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https://www.readbyqxmd.com/read/27912162/serotonin-2a-receptor-5-ht2a-gene-promoter-variant-interacts-with-chronic-perceived-stress-to-modulate-resting-parasympathetic-activity-in-humans
#1
Chuan-Chia Chang, Wen-Hui Fang, Hsin-An Chang, Tieh-Ching Chang, Jia-Fwa Shyu, San-Yuan Huang
Decreased resting vagal (parasympathetic) tone is implicated in the development of stress-related disorders, including anxiety and depression. Chronic stress elevates the expression of serotonin 2A receptors (5-HT2A), while activation of 5-HT2A leads to inhibition of parasympathetic synaptic transmission. The T allele of the promoter variant, rs6311 (C>T), of the 5-HT2A gene has been shown to increase the 5-HT2A expression in vitro and to be associated with anxiety and depressive disorders. We thus hypothesized that the 5-HT2A functional polymorphism may influence resting vagal activity among persons with chronically high levels of perceived stress...
November 16, 2016: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/27909009/association-of-protein-distribution-and-gene-expression-revealed-by-pet-and-post-mortem-quantification-in-the-serotonergic-system-of-the-human-brain
#2
A Komorowski, G M James, C Philippe, G Gryglewski, A Bauer, M Hienert, M Spies, A Kautzky, T Vanicek, A Hahn, T Traub-Weidinger, D Winkler, W Wadsak, M Mitterhauser, M Hacker, S Kasper, R Lanzenberger
Regional differences in posttranscriptional mechanisms may influence in vivo protein densities. The association of positron emission tomography (PET) imaging data from 112 healthy controls and gene expression values from the Allen Human Brain Atlas, based on post-mortem brains, was investigated for key serotonergic proteins. PET binding values and gene expression intensities were correlated for the main inhibitory (5-HT1A) and excitatory (5-HT2A) serotonin receptor, the serotonin transporter (SERT) as well as monoamine oxidase-A (MAO-A), using Spearman's correlation coefficients (rs) in a voxel-wise and region-wise analysis...
November 30, 2016: Cerebral Cortex
https://www.readbyqxmd.com/read/27903793/the-serotonin-5-ht2c-receptor-and-the-non-addictive-nature-of-classic-hallucinogens
#3
REVIEW
Clinton E Canal, Kevin S Murnane
Classic hallucinogens share pharmacology as serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptor agonists. Unique among most other Schedule 1 drugs, they are generally non-addictive and can be effective tools in the treatment of addiction. Mechanisms underlying these attributes are largely unknown. However, many preclinical studies show that 5-HT2C agonists counteract the addictive effects of drugs from several classes, suggesting this pharmacological property of classic hallucinogens may be significant. Drawing from a comprehensive analysis of preclinical behavior, neuroanatomy, and neurochemistry studies, this review builds rationale for this hypothesis, and also proposes a testable, neurobiological framework...
November 15, 2016: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/27900674/serotonergic-hallucinogen-induced-visual-perceptual-alterations
#4
Michael Kometer, Franz X Vollenweider
Serotonergic hallucinogens, such as lysergic acid diethylamide (LSD), psilocybin, and N,N-dimethyltryptamine (DMT), are famous for their capacity to temporally and profoundly alter an individual's visual experiences. These visual alterations show consistent attributes despite large inter- and intra-individual variances. Many reports document a common perception of colors as more saturated, with increased brightness and contrast in the environment ("Visual Intensifications"). Environmental objects might be altered in size ("Visual illusions") or take on a modified and special meaning for the subject ("Altered self-reference")...
November 30, 2016: Current Topics in Behavioral Neurosciences
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
#5
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/27886063/d-lysergic-acid-diethylamide-lsd-as-a-model-of-psychosis-mechanism-of-action-and-pharmacology
#6
REVIEW
Danilo De Gregorio, Stefano Comai, Luca Posa, Gabriella Gobbi
d-Lysergic Acid Diethylamide (LSD) is known for its hallucinogenic properties and psychotic-like symptoms, especially at high doses. It is indeed used as a pharmacological model of psychosis in preclinical research. The goal of this review was to understand the mechanism of action of psychotic-like effects of LSD. We searched Pubmed, Web of Science, Scopus, Google Scholar and articles' reference lists for preclinical studies regarding the mechanism of action involved in the psychotic-like effects induced by LSD...
November 23, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27857753/serotonin-regulates-brain-derived-neurotrophic-factor-expression-in-select-brain-regions-during-acute-psychological-stress
#7
De-Guo Jiang, Shi-Li Jin, Gong-Ying Li, Qing-Qing Li, Zhi-Ruo Li, Hong-Xia Ma, Chuan-Jun Zhuo, Rong-Huan Jiang, Min-Jie Ye
Previous studies suggest that serotonin (5-HT) might interact with brain-derived neurotrophic factor (BDNF) during the stress response. However, the relationship between 5-HT and BDNF expression under purely psychological stress is unclear. In this study, one hour before psychological stress exposure, the 5-HT1A receptor agonist 8-OH-DPAT or antagonist MDL73005, or the 5-HT2A receptor agonist DOI or antagonist ketanserin were administered to rats exposed to psychological stress. Immunohistochemistry and in situ hybridization revealed that after psychological stress, with the exception of the ventral tegmental area, BDNF protein and mRNA expression levels were higher in the 5-HT1A and the 5-HT2A receptor agonist groups compared with the solvent control no-stress or psychological stress group in the CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and the midbrain periaqueductal gray...
September 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/27857126/repeated-7-day-treatment-with-the-5-ht2c-agonist-lorcaserin-or-the-5-ht2a-antagonist-pimavanserin-alone-or-in-combination-fails-to-reduce-cocaine-vs-food-choice-in-male-rhesus-monkeys
#8
Matthew L Banks, S Stevens Negus
Cocaine use disorder is a global public health problem for which there are no Food and Drug Administration-approved pharmacotherapies. Emerging preclinical evidence has implicated both serotonin (5-HT) 2C and 2A receptors as potential mechanisms for mediating serotonergic attenuation of cocaine abuse-related neurochemical and behavioral effects. Therefore, the present study aim was to determine whether repeated 7-day treatment with the 5-HT2C agonist lorcaserin (0.1-1.0 mg/kg/day, intramuscular; 0.032-0.1 mg/kg/h, intravenous) or the 5-HT2A inverse agonist/antagonist pimavanserin (0...
November 18, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27856786/a-high-resolution-in-vivo-atlas-of-the-human-brain-s-serotonin-system
#9
Vincent Beliveau, Melanie Ganz, Ling Feng, Brice Ozenne, Liselotte Højgaard, Patrick M Fisher, Claus Svarer, Douglas N Greve, Gitte M Knudsen
: The serotonin (5-HT) system modulates many important brain functions and is critically involved in many neuropsychiatric disorders. We here present a high-resolution multi-dimensional in vivo atlas of four of the human brain's 5-HT receptors (5-HT1A, 5-HT1B, 5-HT2A, and 5-HT4) as well as of 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...
November 17, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27856625/longitudinal-micropet-imaging-of-the-zq175-mouse-model-of-huntington-s-disease-shows-in-vivo-changes-of-molecular-targets-in-the-striatum-and-the-cerebral-cortex
#10
Jenny Häggkvist, Miklós Tóth, Lenke Tari, Katarina Varnäs, Marie Svedberg, Anton Forsberg, Sangram Nag, Celia Dominguez, Ignacio Munoz-Sanjuan, Jonathan Bard, John Wityak, Andrea Varrone, Christer Halldin, Ladislav Mrzljak
RATIONALE: Since the discovery of the HTT gene in 1993, numerous animal models have been developed to study the progression of Huntington's disease, as well as to evaluate potential new therapeutics. In the present study we used small animal positron emission tomography (PET) to characterize the expression of molecular targets in the recently reported HD animal model, the zQ175 mouse model. METHODS: Male heterozygous zQ175 (Htttm1Mfc/190JChdi, CHDI-81003003) and wild type (WT, C57BL/6J) animals were imaged with the dopamine D2-receptor radioligand [(11)C]raclopride, the PDE10A radioligand [(18)F]MNI-659, the dopamine D1-receptor radioligand [(11)C]NNC 112 and the 5-HT2A radioligand [(11)C]MDL 100907 at 6 and 9 months of age...
November 10, 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27847437/facilitation-of-serotonin-induced-contraction-of-rat-mesenteric-artery-by-ketamine
#11
Sang Woong Park, Hyun Ju Noh, Jung Min Kim, Bokyung Kim, Sung-Il Cho, Yoon Soo Kim, Nam Sik Woo, Sung Hun Kim, Young Min Bae
Ketamine is an anesthetic with hypertensive effects, which make it useful for patients at risk of shock. However, previous ex vivo studies reported vasodilatory actions of ketamine in isolated arteries. In this study, we reexamined the effects of ketamine on arterial tones in the presence and absence of physiological concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) by measuring the isometric tension of endothelium-denuded rat mesenteric arterial rings. Ketamine little affected the resting tone of control mesenteric arterial rings, but, in the presence of 5-HT (100~200 nM), ketamine (10~100 µM) markedly contracted the arterial rings...
November 2016: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/27833522/histamine-h3-receptors-and-its-antagonism-as-a-novel-mechanism-for-antipsychotic-effect-a-current-preclinical-clinical-perspective
#12
REVIEW
Danish Mahmood
Histamine H3 receptors are present as autoreceptors on histaminergic neurons and as heteroreceptors on nonhistaminergic neurones. They control the release and synthesis of histamine and several other key neurotransmitters in the brain. H3 antagonism may be a novel approach to develop a new class of antipsychotic medications given the gathering evidence reporting therapeutic efficacy in several central nervous system disorders. Several medications such as cariprazine, lurasidone, LY214002, bexarotene, rasagiline, raloxifene, BL-1020 and ITI-070 are being developed to treat the negative symptoms and cognitive impairments of schizophrenia...
October 2016: International Journal of Health Sciences
https://www.readbyqxmd.com/read/27830568/psychosis-in-parkinson-disease-a-review-of-etiology-phenomenology-and-management
#13
REVIEW
Niyatee Samudra, Neepa Patel, Kyle B Womack, Pravin Khemani, Shilpa Chitnis
Parkinson disease psychosis (PDP) is a common phenomenon in Parkinson disease (PD) patients treated with dopaminergic drugs, and is associated with high morbidity and mortality. It also correlates with depression and dementia, and can contribute to considerable caregiver stress and burnout. While symptoms can be relieved by decreasing doses or number of anti-PD medications, this may lead to an unacceptable worsening of motor function. When general medical or psychiatric conditions have been ruled out, and decreasing dopaminergic agents is not effective in treating psychosis, therapies include atypical antipsychotics, primarily clozapine and quetiapine...
December 2016: Drugs & Aging
https://www.readbyqxmd.com/read/27824106/peripheral-and-spinal-5-ht-receptors-participate-in-cholestatic-itch-and-antinociception-induced-by-bile-duct-ligation-in-rats
#14
Bin Tian, Xue-Long Wang, Ya Huang, Li-Hua Chen, Ruo-Xiao Cheng, Feng-Ming Zhou, Ran Guo, Jun-Cheng Li, Tong Liu
Although 5-HT has been implicated in cholestatic itch and antinociception, two common phenomena in patients with cholestatic disease, the roles of 5-HT receptor subtypes are unclear. Herein, we investigated the roles of 5-HT receptors in itch and antinociception associated with cholestasis, which was induced by common bile duct ligation (BDL) in rats. 5-HT-induced enhanced scratching and antinociception to mechanical and heat stimuli were demonstrated in BDL rats. 5-HT level in the skin and spinal cord was significantly increased in BDL rats...
November 8, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27810345/classical-hallucinogens-and-neuroimaging-a-systematic-review-of-human-studies-hallucinogens-and-neuroimaging
#15
REVIEW
Rafael G Dos Santos, Flávia L Osório, José Alexandre S Crippa, Jaime E C Hallak
Serotonergic hallucinogens produce alterations of perceptions, mood, and cognition, and have anxiolytic, antidepressant, and antiaddictive properties. These drugs act as agonists of frontocortical 5-HT2A receptors, but the neural basis of their effects are not well understood. Thus, we conducted a systematic review of neuroimaging studies analyzing the effects of serotonergic hallucinogens in man. Studies published in the PubMed, Lilacs, and SciELO databases until 12 April 2016 were included using the following keywords: "ayahuasca", "DMT", "psilocybin", "LSD", "mescaline" crossed one by one with the terms "mri", "fmri", "pet", "spect", "imaging" and "neuroimaging"...
October 31, 2016: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/27793702/clinical-and-biological-predictors-of-response-to-electroconvulsive-therapy-ect-a-review
#16
REVIEW
Martina Pinna, Mirko Manchia, Rossana Oppo, Filomena Scano, Gianluca Pillai, Anna Paola Loche, Piergiorgio Salis, Gian Paolo Minnai
Electroconvulsive therapy (ECT), developed in the 30's by Bini and Cerletti, remains a key element of the therapeutic armamentarium in psychiatry, particularly for severe and life-threatening psychiatric symptoms. However, despite its well-established clinical efficacy, the prescription of ECT has declined constantly over the years due to concerns over its safety (cognitive side effects) and an increasingly negative public perception. As for other treatments in the field of psychiatry, ECT is well suited to a personalized approach that would increment its efficacy, as well as reducing the impact of side effects...
October 25, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27788033/effects-of-antipsychotic-drugs-haloperidol-and-clozapine-on-visual-responses-of-retinal-ganglion-cells-in-a-rat-model-of-retinitis-pigmentosa
#17
Ralph J Jensen
PURPOSE: In the P23H rat model of retinitis pigmentosa, the dopamine D2 receptor antagonists sulpiride and eticlopride appear to improve visual responses of retinal ganglion cells (RGCs) by increasing light sensitivity of RGCs and transforming abnormal, long-latency ON-center RGCs into OFF-center cells. Antipsychotic drugs are believed to mediate their therapeutic benefits by blocking D2 receptors. This investigation was conducted to test whether haloperidol (a typical antipsychotic drug) and clozapine (an atypical antipsychotic drug) could similarly alter the light responses of RGCs in the P23H rat retina...
October 27, 2016: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27781135/adjunctive-brexpiprazole-in-patients-with-major-depressive-disorder-and-anxiety-symptoms-an-exploratory-study
#18
Lori L Davis, Ai Ota, Pamela Perry, Kana Tsuneyoshi, Emmanuelle Weiller, Ross A Baker
BACKGROUND: Major depressive disorder (MDD) with concurrent anxiety symptoms may signal a difficult-to-treat patient. Brexpiprazole is a serotonin-dopamine activity modulator: a partial agonist at 5-HT1A and dopamine D2 receptors at similar potency, and an antagonist at 5-HT2A and noradrenaline alpha1B/2C receptors. The objective of this Phase IIIb study was to explore effectiveness, safety, and tolerability of brexpiprazole adjunctive to antidepressant (ADT) monotherapy in patients with MDD and anxiety symptoms (NCT02013531)...
October 2016: Brain and Behavior
https://www.readbyqxmd.com/read/27771722/inhibitory-effects-of-antidepressants-on-acetylcholine-induced-contractions-in-isolated-guinea-pig-urinary-bladder-smooth-muscle
#19
Junji Uno, Keisuke Obara, Hiroko Suzuki, Satomi Miyatani, Daisuke Chino, Takashi Yoshio, Yoshio Tanaka
BACKGROUND/AIMS: To investigate the potential inhibitory effects of 18 clinically available antidepressants on acetylcholine (ACh)-induced contractions in guinea pig urinary bladder smooth muscle (UBSM) in order to predict whether they may induce voiding impairment. METHODS: Concentration-response curves for ACh-induced contractions in guinea pig UBSM strips were obtained in the absence or presence of selected antidepressants. When inhibitory effects indicated competitive antagonism, pA2 values against ACh were calculated and compared to plausible antidepressant blood concentrations...
October 22, 2016: Pharmacology
https://www.readbyqxmd.com/read/27761079/elucidation-of-molecular-mechanism-s-of-cognition-enhancing-activity-of-bacomind-%C3%A2-a-standardized-extract-of-bacopa-monnieri
#20
Shekhar Dethe, M Deepak, Amit Agarwal
BACKGROUND: Bacopa monnieri (L.) Wettst., commonly known as Brahmi, is renowned in Indian traditional system for its potent memory enhancing activity, which has been validated by various scientific studies. OBJECTIVE: The objective of this study was to understand the molecular mechanism of memory enhancing activity of BacoMind(®) (BM), a standardized extract of B. monnieri. MATERIALS AND METHODS: BM was screened in vitro in a panel of cell-free and receptor-transfected cell assays...
July 2016: Pharmacognosy Magazine
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