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https://www.readbyqxmd.com/read/27896660/ayahuasca-exposure-descriptive-analysis-of-calls-to-us-poison-control-centers-from-2005-to-2015
#1
C William Heise, Daniel E Brooks
BACKGROUND: Ayahuasca is a hallucinogenic plant preparation which usually contains the vine Banisteriopsis caapi and the shrub Psychotria viridis. This tea originates from the Amazon Basin where it is used in religious ceremonies. Because interest in these religious groups spreading as well as awareness of use of ayahuasca for therapeutic and recreational purposes, its use is increasing. Banisteriopsis caapi is rich in β-carbolines, especially harmine, tetrahydroharmine and harmaline, which have monoamine oxidase inhibiting (MAOI) activity...
November 28, 2016: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
https://www.readbyqxmd.com/read/27889455/in-vivo-evaluation-of-18-f-fecimbi-36-an-agonist-5-ht2a-2c-receptor-pet-radioligand-in-nonhuman-primate
#2
Jaya Prabhakaran, Kiran Kumar Solingapuram Sai, Francesca Zanderigo, Harry Rubin-Falcone, Matthew J Jorgensen, Jay R Kaplan, Katharine I Tooke, Akiva Mintz, J John Mann, J S Dileep Kumar
We recently reported the radiosynthesis and in vitro evaluation of [(18)F]-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine, ([(18)F]FECIMBI-36) or ([(18)F]1), an agonist radioligand for 5HT2A/2C receptors in postmortem samples of human brain. Herein we describe the in vivo evaluation of [(18)F]FECIMBI-36 in vervet/African green monkeys by PET imaging. PET images show that [(18)F]FECIMBI-36 penetrates the blood-brain barrier and a low retention of radioactivity is observed in monkey brain...
November 16, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27800022/evidence-for-the-use-of-pimavanserin-in-the-treatment-of-parkinson-s-disease-psychosis
#3
REVIEW
Harini Sarva, Claire Henchcliffe
Parkinson's disease (PD) is a progressive neurodegenerative disorder with both motor and nonmotor symptoms (NMS), leading to significant morbidity and caregiver burden. Psychosis is common but is under recognized by physicians. When present, it increases the patient's risk of hospitalization and nursing home placement and caregiver burden. Although the atypical antipsychotic agent, clozapine, has been considered the gold standard treatment, severe agranulocytosis in 0.38% of patients and more commonly milder leukopenia, resulting in frequent blood testing, limit its use...
November 2016: Therapeutic Advances in Neurological Disorders
https://www.readbyqxmd.com/read/27788337/adjunctive-brexpiprazole-for-the-treatment-of-major-depressive-disorder
#4
John L Beyer, Richard H Weisler
The lifetime prevalence of major depressive episodes in the United States is nearly 17%. Clinical trials and clinical effectiveness studies have demonstrated that many patients will fail to achieve remission using traditional monotherapy, contributing to significant morbidity and suffering. Because of this, augmentation strategies have been proposed to improve both treatment response and remission. Areas covered: Brexpiprazole is a second generation antipsychotic (SGA) approved by the US FDA in 2015 as an add-on treatment to an antidepressant medication for the treatment of adults with MDD, based on the results of two large-scale, randomized, placebo-controlled trials...
October 27, 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27717169/5ht2a-receptor-blockade-in-dorsomedial-striatum-reduces-repetitive-behaviors-in-btbr-mice
#5
D A Amodeo, E Rivera, E H Cook, J A Sweeney, M E Ragozzino
Restricted and repetitive behaviors are a defining feature of autism, which can be expressed as a cognitive flexibility deficit or stereotyped, motor behaviors. There is limited knowledge about the underlying neuropathophysiology contributing to these behaviors. Previous findings suggest that central 5HT2A receptor activity is altered in autism, while recent work indicates that systemic 5HT2A receptor antagonist treatment reduces repetitive behaviors in an idiopathic model of autism. 5HT2A receptors are expressed in the orbitofrontal cortex and striatum...
September 22, 2016: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/27687785/an-original-pharmacoepidemiologic-pharmacodynamic-method-application-to-antipsychotic-induced-movement-disorders
#6
Thi Thu Ha Nguyen, Antoine Pariente, Jean-Louis Montastruc, Maryse Lapeyre-Mestre, Vanessa Rousseau, Olivier Rascol, Bernard Bégaud, François Montastruc
AIMS: Pharmacovigilance databases are usually used to detect new potential signals relevant for drug safety. They are seldom used for explanatory purposes, e.g. to understand the mechanisms of adverse drug reactions (ADRs). The aim of the present study was to combine pharmacovigilance and pharmacodynamic data to investigate the association between D2, 5HT2A, and M1 receptor occupancy and the risks of antipsychotic (AP)-induced movement disorders. METHODS: First, we performed a case non-case analysis using spontaneous reports from the World Health Organization (WHO) Global Individual Case Safety Report (ICSR) database, VigiBase®...
September 30, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27669299/vasoactivity-and-vasoconstriction-changes-in-cattle-related-to-time-off-toxic-endophyte-infected-tall-fescue
#7
James L Klotz, Glen E Aiken, Jessica R Bussard, Andrew P Foote, David L Harmon, Ben M Goff, F Neal Schrick, James R Strickland
Previous research has indicated that serotonergic and α-adrenergic receptors in peripheral vasculature are affected by exposure of cattle grazing toxic endophyte-infected (E+; Epichlöe coenophialia) tall fescue (Lolium arundinaceum). The objective of this experiment was to determine the period of time necessary for the vascular effects of ergot alkaloids to subside. Two experiments were conducted to investigate changes in vascular contractile response and vasoconstriction over time relative to removal from an ergot alkaloid-containing E+ tall fescue pasture...
2016: Toxins
https://www.readbyqxmd.com/read/27619519/cholinergic-and-serotonergic-modulation-of-visual-information-processing-in-monkey-v1
#8
Satoshi Shimegi, Akihiro Kimura, Akinori Sato, Chisa Aoyama, Ryo Mizuyama, Keisuke Tsunoda, Fuyuki Ueda, Sera Araki, Ryoma Goya, Hiromichi Sato
The brain dynamically changes its input-output relationship depending on the behavioral state and context in order to optimize information processing. At the molecular level, cholinergic/monoaminergic transmitters have been extensively studied as key players for the state/context-dependent modulation of brain function. In this paper, we review how cortical visual information processing in the primary visual cortex (V1) of macaque monkey, which has a highly differentiated laminar structure, is optimized by serotonergic and cholinergic systems by examining anatomical and in vivo electrophysiological aspects to highlight their similarities and distinctions...
September 9, 2016: Journal of Physiology, Paris
https://www.readbyqxmd.com/read/27572262/serotonin-signaling-mediates-protein-valuation-and-aging
#9
Jennifer Ro, Gloria Pak, Paige A Malec, Yang Lyu, David B Allison, Robert T Kennedy, Scott D Pletcher
Research into how protein restriction improves organismal health and lengthens lifespan has largely focused on cell-autonomous processes. In certain instances, however, nutrient effects on lifespan are independent of consumption, leading us to test the hypothesis that central, cell non-autonomous processes are important protein restriction regulators. We characterized a transient feeding preference for dietary protein after modest starvation in the fruit fly, Drosophila melanogaster, and identified tryptophan hydroxylase (Trh), serotonin receptor 2a (5HT2a), and the solute carrier 7-family amino acid transporter, JhI-21, as required for this preference through their role in establishing protein value...
August 23, 2016: ELife
https://www.readbyqxmd.com/read/27511837/control-of-sensory-neuron-excitability-by-serotonin-involves-5ht2c-receptors-and-ca-2-activated-chloride-channels
#10
Isabella Salzer, Enkhbileg Gantumur, Arsalan Yousuf, Stefan Boehm
Serotonin (5HT) is a constituent of the so-called "inflammatory soup" that sensitizes nociceptors during inflammation. Nevertheless, receptors and signaling mechanisms that mediate an excitation of dorsal root ganglion (DRG) neurons by 5HT remained controversial. Therefore, capsaicin-sensitive nociceptive neurons dissociated from rat DRGs were used to investigate effects of 5HT on membrane excitability and currents through ligand- as well as voltage-gated ion channels. In 58% of the neurons tested, 5HT increased action potential firing, an effect that was abolished by the 5HT2 receptor antagonist ritanserin, but not by the 5HT3 antagonist tropisetron...
November 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27503570/mechanism-of-action-of-pimavanserin-in-parkinson-s-disease-psychosis-targeting-serotonin-5ht2a-and-5ht2c-receptors
#11
Stephen M Stahl
Pimavanserin, a novel agent approved for the treatment of Parkinson's disease psychosis, has potent actions as an antagonist/inverse agonist at serotonin 5HT2A receptors and less potent antagonist/inverse agonist actions at 5HT2C receptors.
August 2016: CNS Spectrums
https://www.readbyqxmd.com/read/27479537/suicide-behavior-as-a-quantitative-trait-and-its-genetic-background
#12
Joanna Pawlak, Monika Dmitrzak-Weglarz, Monika Wilkosc, Aleksandra Szczepankiewicz, Anna Leszczynska-Rodziewicz, Dorota Zaremba, Pawel Kapelski, Aleksandra Rajewska-Rager, Joanna Hauser
INTRODUCTION: Studies have not given yet a clear answer what is the genetic background of suicidal predisposition. The associations between polymorphisms of the TPH1 and 5-HTTLPR genes and violent suicidal behavior was revealed with the least inconsistencies. METHOD: We selected 10 "strong candidate genes" and 35 SNPs, SLC6A4 and ACP1 for replication study. We searched associations between precisely described suicidal phenotype in 825 affective patients and polymorphisms of selected neurobiological pathways genes as well as their interactions that constitute suicidal risk...
July 19, 2016: Journal of Affective Disorders
https://www.readbyqxmd.com/read/27378338/m100907-attenuates-elevated-grooming-behavior-in-the-btbr-mouse
#13
Dionisio A Amodeo, Elaine Rivera, Jeffrey T Dunn, Michael E Ragozzino
Individuals with autism spectrum disorder (ASD) exhibit social-communication deficits along with restricted interests and repetitive behaviors (RRBs). To date, there is a lack of effective treatments to alleviate RRBs. A recent study found that treatment with the 5HT2A receptor antagonist M100907 attenuates a reversal learning deficit in the BTBR mouse model of autism. The BTBR mouse also exhibits elevated grooming behavior which may model stereotyped motor behaviors also observed in ASD. The present study examined whether 5HT2A receptor blockade with M100907 at either 0...
October 15, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27362381/antidepressant-antipsychotic-and-hallucinogen-drugs-for-the-treatment-of-psychiatric-disorders-a-convergence-at-the-serotonin-2a-receptor
#14
Robert H Howland
Antidepressant, atypical antipsychotic, and hallucinogen drugs mediate their actions in part by interactions with the serotonin-2A (5HT2A) receptor. Serotonergic hallucinogen drugs, such as psilocybin, bind most potently as agonists at the 5HT2A receptor, producing profound changes in perception, mood, and cognition. Some of these drugs have been or are currently being investigated in small Phase 2 studies for depression, alcoholism, smoking cessation, anxiety, and posttraumatic stress disorder. However, unlike the synergistic effects of combining antidepressant and atypical antipsychotic drugs, the potential therapeutic effects of hallucinogen drugs may be attenuated by the concurrent use of these medications because antidepressant and atypical antipsychotic drugs desensitize and/or down-regulate 5HT2A receptors...
July 1, 2016: Journal of Psychosocial Nursing and Mental Health Services
https://www.readbyqxmd.com/read/27274197/spotlight-on-brexpiprazole-and-its-potential-in-the-treatment-of-schizophrenia-and-as-adjunctive-therapy-for-the-treatment-of-major-depression
#15
REVIEW
Dawn Bruijnzeel, Rajiv Tandon
Antipsychotic agents, utilized for the treatment of a range of psychiatric disorders, differ substantially in terms of their pharmacology and adverse effect profiles. Incomplete and variable efficacy, differences in safety-tolerability, and highly heterogeneous response across individuals prompt development of new agents. Brexpiprazole is one of the two most recently introduced antipsychotic agents approved for the treatment of schizophrenia and as an adjunct for treatment of major depressive disorder. Its pharmacology, clinical trial data, and efficacy and side effects in comparison with other antipsychotic agents are discussed...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27245248/pimavanserin-an-inverse-agonist-antipsychotic-drug
#16
Robert H Howland
Approximately all clinically useful antipsychotic drugs have known activity as dopamine receptor antagonists, but many of these drugs also are inverse agonists at the serotonin-2A (5HT2A) receptor. Pimavanserin is an inverse agonist at the 5HT2A receptor, with a lower binding affinity at the serotonin-2C receptor and sigma 1 receptor, but no significant binding to dopamine or other receptors. Because of its unique pharmacology, pimavanserin was approved for the treatment of psychosis associated with Parkinson's disease, and it has a low risk for exacerbating motor symptoms compared to standard antipsychotic medications...
June 1, 2016: Journal of Psychosocial Nursing and Mental Health Services
https://www.readbyqxmd.com/read/27222264/current-trends-on-antipsychotics-focus-on-asenapine
#17
REVIEW
Donatella Marazziti, Armando Piccinni, Stefano Baroni, Francesco Mungai, Silvio Presta, Federico Mucci, Liliana Dell'Osso
Over the years, both first- (FGAs) and second-generation antipsychotics (SGAs), continue to gain increasing evidence of being effective in the treatment of psychotic symptoms. Currently, they represent the first-line treatment of schizophrenia and bipolar disorder, although they are widely used in psychotic depression and other clinical conditions, such as agitation and/or behavioural disturbances. Despite representing an indispensable tool for the treatment of severe psychotic disorders, they are widely known to have a number of unwanted side effects that the clinician must be aware of, and handle carefully to provide the patient the best available treatment in the short and long-term...
2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27130903/risperidone-induces-long-lasting-changes-in-the-conditioned-avoidance-response-and-accumbal-gene-expression-selectively-in-animals-treated-as-adolescents
#18
Aung Aung Kywe Moe, Nyoman D Kurniawan, Suzanne Alexander, Xiaoying Cui, Thomas H J Burne, Darryl W Eyles
Adolescence is a period of dynamic remodeling and maturation in the brain. Exposure to psychotropic drugs during adolescence can potentially alter neural maturation in the adolescent brain subsequently altering neural function at maturity. In this regard, antipsychotic drugs (APDs) are important given a notable global increase in prescription of these APDs to adolescents for a variety of behavioural symptoms and conditions over the past twenty years. However, there is a paucity of data on the long-term consequences of APDs on the adolescent brain...
September 2016: Neuropharmacology
https://www.readbyqxmd.com/read/26899026/serotonin-promotes-feminization-of-the-sexually-dimorphic-nucleus-of-the-preoptic-area-but-not-the-calbindin-cell-group
#19
Amanda M K Madden, Alexandria T Paul, Rory A Pritchard, Rebecca Michel, Susan L Zup
Testosterone and its metabolites masculinize the brain during a critical perinatal window, including the relative volume of sexually dimorphic brain areas such as the sexually dimorphic nucleus of the preoptic area (SDN), which is larger in males than females. Serotonin (5HT) may mediate this hormone action, since 5HT given during the second week of life decreases (i.e., feminizes) SDN volume in males and testosterone-treated females. Although previous work indicates that the 5HT2A/2C receptor is sufficient to induce feminization, it is unclear whether other serotonin receptors are required and which subpopulation(s) of SDN cells are specifically organized by 5HT...
February 22, 2016: Developmental Neurobiology
https://www.readbyqxmd.com/read/26857363/clearance-of-cerebrospinal-fluid-jcv-dna-with-mirtazapine-in-a-patient-with-progressive-multifocal-leukoencephalopathy-and-sarcoidosis
#20
Alice Trentalange, Andrea Calcagno, Valeria Ghisetti, Cristiana Atzori, Paolo Busolli, Stefano Bonora, Daniele Imperiale
Progressive multifocal leukoencephalopathy (PML) is a severe encephalic demyelinating disease associated with JC virus (JCV) reactivation that occurs mostly in patients with immune disorders. Patients affected by sarcoidosis are at risk for developing PML both for leukocyte dysfunction and for receiving immunosuppressive medications: delayed diagnosis and high-dose corticosteroids are associated with a reduced survival. Although no specific treatment for PML exists, several therapeutic possibilities have been assessed with uncertain benefits (5HT2a receptor inhibitors are active in vitro against JCV): the cornerstone of sarcoidosis-associated PML is immunosuppressants withdrawal...
February 9, 2016: Antiviral Therapy
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