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https://www.readbyqxmd.com/read/28637246/effect-of-psilocybin-on-empathy-and-moral-decision-making
#1
Thomas Pokorny, Katrin H Preller, Michael Kometer, Isabel Dziobek, Franz X Vollenweider
Background: Impaired empathic abilities lead to severe negative social consequences and influence the development and treatment of several psychiatric disorders. Furthermore, empathy has been shown to play a crucial role in moral and prosocial behaviour. Although the serotonin (5-HT) system has been implicated in modulating empathy and moral behaviour, the relative contribution of the various 5-HT receptor subtypes is still unknown. Methods: We investigated the acute effect of psilocybin (0...
June 16, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28636360/proneurogenic-effects-of-trazodone-in-murine-and-human-neural-progenitors
#2
Valeria Bortolotto, Francesca Mancini, Giorgina Mangano, Rita Salem, Er Xia, Erika Del Grosso, Michele Bianchi, Pier Luigi Canonico, Lorenzo Polenzani, Mariagrazia Grilli
Several antidepressants increase adult hippocampal Neurogenesis (ahNG) in rodents, primates and, potentially, in humans. This effect may at least partially account for their therapeutic activity. The availability of antidepressants whose mechanism of action involves different neurotransmitter receptors represents an opportunity for increasing our knowledge on their distinctive peculiarities and for dissecting the contribution of receptor subtypes in ahNG modulation. The aim of this study was to evaluate, in vitro, the effects of the antidepressant trazodone (TZD) on ahNG by using primary cultures of adult hippocampal Neural Progenitor Cells (ahNPC) and human iPSC-derived NPC...
June 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28635286/utilization-of-an-active-site-mutant-receptor-for-the-identification-of-potent-and-selective-atypical-5-ht2c-receptor-agonists
#3
Joseph Carpenter, Ying Wang, Gang Wu, Jianxin Feng, Xiang-Yang Ye, Christian L Morales, Matthias Broekema, Karen A Rossi, Keith J Miller, Brian J Murphy, Ginger Yingzhe Wu, Sarah E Malmstrom, Anthony V Azzara, Philip M Sher, John M Fevig, Andrew Alt, Robert L Bertekap, Mary Jane Cullen, Timothy M Harper, Kimberly A Foster, Chiuwa Emily Luk, Qian Xiang, Mary F Grubb, Jeffrey A Robl, Dean A Wacker
Agonism of the 5-HT2C receptor represents one of the most well-studied and clinically-proven mechanisms for pharmacological weight reduction. Selectivity over the closely related 5-HT2A and 5-HT2B receptors is critical as their activation has been shown to lead to undesirable side-effects and major safety concerns. In this communication, we report the development of a new screening paradigm which utilizes an active site mutant D134A 5-HT2C receptor to identify atypical agonist structures. We additionally report the discovery and optimization of a novel class of non-basic heterocyclic amide agonists of 5-HT2C...
June 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28628756/atypical-sympathomimetic-drug-lerimazoline-mediates-contractile-effects-in-rat-aorta-predominantly-by-5-ht2a-receptors
#4
Eldina Rizvić, Goran Janković, Slađana Kostić-Rajačić, Miroslav M Savić
Lerimazoline is a sympathomimetic drug that belongs to the imidazoline class of compounds, and is used as a nasal decongestant. Studies on lerimazoline are rare, and its pharmacological profile is not completely understood. Here, we analyzed the affinity of lerimazoline for dopamine receptor D2, serotonin 5-HT1A and 5-HT2A receptors and α1-adrenoceptor, and investigated lerimazoline contractile effects in isolated rat thoracic aorta. We also determined the effect of several antagonists on the contractile response to lerimazoline, including prazosin (α1-adrenoceptor antagonist), RX 821002 and rauwolscine (α2-adrenoceptor antagonists), JP 1302 (α2C-adrenoceptor antagonist), methiothepin (non-selective 5-HT receptor antagonist), SB 224289 (5-HT1B receptor antagonist), BRL 15572 (5-HT1D receptor antagonist), and ketanserin (5-HT2A receptor antagonist)...
June 19, 2017: Bosnian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28626787/5-ht2a-receptor-deficiency-alters-the-metabolic-and-transcriptional-but-not-the-behavioral-consequences-of-chronic-unpredictable-stress
#5
Minal Jaggar, Noelia Weisstaub, Jay A Gingrich, Vidita A Vaidya
Chronic stress enhances risk for psychiatric disorders, and in animal models is known to evoke depression-like behavior accompanied by perturbed neurohormonal, metabolic, neuroarchitectural and transcriptional changes. Serotonergic neurotransmission, including serotonin2A (5-HT2A) receptors, have been implicated in mediating specific aspects of stress-induced responses. Here we investigated the influence of chronic unpredictable stress (CUS) on depression-like behavior, serum metabolic measures, and gene expression in stress-associated neurocircuitry of the prefrontal cortex (PFC) and hippocampus in 5-HT2A receptor knockout (5-[Formula: see text]) and wild-type mice of both sexes...
December 2017: Neurobiology of Stress
https://www.readbyqxmd.com/read/28624893/ly294002-a-pi3k-inhibitor-attenuates-tourette-syndrome-in-rats
#6
Long Hongyan, Wang Chunyan, Yang Yue'e
The present study was designed to investigate the effects of LY294002 on Tourette syndrome (TS) in rats. TS model was induced in rats by DOI (the selective 5-HT2A/2C agonist 1- (2, 5- dimethoxy -4 - iodophenyl) -2- aminopropane). Behavior was assessed by stereotypic score and autonomic activity. Inflammatory cytokines such as interleukin-6 (IL-6), interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) in serum and striatum were detected. The protein levels of PI3K/Akt/NF-B in striatum were detected by Western Blot...
June 18, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28623711/contribution-of-dopaminergic-and-noradrenergic-systems-in-the-antinociceptive-effect-of-%C3%AE-phenylalanyl-acetophenone
#7
Fernanda S S Sousa, Roberta G Anversa, Paloma T Birmann, Maurice N de Souza, Renata Balaguez, Diego Alves, Cristiane Luchese, Ethel A Wilhelm, Lucielli Savegnago
BACKGROUND: This study evaluated the antinociceptive action of α-(phenylalanyl) acetophenone (PSAP) in mice. METHODS: Evaluated whether the serotonergic, adrenergic and dopaminergic systems are involved in PSAP antinociceptive activity. PSAP was administered intragastrically (ig) 30min prior to formalin or glutamate test and compared with a standard drug, meloxicam (10mg/kg, ig). RESULTS: The treatment with PSAP (10-50mg/kg) caused inhibition in the neurogenic phase and reduced the paw oedema caused by intraplantar (ipl) injection of formalin...
March 27, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28623179/modulation-of-tgf-%C3%AE-smad-and-erk-signaling-pathways-mediates-the-anti-fibrotic-effect-of-mirtazapine-in-mice
#8
Dalia M El-Tanbouly, Walaa Wadie, Rabab H Sayed
Serotonin (5-HT) has been implicated as a key driver of liver fibrosis, acting via 5-HT2 receptor activation in the hepatic stellate cells. The current study was conducted to investigate the effects of mirtazapine, a 5-HT2A antagonist, in a mouse model of liver fibrosis. Mice received thioacetamide (TAA, 150mg/kg/biweekly, ip) for nine successive weeks for induction of liver fibrosis. Administration of mirtazapine significantly improved the plasma aminotransferases, reduced hepatic 5-HT concentration and ameliorated TAA-induced liver fibrosis, as demonstrated by reduced portal blood pressure, liver procollagen I content and α alpha smooth muscle actin expression...
June 13, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28622212/a-retrospective-study-of-pimavanserin-use-in-a-movement-disorders-clinic
#9
Joseph H Friedman
Pimavanserin, a 5-HT2A inverse agonist, was commercially released in the United States in April 2016 for the treatment of Parkinson disease psychosis. No "naturalistic" treatment results have yet been published. Charts from the movement disorders clinic were reviewed for all patients who received this drug as treatment for psychosis associated with primary parkinsonism due to α-synucleinopathies. Data of 10 patients with idiopathic Parkinson disease, including 1 with a long history of schizophrenia, 4 with dementia with Lewy bodies, and 1 with multiple-system atrophy, were reviewed...
June 16, 2017: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/28608926/the-pharmacodynamic-effects-of-combined-administration-of-flibanserin-and-alcohol
#10
D M Stevens, J M Weems, L Brown, K A Barbour, S M Stahl
WHAT IS KNOWN AND OBJECTIVE: Flibanserin is a serotonin 5-HT1A agonist and 5-HT2A antagonist approved for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. Because of the increased risk of hypotension- and syncope-related adverse events (AEs) observed with coadministration of flibanserin and alcohol, alcohol use is contraindicated. To provide a more comprehensive understanding of the interaction between flibanserin and alcohol, the results of a dedicated phase 1 alcohol-interaction study and a pooled analysis of phase 3 studies of premenopausal women with HSDD are presented...
June 13, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28597539/developmental-effects-of-antipsychotic-drugs-on-serotonin-receptor-subtypes
#11
Yong Kee Choi, Matthew P Gardner, Frank I Tarazi
Antipsychotic medications are increasingly prescribed to pediatric and adolescent patients with psychotic diseases in spite of limited knowledge on the long-term effects of dissimilar antipsychotic drugs on developing brain. In this study, we quantified the levels of two major serotonin 5-HT1A , and 5-HT2A receptors in brain regions of developing rats after 3 weeks of treatment with typical (fluphenazine) and atypical (clozapine and olanzapine) antipsychotics, and compared to similarly treated adult rats treated with olanzapine, risperidone and quetiapine examined in previous studies...
June 8, 2017: Synapse
https://www.readbyqxmd.com/read/28594246/a-review-of-vilazodone-exposures-with-focus-on-serotonin-syndrome-effects
#12
C William Heise, Hannah Malashock, Daniel E Brooks
BACKGROUND: Vilazodone is an antidepressant with selective serotonin reuptake inhibition and partial 5HT1A agonism. Serotonin syndrome is believed to be due to excessive stimulation of 5-HT2A and 5-HT1A receptors, resulting in the clinical triad of altered mentation, autonomic instability and neuromuscular abnormalities. The goal of this study is to define serotonergic effects after vilazodone exposure. METHODS: A retrospective review of two databases: the American Association of Poison Controls Centers' National Poison Data System (NPDS) and the American College of Medical Toxicology's Toxicology Investigators Consortium (ToxIC Registry)...
June 8, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28588509/behavioral-effects-of-a-novel-benzofuranyl-piperazine-serotonin-2c-receptor-agonist-suggest-a-potential-therapeutic-application-in-the-treatment-of-obsessive-compulsive-disorder
#13
Michelle M Rodriguez, Carl Overshiner, J David Leander, Xia Li, Denise Morrow, Richard G Conway, David L Nelson, Karin Briner, Jeffrey M Witkin
Selective serotonin reuptake inhibitors (SSRIs) are the only effective pharmacological treatments for obsessive-compulsive disorder (OCD). Nonetheless, their generally limited efficacy, side-effects, and delayed onset of action require improved medications for this highly prevalent disorder. Preclinical and clinical findings have suggested serotonin2C (5-HT2C) receptors as a potential drug target. Data in rats and mice are presented here on the effects of a novel 5-HT2C receptor agonist ((3S)-3-Methyl-1-[4-(trifluoromethyl)-7-benzofuranyl]-piperazine) (CPD 1) with high potency and full efficacy at 5-HT2C receptors and less potency and partial agonism at 5-HT2A and 5-HT2B receptors...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28585392/return-of-the-lysergamides-part-iv-analytical-and-pharmacological-characterization-of-lysergic-acid-morpholide-lsm-775
#14
Simon D Brandt, Pierce V Kavanagh, Brendan Twamley, Folker Westphal, Simon P Elliott, Jason Wallach, Alexander Stratford, Landon M Klein, John D McCorvy, David E Nichols, Adam L Halberstadt
Lysergic acid diethylamide (LSD) is perhaps one of the best-known psychoactive substances and many structural modifications of this prototypical lysergamide have been investigated. Several lysergamides were recently encountered as "research chemicals" or new psychoactive substances (NPS). Although lysergic acid morpholide (LSM-775) appeared on the NPS market in 2013, there is disagreement in the literature regarding the potency and psychoactive properties of LSM-775 in humans. The present investigation attempts to address the gap of information that exists regarding the analytical profile and pharmacological effects of LSM-775...
June 5, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28577964/rp5063-a-novel-multimodal-serotonin-receptor-modulator-prevents-monocrotaline-induced-pulmonary-arterial-hypertension-in-rats
#15
Laxminarayan Bhat, Jon Hawkinson, Marc Cantillon, Dasharatha G Reddy, Seema R Bhat, Charles E Laurent, Annie Bouchard, Marzena Biernat, Dany Salvail
Pulmonary arterial hypertension (PAH), a condition characterized by pulmonary vasculature constriction and remodeling, involves dysregulation of the serotonin (5-HT) receptors 5-HT2A and 5-HT2B. A rat model of monocrotaline (MCT)-induced PAH was used to examine the potential beneficial effects of RP5063, a 5-HT receptor modulator. After a single 60 mg/kg dose of MCT, rats were gavaged twice-daily (b.i.d.) with vehicle, RP5063 (1, 3, or 10 mg/kg), or sildenafil (50 mg/kg) for 28 days. RP5063 at a dose as low as 1 mg/kg, b...
May 31, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28576407/rp5063-a-novel-multimodal-serotonin-receptor-modulator-prevents-sugen-5416-hypoxia-induced-pulmonary-arterial-hypertension-in-rats
#16
Laxminarayan Bhat, Jon Hawkinson, Marc Cantillon, Dasharatha G Reddy, Seema R Bhat, Charles E Laurent, Annie Bouchard, Marzena Biernat, Dany Salvail
RP5063, a multimodal dopamine (DA) and serotonin (5-HT) modulator with high affinity for DA2/3/4 and 5-HT2A/2B/7 receptors and moderate affinity for SERT, is a novel therapeutic of special interest in the treatment of pulmonary arterial hypertension (PAH). Evidence indicates that therapeutics targeting the 5-HT2A/2B receptors can influence the pathogenesis of PAH. However, the effect of RP5063 has yet to be investigated. A Sugen 5416-hypoxia (SuHx)-induced PAH model was used to evaluate twice-daily (b.i.d.) RP5063 at 10 mg/kg (RP-10) and 20 mg/kg (RP-20), as compared with positive (sildenafil 50 mg/kg b...
May 31, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28575721/synthesis-of-a-new-series-of-aryl-heteroarylpiperazinyl-derivatives-of-8-acetyl-7-hydroxy-4-methylcoumarin-with-low-nanomolar-5-ht1a-affinities
#17
Kinga Ostrowska, Katarzyna Młodzikowska, Monika Głuch-Lutwin, Anna Gryboś, Agata Siwek
We synthesized a series of aryl/heteroarylpiperazinyl derivatives of 8-acetyl-7-hydroxy-4-methylcoumarin and evaluated their antidepressant-like activity. We used a fast, microwave-assisted synthesis protocol and (1)H, (13)C NMR and HRMS spectrometry to confirm the structure of all compounds. We also used radioligand binding assays to determine the affinities towards 5-HT1A and 5-HT2A receptors and performed molecular docking studies to rationalize obtained results. Among the evaluated compounds seven displayed high affinity to the 5-HT1A (3a-1...
May 26, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28566634/effect-of-docosahexaenoic-acid-on-voltage-independent-ca-2-entry-pathways-in-cultured-vascular-smooth-muscle-cells-stimulated-with-5-hydroxytryptamine
#18
Takuji Machida, Akina Onoguchi, Kenji Iizuka, Sayuri Ishibashi, Mikiko Yutani, Masahiko Hirafuji
We previously reported that docosahexaenoic acid (DHA) inhibits an increase in intracellular Ca(2+) concentration ([Ca(2+)]i) in cultured rat vascular smooth muscle cells (VSMCs) through a mechanism involving mainly voltage-dependent Ca(2+) channels; however, the effect of DHA on voltage-independent pathways, such as store-operated and receptor-operated Ca(2+) entry, and Ca(2+) entry through Na(+)/Ca(2+) exchanger (NCX), has not been clarified. In the present study, we investigated the effect of DHA treatment on the expression of transient receptor potential canonical (TRPC) channels, capacitative Ca(2+) entry, and Ca(2+) entry through NCX in rat cultured VSMCs stimulated with 5-hydroxytryptamine (5-HT)...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28555112/caveolin-1-functional-insights-into-its-role-in-muscarine-and-serotonin-induced-smooth-muscle-constriction-in-murine-airways
#19
Maryam Keshavarz, Heike Schwarz, Petra Hartmann, Silke Wiegand, Melanie Skill, Mike Althaus, Wolfgang Kummer, Gabriela Krasteva-Christ
An increased bronchoconstrictor response is a hallmark in the progression of obstructive airway diseases. Acetylcholine and 5-hydroxytryptamine (5-HT, serotonin) are the major bronchoconstrictors. There is evidence that both cholinergic and serotonergic signaling in airway smooth muscle (ASM) involve caveolae. We hypothesized that caveolin-1 (cav-1), a structural protein of caveolae, plays an important regulatory role in ASM contraction. We analyzed airway contraction in different tracheal segments and extra- and intrapulmonary bronchi in cav-1 deficient (cav-1-/-) and wild-type mice using organ bath recordings and videomorphometry of methyl-beta-cyclodextrin (MCD) treated and non-treated precision-cut lung slices (PCLS)...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28551554/antihyperalgesic-activity-of-a-mexicanolide-isolated-from-swietenia-humilis-extract-in-nicotinamide-streptozotocin-hyperglycemic-mice
#20
Berenice Ovalle-Magallanes, Myrna Déciga-Campos, Rachel Mata
Swietenia humilis Zucc. (Meliaceae) seeds are used in Mexico for the treatment of type 2 diabetes mellitus. Mexicanolides are the main hypoglycemic and antihyperglycemic compounds of the species. This study was conducted to investigate the antihyperalgesic effect of an aqueous extract of the seeds of Swietenia humilis (SHAE) and of mexicanolide 2-hydroxy-destigloyl-6-deoxyswietenine acetate (1), using the formalin test in mice. The antihyperalgesic actions of SHAE and mexicanolide 1, as well as its possible transductional activity, were assessed in nicotinamide-streptozotocin (NA-STZ) hyperglycemic mice...
May 25, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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