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https://www.readbyqxmd.com/read/28624721/assessing-the-role-of-serotonergic-receptors-in-cannabidiol-s-anticonvulsant-efficacy
#1
Madeline C Pelz, Kathleen D Schoolcraft, Chloe Larson, Mitchell G Spring, Hassan H López
Cannabidiol (CBD) is a phytocannabinoid that has demonstrated anticonvulsant efficacy in several animal models of seizure. The current experiment validated CBD's anticonvulsant effect using the acute pentylenetetrazol (PTZ) model. Furthermore, it tested whether CBD reduces seizure activity by interacting with either the serotonergic 5HT1A or 5HT2A receptor. 120 male adolescent Wistar-Kyoto rats were randomly assigned to 8 treatment groups in two consecutive experiments. In both experiments, subjects received either CBD (100mg/kg) or vehicle 60min prior to seizure testing...
June 15, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28611364/association-of-polymorphisms-in-pharmacogenetic-candidate-genes-with-propofol-susceptibility
#2
Qi Zhong, Xiangdong Chen, Yan Zhao, Ru Liu, Shanglong Yao
Significant individual susceptibility to intravenous anesthetic propofol exists. The etiology of individual variability in the response to propofol may be influenced by genetic polymorphisms in metabolic and functional pathways. With current pharmacogenetics and modern molecular biology technologies, it is possible to study the influence of genetic polymorphisms on susceptibility to propofol. When inducing general anesthesia with intravenous propofol, high individual susceptibility to propofol was found. Using Sequenom MassARRAY single-nucleotide polymorphism (SNP) genotyping, we identified a mutation (rs6313) in the 5HT2A gene that was correlated to individual susceptibility to propofol effect-site concentration (Cep) and onset time of propofol induction...
June 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28546314/chronic-stress-induced-behavioral-changes-associated-with-subregion-selective-serotonin-cell-death-in-the-dorsal-raphe
#3
Reka Natarajan, Laura Forrester, Nicolas Chiaia, Bryan K Yamamoto
The current study examined the neurochemical mechanisms and neuroanatomical changes underlying co-existing behavioral effects associated with chronic stress-induced alterations in serotonin (5HT) neurons. Chronic unpredictable stress (CUS) to adult male rats produced depression-like changes with cognitive dysfunction and selective cell death in the interfascicular nucleus of the dorsal raphe (DRif) resulting in decreased 5HTergic innervation of medial prefrontal cortex (mPFC). Twenty-one days of CUS decreased basal plasma levels of corticosterone and produced a shorter latency to immobility and longer durations of immobility in the force-swim test that persisted for one month after CUS...
May 25, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28512684/therapeutic-applications-of-classic-hallucinogens
#4
Michael P Bogenschutz, Stephen Ross
This chapter reviews what is known about the therapeutic uses of the serotonergic or classic hallucinogens, i.e., psychoactive drugs such as LSD and psilocybin that exert their effects primarily through agonist activity at serotonin 2A (5HT2A) receptors. Following a review of the history of human use and scientific study of these drugs, the data from clinical research are summarized, including extensive work on the use of classic hallucinogens in the treatment of alcoholism and other addictions, studies of the use of LSD and psilocybin to relieve distress concerning death, particularly in patients with advanced or terminal cancer, and more limited data concerning the use of classic hallucinogens to treat mood and anxiety disorders...
May 18, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28459524/growing-evidence-for-heterogeneous-synaptic-localization-of-5-ht2a-receptors
#5
Carine Bécamel, Coralie Berthoux, Alexander Barre, Philippe Marin
The serotonin 2A (5-HT2A) receptor subtype continues to attract attention as a target for numerous psychoactive drugs including psychedelic hallucinogens, antidepressants, anxiolytics, and atypical antipsychotics. 5-HT2A receptors are a principal G protein-coupled receptor subtype mediating the excitatory effects of serotonin. Nonetheless, pre- vs postsynaptic localization of 5HT2A receptors, relative to glutamatergic synapses, has remained controversial. Here, we discuss recent findings highlighting the existence and roles of presynaptic 5-HT2A receptors in regulating glutamatergic transmission and cognition...
May 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28302574/the-arginine-vasotocin-and-serotonergic-systems-affect-interspecific-social-behaviour-of-client-fish-in-marine-cleaning-mutualism
#6
Zegni Triki, Redouan Bshary, Alexandra S Grutter, Albert F H Ros
Many species engage in mutualistic relationships with other species. The physiological mechanisms that affect the course of such social interactions are little understood. In the cleaning mutualism, cleaner fish Labroides dimidiatus do not always act cooperatively by eating ectoparasites, but sometimes cheat by taking bites of mucus from so-called "client" reef fish. The physiological mechanisms in these interspecific interactions, however, are little studied. Here, we focussed on three neuromodulator systems known to play important roles in intraspecific social behaviour of vertebrates to examine their role in clients' interspecific behaviour...
March 14, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28291301/-acute-dystonia-due-to-aripiprazole-use-in-two-children-with-autism-spectrum-disorder-in-the-first-five-years-of-life
#7
Mustafa Küçükköse, Bürge Kabukçu Başay
Autism spectrum disorders (ASD) are neuropsychiatric disorders characterized by impairment in social interactions, in verbal and non-verbal communication, and restricted and stereotyped patterns of interest and behavior within the first 3 years of life. Pharmacologic interventions may be needed for the treatment of temper tantrums, aggression, hyperactivity, and stereotypes in children with ASD. The approval of aripiprazole by the United States Food and Drug Administration (USFDA) for the treatment of temper tantrums in children and adolescents with ASD has gained increased interest for the use in these patients...
2017: Türk Psikiyatri Dergisi, Turkish Journal of Psychiatry
https://www.readbyqxmd.com/read/28202580/spinal-disinhibition-in-experimental-and-clinical-painful-diabetic-neuropathy
#8
Andrew G Marshall, Corinne Lee-Kubli, Shazli Azmi, Michael Zhang, Maryam Ferdousi, Teresa Mixcoatl-Zecuatl, Ioannis N Petropoulos, Georgios Ponirakis, Mark S Fineman, Hassan Fadavi, Katie Frizzi, Mitra Tavakoli, Maria Jeziorska, Corinne G Jolivalt, Andrew J M Boulton, Nathan Efron, Nigel A Calcutt, Rayaz A Malik
Impaired rate-dependent depression (RDD) of the Hoffman reflex is associated with reduced dorsal spinal cord potassium chloride cotransporter expression and impaired spinal γ-aminobutyric acid type A receptor function, indicative of spinal inhibitory dysfunction. We have investigated the pathogenesis of impaired RDD in diabetic rodents exhibiting features of painful neuropathy and the translational potential of this marker of spinal inhibitory dysfunction in human painful diabetic neuropathy. Impaired RDD and allodynia were present in type 1 and type 2 diabetic rats but not in rats with type 1 diabetes receiving insulin supplementation that did not restore normoglycemia...
May 2017: Diabetes
https://www.readbyqxmd.com/read/28125323/increased-levels-of-5ht2a-receptor-mrna-expression-in-peripheral-blood-mononuclear-cells-of-patients-with-major-depression-correlations-with-severity-and-duration-of-illness
#9
Meysam Amidfar, Yong-Ku Kim, Lejla Colic, Mohammad Arbabi, Gholamhossein Mobaraki, Gholamreza Hassanzadeh, Martin Walter
BACKGROUND: Neuroimaging, immunologic, and pharmacologic studies have emphasized the role of 5-HT2A and 5-HT3A serotonin receptors in the pathophysiology of major depression. AIM: The aim of this study was to measure the relative expression of 5-HT2A and 5-HT3A receptor mRNA in peripheral blood mononuclear cells (PBMCs) of patients with major depressive disorder (MDD). METHOD: 5-HT2A and 5-HT3A receptor mRNA expressions were examined in PBMCs of 25 medication-naïve-patients with MDD, 25 medication-free MDD patients, and 25 healthy controls...
May 2017: Nordic Journal of Psychiatry
https://www.readbyqxmd.com/read/28057699/glucagon-like-peptide-1-and-its-analogs-act-in-the-dorsal-raphe-and-modulate-central-serotonin-to-reduce-appetite-and-body-weight
#10
Rozita H Anderberg, Jennifer E Richard, Kim Eerola, Lorena López-Ferreras, Elin Banke, Caroline Hansson, Hans Nissbrandt, Filip Berqquist, Fiona M Gribble, Frank Reimann, Ingrid Wernstedt Asterholm, Christophe M Lamy, Karolina P Skibicka
Glucagon-like peptide 1 (GLP-1) and serotonin play critical roles in energy balance regulation. Both systems are exploited clinically as antiobesity strategies. Surprisingly, whether they interact in order to regulate energy balance is poorly understood. Here we investigated mechanisms by which GLP-1 and serotonin interact at the level of the central nervous system. Serotonin depletion impaired the ability of exendin-4, a clinically used GLP-1 analog, to reduce body weight in rats, suggesting that serotonin is a critical mediator of the energy balance impact of GLP-1 receptor (GLP-1R) activation...
April 2017: Diabetes
https://www.readbyqxmd.com/read/27896660/ayahuasca-exposure-descriptive-analysis-of-calls-to-us-poison-control-centers-from-2005-to-2015
#11
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
#12
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...
January 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27800022/evidence-for-the-use-of-pimavanserin-in-the-treatment-of-parkinson-s-disease-psychosis
#13
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
#14
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...
December 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27717169/5ht2a-receptor-blockade-in-dorsomedial-striatum-reduces-repetitive-behaviors-in-btbr-mice
#15
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...
March 2017: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/27687785/an-original-pharmacoepidemiological-pharmacodynamic-method-application-to-antipsychotic-induced-movement-disorders
#16
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 that are 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 dopamine D2, serotonin 5HT2A, and muscarinic M1 receptor occupancy and the risks of antipsychotic drug (AP)-induced movement disorders...
March 2017: 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
#17
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...
September 22, 2016: Toxins
https://www.readbyqxmd.com/read/27619519/cholinergic-and-serotonergic-modulation-of-visual-information-processing-in-monkey-v1
#18
REVIEW
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 2016: Journal of Physiology, Paris
https://www.readbyqxmd.com/read/27572262/serotonin-signaling-mediates-protein-valuation-and-aging
#19
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
#20
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
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