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https://www.readbyqxmd.com/read/30108716/cu-ii-immobilized-on-fe-3-o-4-aptms-dfx-nanoparticles-an-efficient-catalyst-for-the-synthesis-of-5-substituted-1-h-tetrazoles-with-cytotoxic-activity
#1
Faezeh Taghavi, Mostafa Gholizadeh, Amir Sh Saljooghi, Mohammad Ramezani
Cu(ii) immobilized on deferasirox loaded amine functionalized magnetic nanoparticles (Cu(ii)/Fe3 O4 @APTMS-DFX) as a novel magnetically recyclable heterogeneous catalyst is able to catalyze the [3 + 2] cycloaddition reactions of various organic nitriles with sodium azide. Using this method, a series of 5-substituted-1 H -tetrazoles under mild conditions in DMSO were prepared. The reaction involves mild reaction conditions with efficient transformation capability. The developed catalyst could be easily separated by applying an external magnetic field...
October 1, 2017: MedChemComm
https://www.readbyqxmd.com/read/30102081/psychedelics-as-anti-inflammatory-agents
#2
Thomas W Flanagan, Charles D Nichols
Serotonin (5-hydroxytryptamine, 5-HT)2A receptor agonists have recently emerged as promising new treatment options for a variety of disorders. The recent success of these agonists, also known as psychedelics, like psilocybin for the treatment of anxiety, depression, obsessive-compulsive disorder (OCD), and addiction, has ushered in a renaissance in the way these compounds are perceived in the medical community and populace at large. One emerging therapeutic area that holds significant promise is their use as anti-inflammatory agents...
August 13, 2018: International Review of Psychiatry
https://www.readbyqxmd.com/read/30059705/chronic-oxycodone-self-administration-altered-reward-related-genes-in-the-ventral-and-dorsal-striatum-of-c57bl-6j-mice-an-rna-seq-analysis
#3
Yong Zhang, Yupu Liang, Matthew Randesi, Vadim Yuferov, Connie Zhao, Mary Jeanne Kreek
Prescription opioid abuse, for example of oxycodone, is a pressing public health issue. This study focuses on how chronic oxycodone self-administration (SA) affects the reward pathways in the mouse brain. In this study, we tested the hypothesis that the expression of reward-related genes in the ventral and dorsal striatum, areas involved in different aspects of opioid addiction models, was altered within 1 h after chronic oxycodone SA, using transcriptome-wide sequencing (RNA-seq). Based on results from earlier human genetic and rodent preclinical studies, we focused on a set of genes that may be associated with the development of addictive diseases and the rewarding effect of drugs of abuse, primarily in the opioid, stress response and classical neurotransmitter systems...
July 29, 2018: Neuroscience
https://www.readbyqxmd.com/read/30033381/vasomotor-dysfunction-in-human-subcutaneous-arteries-exposed-ex-vivo-to-food-grade-titanium-dioxide
#4
Ditte Marie Jensen, Gry Freja Skovsted, Jens Lykkesfeldt, Rasmus Dreier, Jais Oliver Berg, Jørgen Lykke Jeppesen, Majid Sheykhzade, Steffen Loft, Peter Møller
Animal studies have shown that titanium dioxide (TiO2 ) exposure affects arterial vasomotor function, whereas little is known about the effects in arteries from humans. This study investigated vasomotor responses after direct exposure of human subcutaneous arteries to food-grade TiO2 (E171) (14 or 140 μg/ml) for 30 min and 18 h. Vasomotor responses to bradykinin, 5-hydroxytryptamine (5-HT), sarafotoxin 6c (S6c) and nitroglycerin were recorded in wire-myographs. Vasoconstrictor responses to 5-HT were increased in arteries exposed to E171 for 18 h (P < 0...
July 7, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29996605/-role-of-ginkgo-biloba-extract-in-regulating-5-hydroxytrytamine-and-its-receptor-in-heart-failure-mice
#5
M Y Liu, L J Zhang
Objective: Exploring the modulation of periphery and central serotonin (5-hydroxytrytamine, 5-HT) and 5-HT(2A) receptor (5-HT(2A)R) in mice with heart failure during the process of heart failure and after treatment. Methods: Thirty mice were allocated into three groups randomly including normal group (NG), heart failure group (HFG) and treatment group (TG) ( n =10). Mice in the NG were sacrificed after evaluating left ventricular ejection fraction (EF) with echocardiogram. Mice in HFG and TG experienced myocardial infarction surgery to achieve EF≤30%, HFG was treated with saline and TG with Ginkgo biloba pills (GBP), once a day for 4 weeks, then EF was assessed again before sacrifice...
July 3, 2018: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/29969592/the-highly-selective-5-ht-2a-antagonist-emd-281-014-reduces-dyskinesia-and-psychosis-in-the-l-dopa-treated-parkinsonian-marmoset
#6
Adjia Hamadjida, Stephen G Nuara, Dominique Bédard, Fleur Gaudette, Francis Beaudry, Jim C Gourdon, Philippe Huot
Blockade of serotonin 2A (5-HT2A ) receptors is regarded as an anti-dyskinetic and anti-psychotic strategy in Parkinson's disease (PD). However, the 5-HT2A antagonists tested so far exhibited affinity for other receptors, which might have played a role in their action. EMD-281,014 is the most selective 5-HT2A antagonist available, with approximately 2,000-fold selectivity over serotonin 2C (5-HT2C ) receptors. EMD-281,014 was previously tested in the clinic and has high translational potential. In the present study, we assessed the effect of EMD-281,014 on dyskinesia and psychosis in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned common marmoset...
September 1, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29950360/successful-treatment-of-intractable-visual-hallucinations-with-5-ht-2a-antagonist-ketanserin
#7
Iris E C Sommer, Hidde Kleijer, Lucy Visser, Teus van Laar
Hallucinations, visual, auditory or in another sensory modality, often respond well to treatment in patients with schizophrenia. Some, however, do not and can be very chronic and debilitating. We present a patient with schizophrenia with intractable hallucinations despite state of the art care, including high-dose clozapine and transcranial magnetic stimulation. Based on the possible role of the 5-HT2A receptor in hallucinations, we treated her with the antihypertensive drug ketanserin, a 5-HT2A receptor antagonist...
June 27, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29944910/blockade-of-serotonin-5-ht-2a-receptors-potentiates-dopamine-d-2-activation-induced-disruption-of-pup-retrieval-on-an-elevated-plus-maze-but-has-no-effect-on-d-2-blockade-induced-one
#8
Lina Nie, Tianqi Di, Yu Li, Peng Cheng, Ming Li, Jun Gao
Appetitive aspect of rat maternal behavior, such as pup retrieval, is motivationally driven and sensitive to dopamine disturbances. Activation or blockade of dopamine D2 receptors causes a similar disruption of pup retrieval, which may also reflect an increase in maternal anxiety and/or a disruption of executive function. Recent work indicates that serotonin 5-HT2A receptors also play an important role in rat maternal behavior. Given the well-known modulation of 5-HT2A on the mesolimbic and mesocortical dopamine functions, the present study examined the extent to which blockade of 5-HT2A receptors on dopamine D2 -mediated maternal effects using a pup retrieval on the elevated plus maze (EPM) test...
August 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29858599/5-ht-2a-receptor-dependent-phosphorylation-of-mglu-2-receptor-at-serine-843-promotes-mglu-2-receptor-operated-g-i-o-signaling
#9
Samy Murat, Mathilde Bigot, Jonathan Chapron, Gabriele M König, Evi Kostenis, Giuseppe Battaglia, Ferdinando Nicoletti, Emmanuel Bourinet, Joël Bockaert, Philippe Marin, Franck Vandermoere
The serotonin 5-HT2A and glutamate mGlu2 receptors continue to attract particular attention, given their implication in psychosis associated with schizophrenia and the mechanism of action of atypical antipsychotics and a new class of antipsychotics, respectively. A large body of evidence indicates a functional crosstalk between both receptors in the brain, but the underlying mechanisms are not entirely elucidated. Here, we have explored the influence of 5-HT2A receptor upon the phosphorylation pattern of mGlu2 receptor in light of the importance of specific phosphorylation events in regulating G protein-coupled receptor signaling and physiological outcomes...
June 1, 2018: Molecular Psychiatry
https://www.readbyqxmd.com/read/29858497/chronic-fluoxetine-treatment-accelerates-kindling-epileptogenesis-in-mice-independently-of-5-ht-2a-receptors
#10
Crystal Li, Juliana Silva, Ezgi Ozturk, Gabriella Dezsi, Terence J O'Brien, Thibault Renoir, Nigel C Jones
Patients with epilepsy often have mood disorders, and these are commonly treated with antidepressant drugs. Although these drugs are often successful in mitigating depressive symptoms, how they affect the epileptogenic processes has been little studied. Recent evidence has demonstrated that treatment with selective serotonin reuptake inhibitor (SSRI) antidepressant drugs adversely promotes epileptogenesis, which may be of great concern considering the number of patients exposed to these drugs. This study investigated 5-HT2A receptor signaling as a potential mechanism driving the pro-epileptogenic effects of the prototypical SSRI fluoxetine...
July 2018: Epilepsia
https://www.readbyqxmd.com/read/29729987/design-synthesis-and-evaluation-of-vilazodone-tacrine-hybrids-as-multitarget-directed-ligands-against-depression-with-cognitive-impairment
#11
Wenwen Liu, Huan Wang, Xiaokang Li, Yixiang Xu, Jian Zhang, Wei Wang, Qi Gong, Xiaoxia Qiu, Jin Zhu, Fei Mao, Haiyan Zhang, Jian Li
Depression, a severe mental disease, is greatly difficult to treat and easy to induce other neuropsychiatric symptoms, the most frequent one is cognitive impairment. In this study, a series of novel vilazodone-tacrine hybrids were designed, synthesized and evaluated as multitarget agents against depression with cognitive impairment. Most compounds exhibited good multitarget activities and appropriate blood-brain barrier permeability. Specifically, compounds 1d and 2a exhibited excellent 5-HT1A agonist activities (1d, EC50  = 0...
July 23, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29724002/synthesis-of-new-benzothiazole-acylhydrazones-as-anticancer-agents
#12
Derya Osmaniye, Serkan Levent, Abdullah Burak Karaduman, Sinem Ilgın, Yusuf Özkay, Zafer Asım Kaplancıklı
During the last five decades, a large number of BT (Benzothiazole) derivatives formed one of the eligible structures in medicinal chemistry as anticancer agents. Most of the studies reveal that various substitutions at specific positions on BT scaffold modulate the antitumor property. The potential of BTs encouraged us to synthesize a number of new 2-((5-substitutedbenzothiazol-2-yl)thio)- N &rsquo;-(2-(4-(substitutedphenyl)ethylidene)acetohydrazide derivatives and investigate their probable anticancer activity...
May 1, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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
#13
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...
August 1, 2018: NeuroImage
https://www.readbyqxmd.com/read/29700292/enhancement-of-5-ht-2a-receptor-function-and-blockade-of-kv1-5-by-mk801-and-ketamine-implications-for-pcp-derivative-induced-disease-models
#14
Haiyue Lin, Jae Gon Kim, Sang Woong Park, Hyun Ju Noh, Jeong Min Kim, Chang Yong Yoon, Nam-Sik Woo, Bokyung Kim, Sung Il Cho, Bok Hee Choi, Dong Jun Sung, Young Min Bae
MK801 and ketamine, which are phencyclidine (PCP) derivative N-methyl-d-aspartate receptor (NMDAr) blockers, reportedly enhance the function of 5-hydroxytryptamine (HT)-2A receptors (5-HT2A Rs). Both are believed to directly affect the pathogenesis of schizophrenia, as well as hypertension. 5-HT2A R signaling involves the inhibition of Kv conductance. This study investigated the interaction of these drugs with Kv1.5, which plays important roles in 5-HT2A R signaling and in regulating the excitability of the cardiovascular and nervous system, and the potential role of this interaction in the enhancement of the 5-HT2A R-mediated response...
April 27, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29680514/brain-blood-cerebrospinal-fluid-and-serum-biomarkers-in-schizophrenia
#15
REVIEW
Alireza Mohammadi, Ehsan Rashidi, Vahid Ghasem Amooeian
Over the last decade, finding a reliable biomarker for the early detection of schizophrenia (Scz) has been a topic of interest. The main goal of the current review is to provide a comprehensive view of the brain, blood, cerebrospinal fluid (CSF), and serum biomarkers of Scz disease. Imaging studies have demonstrated that the volumes of the corpus callosum, thalamus, hippocampal formation, subiculum, parahippocampal gyrus, superior temporal gyrus, prefrontal and orbitofrontal cortices, and amygdala-hippocampal complex were reduced in patients diagnosed with Scz...
July 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29679943/photocatalytic-decomposition-of-selected-biologically-active-compounds-in-environmental-waters-using-tio-2-polyaniline-nanocomposites-kinetics-toxicity-and-intermediates-assessment
#16
Daniela V Šojić Merkulov, Vesna N Despotović, Nemanja D Banić, Sanja J Armaković, Nina L Finčur, Marina J Lazarević, Dragana D Četojević-Simin, Dejan Z Orčić, Marija B Radoičić, Zoran V Šaponjić, Mirjana I Čomor, Biljana F Abramović
A comprehensive study of the removal of selected biologically active compounds (pharmaceuticals and pesticides) from different water types was conducted using bare TiO2 nanoparticles and TiO2 /polyaniline (TP-50, TP-100, and TP-150) nanocomposite powders. In order to investigate how molecular structure of the substrate influences the rate of its removal, we compared degradation efficiency of the initial substrates and degree of mineralization for the active components of pharmaceuticals (propranolol, and amitriptyline) and pesticides (sulcotrione, and clomazone) in double distilled (DDW) and environmental waters...
August 2018: Environmental Pollution
https://www.readbyqxmd.com/read/29661535/synthesis-of-carbon-11-labeled-5-ht-6-r-antagonists-as-new-candidate-pet-radioligands-for-imaging-of-alzheimer-s-disease
#17
Xiaohong Wang, Fugui Dong, Caihong Miao, Wei Li, Min Wang, Mingzhang Gao, Qi-Huang Zheng, Zhidong Xu
Carbon-11-labeled serotonin (5-hydroxytryptamine) 6 receptor (5-HT6 R) antagonists, 1-[(2-bromophenyl)sulfonyl]-5-[11 C]methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole (O-[11 C]2a) and 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-[11 C]methyl-1-piperazinyl)methyl]-1H-indole (N-[11 C]2a), 5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1-(phenylsulfonyl)-1H-indole (O-[11 C]2b) and 5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1-(phenylsulfonyl)-1H-indole (N-[11 C]2b), 1-((4-isopropylphenyl)sulfonyl)-5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1H-indole (O-[11 C]2c) and 1-((4-isopropylphenyl)sulfonyl)-5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1H-indole (N-[11 C]2c), 1-((4-fluorophenyl)sulfonyl)-5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1H-indole (O-[11 C]2d) and 1-((4-fluorophenyl)sulfonyl)-5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1H-indole (N-[11 C]2d), were prepared from their O- or N-desmethylated precursors with [11 C]CH3 OTf through O- or N-[11 C]methylation and isolated by HPLC combined with SPE in 40-50% radiochemical yield, based on [11 C]CO2 and decay corrected to end of bombardment (EOB)...
June 1, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29625175/magi-proteins-can-differentially-regulate-the-signaling-pathways-of-5-ht-2a-r-by-enhancing-receptor-trafficking-and-plc-recruitment
#18
Maha M Hammad, Henry A Dunn, Stephen S G Ferguson
MAGI proteins are Membrane-Associated Guanylate Kinase Inverted proteins that belong to the MAGUK family. They are scaffolding proteins that were shown to mediate the trafficking and signaling of various G protein-coupled receptors (GPCRs). They contain PDZ domains in their structure and many GPCRs interact with these proteins via the PDZ motifs on the carboxyl terminal end of a receptor. In a PDZ overlay assay performed with the carboxyl terminal tail of 5-HT2A R, we were able to detect all three members of the MAGI subfamily, MAGI-1, MAGI-2 and MAGI-3 as interacting PDZ proteins...
July 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29619682/a-population-pharmacokinetic-and-pharmacodynamic-analysis-of-rp5063-phase-2-study-data-in-patients-with-schizophrenia-or-schizoaffective-disorder
#19
Marc Cantillon, Robert Ings, Arul Prakash, Laxminarayan Bhat
BACKGROUND AND OBJECTIVE: RP5063 is a novel multimodal dopamine (D)-serotonin (5-HT) stabilizer possessing partial agonist activity for D2/3/4 and 5-HT1A/2A , antagonist activity for 5-HT2B/2C/7, and moderate affinity for the serotonin transporter. Phase 2 trial data analysis of RP5063 involving patients with schizophrenia and schizoaffective disorder defined: (1) the pharmacokinetic profile; and (2) the pharmacokinetic/pharmacodynamic relationships. METHODS: Pharmacokinetic sample data (175 patients on RP5063; 28 doses/patient) were analyzed, utilized one- and two-compartment models, and evaluated the impact of covariates...
April 4, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29616335/behavioral-mechanisms-underlying-the-maternal-disruptive-effect-of-serotonin-5-ht-2a-receptor-activation-in-sprague-dawley-rats
#20
Ruiyong Wu, Collin Davis, Ming Li
Recent evidence indicates that acute activation of 5-HT2A receptors causes a disruption of maternal behavior in rats. However, the behavioral mechanisms underlying such a disruption are not known. We addressed this issue using two behavioral approaches targeting the maternal motivational and emotional processing systems. First, we used the pup-separation technique to increase maternal motivation to see whether pup separation is capable of reducing the maternal disruptive effect of TCB-2 (a high-affinity 5-HT2A agonist) treatment...
July 2018: Journal of Neural Transmission
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