https://www.readbyqxmd.com/read/29748476/fingerprint-based-machine-learning-approach-to-identify-potent-and-selective-5-ht-2b-r-ligands
#11
Krzysztof Rataj, Ádám Andor Kelemen, José Brea, María Isabel Loza, Andrzej J Bojarski, György Miklós Keserű
The identification of subtype-selective GPCR (G-protein coupled receptor) ligands is a challenging task. In this study, we developed a computational protocol to find compounds with 5-HT2B R versus 5-HT1B R selectivity. Our approach employs the hierarchical combination of machine learning methods, docking, and multiple scoring methods. First, we applied machine learning tools to filter a large database of druglike compounds by the new Neighbouring Substructures Fingerprint (NSFP). This two-dimensional fingerprint contains information on the connectivity of the substructural features of a compound...
May 10, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29747744/yokukansan-contains-compounds-that-antagonize-the-5-ht-3-receptor
#12
Yukiko Nakamura, Yusuke Ishida, Makoto Kondo, Shoichi Shimada
BACKGROUND: We recently focused on alkaloids in Uncaria hook (a constituent of the Kampo medicine, yokukansan) and identified the pharmacological action of geissoschizine methyl ether on several G protein-coupled receptors. However, the functions of other identified alkaloids in Uncaria hook, including hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine, are not clear. PURPOSE: To evaluate the effect of seven alkaloids in Uncaria hook (hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine and geissoschizine methyl ether) on the hydroxytryptamine type-3 (5-HT3 ) receptor ion channel...
April 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29738849/5-ht-1a-receptor-stimulation-in-the-medial-prefrontal-cortex-mediates-the-antidepressant-effects-of-mglu2-3-receptor-antagonist-in-mice
#13
Kenichi Fukumoto, Michihiko Iijima, Takeo Funakoshi, Shigeyuki Chaki
We previously reported that serotonergic transmission is involved in the antidepressant effects of metabotropic glutamate 2/3 (mGlu2/3) receptor antagonists. However, the detailed underlying mechanisms had not yet been explored. In the present study, we investigated the role of the 5-HT1A receptor and its signaling cascade in the medial prefrontal cortex (mPFC) in the antidepressant effects of LY341495, an mGlu2/3 receptor antagonist. LY341495 significantly reduced the immobility time in the forced swimming test which sustained for 24 h after administration...
May 5, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29733594/development-of-a-fluorescent-bodipy-probe-for-visualization-of-the-serotonin-5-ht1a-receptor-in-native-cells-of-the-immune-system
#14
Gloria Hernandez-Torres, Ernesto Enriquez Palacios, Miriam Mecha, Ana Feliu, Ainoa Rueda-Zubiaurre, Alba Angelina, Leticia Martin-Cruz, Mar Martín-Fontecha, Oscar Palomares, Carmen Guaza, Eduardo Peña-Cabrera, María L López-Rodríguez, Silvia Ortega-Gutierrez
Serotonin (5-HT) modulates key aspects of the immune system. However, its precise function and the receptors involved in the observed effects have remained elusive. Among the different serotonin receptors, 5-HT1A plays an important role in the immune system given its presence in cells involved in both the innate and the adaptive immune responses, but its actual levels of expression under different conditions have not been comprehensively studied due to the lack of suitable tools. To further clarify the role of 5-HT1A receptor in the immune system, we have developed a fluorescent small molecule probe that enables the direct study of the receptor levels in native cells...
May 7, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29732102/high-throughput-identification-of-g-protein-coupled-receptor-modulators-through-affinity-mass-spectrometry-screening
#15
Shanshan Qin, Mengmeng Meng, Dehua Yang, Wenwen Bai, Yan Lu, Yao Peng, Gaojie Song, Yiran Wu, Qingtong Zhou, Suwen Zhao, Xiping Huang, John D McCorvy, Xiaoqing Cai, Antao Dai, Bryan L Roth, Michael A Hanson, Zhi-Jie Liu, Ming-Wei Wang, Raymond C Stevens, Wenqing Shui
G protein-coupled receptors (GPCRs) represent the largest class of cell surface proteins and thus constitute an important family of therapeutic targets. Therefore, significant effort has been put towards the identification of novel ligands that can modulate the activity of a GPCR target with high efficacy and selectivity. However, due to limitations inherent to the most common techniques for GPCR ligand discovery, there is a pressing need for more efficient and effective ligand screening methods especially for the identification of potential allosteric modulators...
March 28, 2018: Chemical Science
https://www.readbyqxmd.com/read/29730825/-18-f-f13640-preclinical-evaluation-in-rodent-cat-and-primate-as-a-5-ht-1a-receptor-agonist-for-pet-neuroimaging
#16
Benjamin Vidal, Sylvain Fieux, Matthieu Colom, Thierry Billard, Caroline Bouillot, Olivier Barret, Cristian Constantinescu, Gilles Tamagnan, Adrian Newman-Tancredi, Luc Zimmer
Serotonin 1A receptors are known to play an important role in many psychiatric and neurodegenerative disorders. Currently, all available 5-HT1A receptor PET radiopharmaceuticals that are radiolabeled with fluorine-18 are antagonists. As agonists bind preferentially to the high-affinity state of receptors, it would be of great interest to develop agonist radioligands which could provide a measure of the functional 5-HT1A receptors in pathophysiological processes. The 5-HT1A receptor agonist candidates we recently proposed had promising in vitro properties but were not optimal in terms of PET imaging...
May 5, 2018: Brain Structure & Function
https://www.readbyqxmd.com/read/29723640/dual-radiotracer-translational-spect-neuroimaging-comparison-of-three-methods-for-the-simultaneous-brain-imaging-of-d-2-3-and-5-ht-2a-receptors
#17
Stergios Tsartsalis, Benjamin B Tournier, Selim Habiby, Meriem Ben Hamadi, Cristina Barca, Nathalie Ginovart, Philippe Millet
PURPOSE: SPECT imaging with two radiotracers at the same time is feasible if two different radioisotopes are employed, given their distinct energy emission spectra. In the case of 123 I and 125 I, dual SPECT imaging is not straightforward: 123 I emits photons at a principal energy emission spectrum of 143.1-179.9 keV. However, it also emits at a secondary energy spectrum (15-45 keV) that overlaps with the one of 125 I and the resulting cross-talk of emissions impedes the accurate quantification of 125 I...
April 30, 2018: NeuroImage
https://www.readbyqxmd.com/read/29723540/tnf%C3%AE-dependent-anhedonia-and-upregulation-of-hippocampal-serotonin-transporter-activity-in-a-mouse-model-of-collagen-induced-arthritis
#18
Eric Brown, Conor J Mc Veigh, Leilani Santos, Martina Gogarty, Heidi Kaastrup Müller, Betina Elfving, David J Brayden, Jana Haase
The serotonin transporter (SERT) facilitates high affinity reuptake of 5-HT from the extracellular fluid and dysregulation of transporter function has been implicated in a range of mood disorders including depression. Recent studies have linked immune system activation to depression as well as to altered serotonin transporter activity. Advancing previous studies, which have mainly focussed on acute effects of immune system activation, in this study we used collagen-induced arthritis (CIA) in mice as a model of chronic inflammatory disease, to investigate the effect of prolonged inflammation on brain SERT function and behaviour...
April 30, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29715538/age-and-sex-dependent-effects-of-methamphetamine-on-cognitive-flexibility-and-5-ht-2c-receptor-localization-in-the-orbitofrontal-cortex-of-sprague-dawley-rats
#19
Emily R Hankosky, Sara R Westbrook, Rachel M Haake, Jari Willing, Lori T Raetzman, Janice M Juraska, Joshua M Gulley
Adolescents and females experience worse outcomes of drug use compared to adults and males. This could result from age- and sex-specific consequences of drug exposure on brain function and cognitive behavior. In the current study, we examined whether a history of intravenous methamphetamine (METH) self-administration impacted cognitive flexibility and 5-HT2C R localization in the orbitofrontal cortex (OFC) in an age- and sex-dependent manner. Strategy shifting was assessed in male and female Sprague-Dawley rats that had self-administered METH (0...
April 28, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29706583/serotonergic-signaling-controls-input-specific-synaptic-plasticity-at-striatal-circuits
#20
Anna Cavaccini, Marta Gritti, Andrea Giorgi, Andrea Locarno, Nicolas Heck, Sara Migliarini, Alice Bertero, Maddalena Mereu, Giulia Margiani, Massimo Trusel, Tiziano Catelani, Roberto Marotta, Maria Antonietta De Luca, Jocelyne Caboche, Alessandro Gozzi, Massimo Pasqualetti, Raffaella Tonini
Monoaminergic modulation of cortical and thalamic inputs to the dorsal striatum (DS) is crucial for reward-based learning and action control. While dopamine has been extensively investigated in this context, the synaptic effects of serotonin (5-HT) have been largely unexplored. Here, we investigated how serotonergic signaling affects associative plasticity at glutamatergic synapses on the striatal projection neurons of the direct pathway (dSPNs). Combining chemogenetic and optogenetic approaches reveals that impeding serotonergic signaling preferentially gates spike-timing-dependent long-term depression (t-LTD) at thalamostriatal synapses...
April 25, 2018: Neuron
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