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5-HT2A

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https://www.readbyqxmd.com/read/28920103/existence-of-brain-5-ht1a-5-ht2a-isoreceptor-complexes-with-antagonistic-allosteric-receptor-receptor-interactions-regulating-5-ht1a-receptor-recognition
#1
Dasiel O Borroto-Escuela, Xiang Li, Alexander O Tarakanov, David Savelli, Manuel Narváez, Kirill Shumilov, Yuniesky Andrade-Talavera, Antonio Jimenez-Beristain, Bartosz Pomierny, Zaida Díaz-Cabiale, Riccardo Cuppini, Patrizia Ambrogini, Maria Lindskog, Kjell Fuxe
Studies on serotonin-selective reuptake inhibitors have established that disturbances in the ascending 5-HT neuron systems and their 5-HT receptor subtypes and collateral networks to the forebrain contribute to the etiology of major depression and are targets for treatment. The therapeutic action of serotonin-selective reuptake inhibitors is of proven effectiveness, but the mechanisms underlying their effect are still unclear. There are many 5-HT subtypes involved; some need to be blocked (e.g., 5-HT2A, 5-HT3, and 5-HT7), whereas others need to be activated (e...
August 31, 2017: ACS Omega
https://www.readbyqxmd.com/read/28918777/-classic-psychedelic-drugs-and-their-potential-therapeutic-effect
#2
Michael Bayat
Over the past decade we have witnessed a renewed scientific interest in the classic hallucinogens (psychedelic drugs). These are substances which exert their effects by an agonist action on the 5-HT2A receptors. The purpose of this paper is to provide a short review and discussion of the psychedelic drugs, their safety profile and their potential antidepressive, anxiolytic and antiaddictive effects. The article primarily focusses on the most recent clinical trials.
September 11, 2017: Ugeskrift for Laeger
https://www.readbyqxmd.com/read/28911960/characterization-of-the-adrenocorticotrophic-hormone-induced-mouse-model-of-resistance-to-antidepressant-drug-treatment
#3
Bettadapura N Srikumar, Mahesh Paschapur, Narasimharaju Kalidindi, Bharath Adepu, Manish L Das, Muppana V Sreedhara, Vijaya K Kuchibhotla, Rick L Pieschl, Yu-Wen Li, Durga Shiva Prasad Ega, Justin V Louis, Senthilkumar Murugesan, Pattipati S Naidu, Manjunath Ramarao, Linda J Bristow, Reeba K Vikramadithyan
Approximately 30-60% of patients treated with existing antidepressants fail to achieve remission of depressive symptoms leading to Treatment Resistant Depression (TRD). There is an urgent need to develop novel medications, which is highly limited by the non-availability of relevant animal models with good predictive validity. ACTH administration has been shown to result in the resistance to acute and chronic effects of imipramine. However, the pharmacology of the model and the mechanisms contributing to the resistance are not completely understood...
September 11, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28911007/fenfluramine-reduces-11c-cimbi-36-binding-to-the-5-ht2a-receptor-in-the-nonhuman-primate-brain
#4
Kai-Chun Yang, Vladimir Stepanov, Stefan Martinsson, Anders Ettrup, Akihiro Takano, Gitte M Knudsen, Christer Halldin, Lars Farde, Sjoerd J Finnema
Background: [11C]Cimbi-36 is a serotonin 2A receptor agonist positron emission tomography radioligand that has recently been examined in humans. The binding of agonist radioligand is expected to be more sensitive to endogenous neurotransmitter concentrations than antagonist radioligands. In the current study, we compared the effect of serotonin releaser fenfluramine on the binding of [11C]Cimbi-36, [11C]MDL 100907 (a serotonin 2A receptor antagonist radioligand), and [11C]AZ10419369 (a serotonin 1B receptor partial agonist radioligand with established serotonin sensitivity) in the monkey brain...
September 1, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28899696/serotonin-2a-receptor-disulfide-bridge-integrity-is-crucial-for-ligand-binding-to-different-signalling-states-but-not-for-its-homodimerization
#5
Alba Iglesias, Marta Cimadevila, Rocío Ailim de la Fuente, María Martí-Solano, María Isabel Cadavid, Marián Castro, Jana Selent, María Isabel Loza, José Brea
The serotonin 2A (5-HT2A) receptor is a G-protein coupled receptor (GPCR) with a conserved disulfide bridge formed by Cys(148) (transmembrane helix 3, TM3) and Cys(227) (extracellular loop 2, ECL-2). We hypothesized that disulfide bridges may determine serotonin 5-HT2A receptor functions such as receptor activation, functional selectivity and ligand recognition. We used the reducing agent dithiothreitol (DTT) to determine how the reduction of disulfide bridges affects radioligand binding, second messenger mobilization and receptor dimerization...
September 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28890736/the-psychoactive-drug-25b-nbome-recapitulates-rhabdomyolysis-in-zebrafish-larvae
#6
Genri Kawahara, Hideyuki Maeda, Ruri Kikura-Hanajiri, Ken-Ichi Yoshida, Yukiko K Hayashi
N-Benzyl-substituted 2C class phenethylamines (NBOMes) are psychoactive designer drugs, with strong hallucinogenic and stimulant effects, even at low doses. The designer drug, 2-(4-bromo-2, 5-dimethoxyphenyl)-N-(2-methoxybenzyl) ethanamine (25B-NBOMe) is considered to be one of the most potent agonists of the serotonin-2A (5-HT2A) receptor. Recently, we reported the first lethal case of 25B-NBOMe intoxication with severe rhabdomyolysis, concluded by clinical, pathological and toxicological analyses. There are currently no good animal models that closely recapitulate serotonin receptor-dependent rhabdomyolysis...
2017: Forensic Toxicology
https://www.readbyqxmd.com/read/28887162/extrinsic-nerves-are-not-involved-in-branchial-5-ht-dynamics-or-pulsatile-urea-excretion-in-gulf-toadfish-opsanus-beta
#7
Maria C Cartolano, Molly H B Amador, Velislava Tzaneva, William K Milsom, M Danielle McDonald
Gulf toadfish (Opsanus beta) can switch from continuously excreting ammonia as their primary nitrogenous waste to excreting predominantly urea in distinct pulses. Previous studies have shown that the neurotransmitter serotonin (5-HT) is involved in controlling this process, but it is unknown if 5-HT availability is under central nervous control or if the 5-HT signal originates from a peripheral source. Following up on a previous study, cranial nerves IX (glossopharyngeal) and X (vagus) were sectioned to further characterize their role in controlling pulsatile urea excretion and 5-HT release within the gill...
September 5, 2017: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
https://www.readbyqxmd.com/read/28877377/membrane-cholesterol-effect-on-the-5-ht2a-receptor-insights-into-the-lipid-induced-modulation-of-an-antipsychotic-drug-target
#8
Juan Manuel Ramírez-Anguita, Ismael Rodríguez-Espigares, Ramon Guixà-González, Agostino Bruno, Mariona Torrens-Fontanals, Alejandro Varela-Rial, Jana Selent
The serotonin 5-hydroxytryptamine 2A (5-HT2A ) receptor is a G-protein-coupled-receptor (GPCR) relevant for the treatment of CNS disorders. In this regard, neuronal membrane composition in the brain plays a crucial role in the modulation of the receptor functioning. Since cholesterol is an essential component of neuronal membranes, we have studied its effect on the 5-HT2A receptor dynamics through all-atom MD simulations. We find that the presence of cholesterol in the membrane increases receptor conformational variability in most receptor segments...
September 6, 2017: Biotechnology and Applied Biochemistry
https://www.readbyqxmd.com/read/28875958/5-hydroxytryptamine-changes-under-different-pretreatments-on-rat-models-of-myocardial-infarction-and-or-depression
#9
Mei-Yan Liu, Li-Jun Zhang, Yu-Xin Zhou, Wan-Lin Wei
Background: Psychocardiological researches have suggested a central role of 5-hydroxytryptamine (5-HT) on psychocardiological mechanism. This study aimed to further explore the central role of 5-HT and pretreatment effects of XinLingWan on rats with myocardial infarction (MI) and/or depression. Methods: Ninety Sprague-Dawley rats were randomly divided into three groups: MI group, depression group, and MI + depression group (n = 30 in each group). Each group was then divided into three subgroups (n = 10 in each subgroup): a negative control subgroup (NCS), a Western medicine subgroup (WMS), and a traditional Chinese medicine subgroup (TCMS), which were received pretreatment once a day for 4 weeks by saline, 20 mg/kg sertraline mixed with 2 ml saline, and 40 mg/kg XingLingWan mixed with 2 ml saline, respectively...
September 20, 2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28867940/genetics-of-generalized-anxiety-disorder-and-related-traits
#10
Michael G Gottschalk, Katharina Domschke
This review serves as a systematic guide to the genetics of generalized anxiety disorder (GAD) and further focuses on anxiety-relevant endophenotypes, such as pathological worry fear of uncertainty, and neuroticism. We inspect clinical genetic evidence for the familialityl heritability of GAD and cross-disorder phenotypes based on family and twin studies. Recent advances of linkage studies, genome-wide association studies, and candidate gene studies (eg, 5-HTT, 5-HT1A, MAOA, BDNF) are outlined. Functional and structural neuroimaging and neurophysiological readouts relating to peripheral stress markers and psychophysiology are further integrated, building a multilevel disease framework...
June 2017: Dialogues in Clinical Neuroscience
https://www.readbyqxmd.com/read/28858536/serotonin-and-brain-function-a-tale-of-two-receptors
#11
R L Carhart-Harris, D J Nutt
Previous attempts to identify a unified theory of brain serotonin function have largely failed to achieve consensus. In this present synthesis, we integrate previous perspectives with new and older data to create a novel bipartite model centred on the view that serotonin neurotransmission enhances two distinct adaptive responses to adversity, mediated in large part by its two most prevalent and researched brain receptors: the 5-HT1A and 5-HT2A receptors. We propose that passive coping (i.e. tolerating a source of stress) is mediated by postsynaptic 5-HT1AR signalling and characterised by stress moderation...
August 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28856700/synthesis-radiofluorination-and-preliminary-evaluation-of-the-potential-5-ht2a-receptor-agonists-18-f-cimbi-92-and-18-f-cimbi-150
#12
Fraser Graeme Edgar, Hanne D Hansen, Sebastian Leth-Petersen, Anders Ettrup, Jesper L Kristensen, Gitte M Knudsen, Matthias M Herth
An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [(11) C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, a (18) F-labelled agonist 5-HT2A receptor (5-HT2A R) tracer is highly sought after. Herein we report a two-step, one-pot labelling methodology of two tracer candidates. Both ligands display high in vitro affinities for the 5-HT2A R...
August 30, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28844001/activation-of-5-ht2a-receptors-restores-kcc2-function-and-reduces-neuropathic-pain-after-spinal-cord-injury
#13
Irene Sánchez-Brualla, Pascale Boulenguez, Cécile Brocard, Sylvie Liabeuf, Annelise Viallat-Lieutaud, Xavier Navarro, Esther Udina, Frédéric Brocard
Downregulation of the potassium chloride cotransporter type 2 (KCC2) after a spinal cord injury (SCI) disinhibits motoneurons and dorsal horn interneurons causing spasticity and neuropathic pain, respectively. We showed recently (Bos et al., 2013) that specific activation of 5-HT2A receptors by TCB-2 [(4-bromo-3,6-dimethoxybenzocyclobuten-1-yl)methylamine hydrobromide] upregulates KCC2 function, restores motoneuronal inhibition and reduces SCI-induced spasticity. Here, we tested the potential analgesic effect of TCB-2 on central (thoracic hemisection) and peripheral [spared nerve injury (SNI)] neuropathic pain...
August 30, 2017: Neuroscience
https://www.readbyqxmd.com/read/28831734/interactions-of-hallucinogens-with-the-glutamatergic-system-permissive-network-effects-mediated-through-cortical-layer-v-pyramidal-neurons
#14
Gerard J Marek
Recordings made from layer V (L5) pyramidal cells of the prefrontal cortex (PFC) and neocortex in rodent slice preparations have shown that serotonin (5-hydroxytryptamine, 5-HT) and serotonergic hallucinogens induce an increase in the frequency of spontaneous excitatory postsynaptic currents (EPSCs) in the apical dendritic field by activating 5-HT2A receptors. Serotonergic hallucinogens induce late EPSCs and increase recurrent network activity when subcortical or mid-cortical regions are stimulated at low frequencies (e...
August 23, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28828976/brexpiprazole-a-partial-dopamine-agonist-for-the-treatment-of-schizophrenia
#15
Asli Ekinci, Okan Ekinci
BACKGROUND: Schizophrenia is a chronic and debilitating mental disorder that affects the patient's and their family's life. The disease remains a complicated disorder that is challenging to treat, despite there being a large antipsychotic armamentarium. Brexpiprazole acts both as a partial agonist at the serotonin 5-HT1A and dopamine D2 receptors and as an antagonist at the serotonin 5-HT2A and noradrenaline alpha1B and alpha2C receptors, all with similar potency. This balanced receptor profile may produce promising antipsychotic effects on positive, negative and cognitive symptoms in schizophrenia with minimal adverse effects...
August 20, 2017: Reviews on Recent Clinical Trials
https://www.readbyqxmd.com/read/28821451/5-ht7-receptor-antagonism-sb-269970-attenuates-bleomycin-induced-pulmonary-fibrosis-in-rats-via-downregulating-oxidative-burden-and-inflammatory-cascades-and-ameliorating-collagen-deposition-comparison-to-terguride
#16
Mona K Tawfik, Samy Makary
The neurotransmitter 5-hydroxytryptamine (5-HT) is involved in regulation of local tissue inflammation and repair through a set of receptors (5-HT1-7 receptors), which are expressed in the lung. Considering the protective importance of 5-HT receptor antagonists against development of pulmonary fibrosis, we evaluated whether 5-HT7 receptor antagonist (SB-269970) modulates lung inflammatory and fibrogenic processes in comparison with 5-HT2A/B receptor antagonist (terguride), in bleomycin (BLM)-induced idiopathic pulmonary fibrosis (IPF) model...
August 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28817365/effect-of-flibanserin-treatment-on-body-weight-in-premenopausal-and-postmenopausal-women-with-hypoactive-sexual-desire-disorder-a-post-hoc-analysis
#17
Susan G Kornstein, James A Simon, Stuart C Apfel, James Yuan, Krista A Barbour, Robert Kissling
BACKGROUND: Flibanserin, a 5-HT1A agonist and 5-HT2A antagonist, is indicated for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. This post hoc analysis evaluated the effect of flibanserin treatment on body weight in premenopausal and postmenopausal women with HSDD. MATERIALS AND METHODS: This analysis included three 24-week, double-blind, placebo-controlled studies of flibanserin 100 mg each bedtime (qhs) in premenopausal women, a similarly designed study in postmenopausal women, and a 52-week, open-label extension study in premenopausal women...
August 17, 2017: Journal of Women's Health
https://www.readbyqxmd.com/read/28815279/evaluation-of-training-dose-in-male-sprague-dawley-rats-trained-to-discriminate-4-methylmethcathinone
#18
Michael D Berquist, Nathyn A Thompson, Lisa E Baker
RATIONALE: Although the synthetic cathinone 4-methylmethcathinone (4-MMC, mephedrone) has been a subject of intensive research investigation, the pharmacological mechanisms involved in its interoceptive stimulus effects have yet to be fully characterized. OBJECTIVE: The present study employed drug discrimination methods in rats to compare the interoceptive stimulus properties of two different training doses of 4-MMC to other substances with similar pharmacological actions...
August 16, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28806488/serotonergic-5-ht2b-receptors-in-mitral-valvulopathy-bone-marrow-mobilization-of-endothelial-progenitors
#19
Estelle Ayme-Dietrich, Roland Lawson, Francine Côté, Claudia de Tapia, Sylvia Da Silva, Claudine Ebel, Béatrice Hechler, Christian Gachet, Jérome Guyonnet, Hélène Rouillard, Jordane Stoltz, Emily Quentin, Sophie Banas, François Daubeuf, Nelly Frossard, Bernard Gasser, Jean-Philippe Mazzucotelli, Olivier Hermine, Luc Maroteaux, Laurent Monassier
BACKGROUND: Valvular heart disease is highly prevalent in industrialized countries. Chronic use of anorexigens, amphetamine or ergot derivatives targeting the serotonin system has been associated with valvular heart disease. PURPOSE AND EXPERIMENTAL APPROACH: Here, we investigated the contribution of serotonin receptors in a mouse model of valve degeneration induced by nordexfenfluramine, the main metabolite of the anorexigens dexfenfluramine and benfluorex. KEY RESULTS: Chronically activated 5-HT2B receptors by nordexfenfluramine in mice mimicked early steps of mitral valve remodelling attested by increased valve thickness, and cell density in a thick extracellular matrix...
August 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28796998/microrna-dependent-control-of-serotonin-induced-pulmonary-arterial-contraction
#20
Diana Dahan, Tran Thi Hien, Philip Tannenberg, Mari Ekman, Catarina Rippe, Thomas Boettger, Thomas Braun, Karin Tran-Lundmark, Phan-Kiet Tran, Karl Swärd, Sebastian Albinsson
BACKGROUND: Serotonin (5-HT) is considered to play a role in pulmonary arterial hypertension by regulating vascular remodeling and smooth muscle contractility. Here, arteries from mice with inducible and smooth muscle-specific deletion of Dicer were used to address mechanisms by which microRNAs control 5-HT-induced contraction. METHODS: Mice were used 5 weeks after Dicer deletion, and pulmonary artery contractility was analyzed by wire myography. RESULTS: No change was seen in right ventricular systolic pressure following dicer deletion, but systemic blood pressure was reduced...
2017: Journal of Vascular Research
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