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5-HT2A

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https://www.readbyqxmd.com/read/28735368/mdma-induced-indifference-to-negative-sounds-is-mediated-by-the-5-ht2a-receptor
#1
K P C Kuypers, R de la Torre, Farre, N Pizarro, L Xicota, J G Ramaekers
BACKGROUND: MDMA has been shown to induce feelings of sociability, a positive emotional bias and enhanced empathy. While previous research has used only visual emotional stimuli, communication entails more than that single dimension and it is known that auditory information is also crucial in this process. In addition, it is, however, unclear what the neurobiological mechanism underlying these MDMA effects on social behaviour is. Previously, studies have shown that MDMA-induced emotional excitability and positive mood are linked to the action on the serotonin (5-HT) 2A receptor...
July 22, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28733811/pharmacological-evidence-that-5-ht2c-receptor-blockade-selectively-improves-decision-making-when-rewards-are-paired-with-audiovisual-cues-in-a-rat-gambling-task
#2
Wendy K Adams, Chris Barkus, Jacqueline-Marie N Ferland, Trevor Sharp, Catharine A Winstanley
RATIONALE: Adding reward-concurrent cues to a rat gambling task (rGT) increases risky choice. This cued version of the task may reflect an "addiction-like" cognitive process, more similar to human gambling than the uncued task. Serotonergic drugs that target 5-HT2 receptors alter mechanisms linked to impulse control. However, relatively little is known regarding the impact of such agents on either risky decision making, or the ability of conditioned stimuli to bias the choice process, despite potential relevance to addiction development and treatment...
July 21, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28720478/monoamine-receptor-interaction-profiles-of-4-thio-substituted-phenethylamines-2c-t-drugs
#3
REVIEW
Dino Luethi, Daniel Trachsel, Marius C Hoener, Matthias E Liechti
BACKGROUND: 4-Thio-substituted phenethylamines (2C-T drugs) are potent psychedelics with poorly defined pharmacological properties. Because of their psychedelic effects, 2C-T drugs are sometimes sold as new psychoactive substances (NPSs). The aim of the present study was to characterize the monoamine receptor and transporter interaction profiles of a series of 2C-T drugs. METHODS: We determined the binding affinities of 2C-T drugs at monoamine receptors and transporters in human cells that were transfected with the respective receptors or transporters...
July 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28711602/contribution-of-5-ht2a-receptors-on-diaphragmatic-recovery-after-chronic-cervical-spinal-cord-injury
#4
Kun-Ze Lee, Elisa J Gonzalez-Rothi
Unilateral C2 spinal cord hemisection (C2Hx) interrupts bulbospinal respiratory pathways innervating ipsilateral phrenic motoneurons, resulting in cessation of ipsilateral diaphragm motor output. Plasticity within the spinal neural circuitry controlling the diaphragm can induce partial recovery of phrenic bursting which correlates with the time-dependent return of spinal serotonin (5-HT) immunoreactivity in the vicinity of phrenic motoneurons. The 5-HT2A receptor subtype is present on phrenic motoneurons and its expression is up-regulated after cervical spinal cord injury; however the functional role of these receptors following injury has not been clearly defined...
July 12, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28710888/chronic-spinal-cord-injury-causes-up-regulation-of-serotonin-5-ht-2a-and-2c-receptors-in-lumbosacral-cord-motoneurons
#5
Nailong Cao, Jianshu Ni, Xiaohu Wang, Hongjian Tu, Baojun Gu, Jiemin Si, Gang Wu, Karl-Erik Andersson
OBJECTIVES: To explore if the mechanism of the voiding dysfunction caused by spinal cord injury in rats can be improved by intravenous administration of the 5-HT2A/2C receptor agonist, DOI, and discuss whether it can be ascribed to serotonin 2A and 2C receptor up-regulation in lumbosacral cord motoneurons. MATERIALS AND METHODS: Female Sprague-Dawley rats were used, which were divided into two groups (Spinal cord injury group VS Normal control group). Under urethane anesthesia, cystometry was performed to examine the variation of urodynamic parameters before and after successive intrathecal administration of various doses of DOI into the lumbosacral cord...
July 15, 2017: BJU International
https://www.readbyqxmd.com/read/28706567/25i-nboh-a-new-potent-serotonin-5-ht2a-receptor-agonist-identified-in-blotter-paper-seizures-in-brazil
#6
Luciano Chaves Arantes, Ettore Ferrari Júnior, Luciano Figueiredo de Souza, Andriele Costa Cardoso, Thaynara Lino Fernandes Alcântara, Luciano Morais Lião, Yuri Machado, Rogério Araújo Lordeiro, José Coelho Neto, Ana Flávia B Andrade
A new potent serotonin 5-HT2A receptor agonist was identified in blotter papers by several state level forensic laboratories in Brazil. The 25I-NBOH is a labile molecule, which fragments into 2C-I when analyzed by routine seized material screening gas chromatography (GC) methods. GC-mass spectrometry (MS), liquid chromatography-quadrupole time-of-flight-MS, and Fourier transform infrared and nuclear magnetic resonance analyses were performed to complete molecular characterization. Individual doses range from 300 to 1000 μg...
2017: Forensic Toxicology
https://www.readbyqxmd.com/read/28701958/a-single-dose-of-lsd-does-not-alter-gene-expression-of-the-serotonin-2a-receptor-gene-htr2a-or-early-growth-response-genes-egr1-3-in-healthy-subjects
#7
Patrick C Dolder, Edna Grünblatt, Felix Müller, Stefan J Borgwardt, Matthias E Liechti
Rationale: Renewed interest has been seen in the use of lysergic acid diethylamide (LSD) in psychiatric research and practice. The repeated use of LSD leads to tolerance that is believed to result from serotonin (5-HT) 5-HT2A receptor downregulation. In rats, daily LSD administration for 4 days decreased frontal cortex 5-HT2A receptor binding. Additionally, a single dose of LSD acutely increased expression of the early growth response genes EGR1 and EGR2 in rat and mouse brains through 5-HT2A receptor stimulation...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28692863/identification-of-genetic-correlates-of-response-to-risperidone-findings-of-a-multicentric-schizophrenia-study-from-india
#8
Gurjit Kaur, Deepti Gupta, Bir Singh Chavan, Vikas Sinhmar, Rajendra Prasad, Adarsh Tripathi, P D Garg, Rajiv Gupta, Hitesh Khurana, Shiv Gautam, Mushtaq Ahmed Margoob, Jitender Aneja
Risperidone is most commonly used as an antipsychotic in India for treatment of schizophrenia. However, the response to treatment with risperidone is affected by many factors, genetic factors being one of them. So, we attempted to evaluate the association between dopamine D2 (DRD2) receptor, serotonergic (5HT2A) receptor and CYP2D6 gene polymorphisms and response to treatment with risperidone in persons with schizophrenia from North India. It was a multicentric 12-weeks prospective study, undertaken in patients diagnosed with schizophrenia according to International Classification of Diseases 10th revision, Diagnostic Criteria for Research module (ICD-10 DCR)...
July 6, 2017: Asian Journal of Psychiatry
https://www.readbyqxmd.com/read/28687907/functional-activation-of-g%C3%AE-q-coupled-to-5-ht2a-receptor-and-m1-muscarinic-acetylcholine-receptor-in-postmortem-human-cortical-membranes
#9
Yuji Odagaki, Masakazu Kinoshita, Toshio Ota, J Javier Meana, Luis F Callado, Jesús A García-Sevilla
Heterotrimeric guanine nucleotide-binding proteins (G-proteins) play a pivotal role in a wide range of signal transduction pathways, and receptor/G-protein coupling has been implicated in the pathophysiology of mental disorders. In this study, guanosine-5'-O-(3-[(35)S]thio)triphosphate ([(35)S]GTPγS) binding/immunoprecipitation assay for Gαq was applied to postmortem human brains. After its optimization for human prefrontal cortical membranes, we selected 5-hydroxytryptamine (5-HT) and carbachol as efficient agonists for subsequent experiments...
July 7, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28686543/a-physician-s-attempt-to-self-medicate-bipolar-depression-with-n-n-dimethyltryptamine-dmt
#10
Tanida Brown, Wanda Shao, Shehzad Ayub, David Chong, Christian Cornelius
N,N-dimethyltryptamine (DMT) is a psychoactive substance that has been gaining popularity in therapeutic and recreational use. This is a case of a physician who chronically took DMT augmented with phenelzine in an attempt to self-medicate refractory bipolar depression. His presentation of altered mental status, mania, and psychosis is examined in regards to his DMT use. This case discusses DMT, the possible uses of DMT, and the theorized mechanism of DMT in psychosis and treatment of depression, particularly involving its agonist activity at 5-HT1A, 5-HT2A, and 5-HT2C...
July 7, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28677096/hallucinogens-and-serotonin-5-ht2a-receptor-mediated-signaling-pathways
#11
Juan F López-Giménez, Javier González-Maeso
The neuropsychological effects of naturally occurring psychoactive chemicals have been recognized for millennia. Hallucinogens, which include naturally occurring chemicals such as mescaline and psilocybin, as well as synthetic compounds, such as lysergic acid diethylamide (LSD), induce profound alterations of human consciousness, emotion, and cognition. The discovery of the hallucinogenic effects of LSD and the observations that LSD and the endogenous ligand serotonin share chemical and pharmacological profiles led to the suggestion that biogenic amines like serotonin were involved in the psychosis of mental disorders such as schizophrenia...
July 5, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28677095/the-effects-of-hallucinogens-on-gene-expression
#12
David A Martin, Charles D Nichols
The classic serotonergic hallucinogens, or psychedelics, have the ability to profoundly alter perception and behavior. These can include visual distortions, hallucinations, detachment from reality, and mystical experiences. Some psychedelics, like LSD, are able to produce these effects with remarkably low doses of drug. Others, like psilocybin, have recently been demonstrated to have significant clinical efficacy in the treatment of depression, anxiety, and addiction that persist for at least several months after only a single therapeutic session...
July 5, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28676029/cardiovascular-concern-of-5-ht2b-receptor-and-recent-vistas-in-the-development-of-its-antagonists
#13
Komal Padhariya, Richie R Bhandare, Daniel Canney, Vinay Velingkar
The serotonin 2B receptor subtype (5-HT2BR), located in central nervous system (CNS), cardiovascular system (CVS) and the gastrointestinal tract (GIT), is an important target for the treatment of migraine, obesity and irritable bowel syndrome. 5-HT2BR is necessary for the myocardial cell proliferation and differentiation at the embroyonic stage for healthy development of heart. Recently, its involvement in drug induced valvulopathy and other myocardial disorders have paved a way for selective antagonist for the treatment of cardiac disorders...
July 3, 2017: Cardiovascular & Hematological Disorders Drug Targets
https://www.readbyqxmd.com/read/28672848/mechanism-exploration-of-arylpiperazine-derivatives-targeting-the-5-ht2a-receptor-by-in-silico-methods
#14
Feng Lin, Feng Li, Chao Wang, Jinghui Wang, Yinfeng Yang, Ling Yang, Yan Li
As a G-protein coupled receptor, the 5-hydroxytryptamine 2A (5-HT2A) receptor is known for its critical role in the cognitive, behavioural and physiological functions, and thus is a primary molecular target to treat psychiatric diseases, including especially depression. With purpose to explore the structural traits affecting the inhibitory activity, currently a dataset of 109 arylpiperazine derivatives as promising 5-HT2A antagonists was built, based on which the ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) study by using both comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) approaches was carried out...
June 26, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28671718/antinociceptive-effects-of-low-level-laser-therapy-at-3-and-8%C3%A2-j-cm-2-in-a-rat-model-of-postoperative-pain-possible-role-of-endogenous-opioids
#15
Fabio C Pereira, Julia R Parisi, Caio B Maglioni, Gabriel B Machado, Paulino Barragán-Iglesias, Josie R T Silva, Marcelo L Silva
Low-level laser therapy (LLLT) is the direct application of light to stimulate cell responses (photobiomodulation) to promote tissue healing, reduce inflammation, and induce analgesia; the molecular basis for these effects of LLLT remains unclear. The objective of this study was to evaluate the analgesic effect of LLLT in the rat plantar incision model of postoperative pain as well as to investigate some of the possible mechanisms involved in this effect. Wistar rats were submitted to plantar incision and treated with LLLT (830 nm, continuous-mode, 30 mW/cm(2) , 1-12 J/cm(2) )...
July 3, 2017: Lasers in Surgery and Medicine
https://www.readbyqxmd.com/read/28668504/mirtazapine-attenuates-the-expression-of-nicotine-induced-locomotor-sensitization-in-rats
#16
Susana Barbosa-Méndez, Noé Jurado, Maura Matus-Ortega, Silvia Martiñón-Gutiérrez, Gerardo Heinze, Alberto Salazar-Juárez
Nicotine is the primary psychoactive component of tobacco. Many addictive nicotinic actions are mediated by an increase in the activity of the serotonin (5-HT) system. Some studies show that the 5-HT2A, 5-HT2C, and 5-HT3 receptors have a central role in the induction and expression of nicotine-induced locomotor sensitization. Mirtazapine, an antagonist of the α2-adrenergic receptors, the 5-HT2A/C, and the 5-HT3 receptors, has proven effective in reducing behavioral effects induced by drugs like cocaine and methamphetamines in human and animal...
June 28, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28659464/impact-of-glutamatergic-and-serotonergic-neurotransmission-on-diaphragm-muscle-activity-after-cervical-spinal-hemisection
#17
Carlos B Mantilla, Heather M Gransee, Wen-Zhi Zhan, Gary C Sieck
Incomplete cervical spinal cord hemisection at C2 (SH) disrupts descending excitatory drive to phrenic motoneurons, paralyzing the ipsilateral diaphragm muscle. Spontaneous recovery over time is associated with increased phrenic motoneuron expression of glutamatergic N-methyl-D-aspartate (NMDA) and serotonergic 5-HT2A receptors. We hypothesized that NMDA and 5-HT2A receptor-mediated neurotransmission play a role in ipsilateral diaphragm muscle activity post-SH. Adult male Sprague-Dawley rats were implanted with bilateral diaphragm EMG electrodes for chronic EMG recordings up to 28 days post-SH (SH 28D)...
June 28, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28645584/effects-of-intranasal-treatment-with-slow-gyy4137-and-rapid-nahs-donors-of-hydrogen-sulfide-in-lipopolysaccharide-induced-airway-inflammation-in-mice
#18
Yesim Kaya-Yasar, Yasemin Karaman, Turgut Emrah Bozkurt, Sevgen Celik Onder, Inci Sahin-Erdemli
We have investigated the effects of slow (GYY4137) and rapid (NaHS) hydrogen sulfide (H2S) releasing donors in lipopolysaccharide (LPS)-induced airway inflammation in mice. LPS (0.1 mg/ml) in 60 μl PBS was administered by the intranasal (i.n.) route and control group received vehicle, whereas the subgroups of mice were treated with i.n. GYY4137 or NaHS. The tracheal reactivity, inflammatory cell count in bronchoalveolar lavage (BAL) fluid and lung histopathology were evaluated in all groups 48 h after LPS/PBS applications...
June 20, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28639321/association-of-the-5-ht2a-receptor-gene-promoter-polymorphism-1438g-a-with-anorexia-nervosa-and-psychopathological-traits-in-the-chinese-han-population-a-preliminary-study
#19
Qing Kang, Jue Chen, Shunying Yu, Aihua Yuan, Yanxia Zhang, Ran Zhang, Wenhui Jiang, Chen Zhang, Haiyin Zhang, Mingdao Zhang, Zeping Xiao
OBJECTIVE: The aim of the study was to explore the possible role of the 5-HT2A -1438G/A polymorphism in the susceptibility to anorexia nervosa (AN) in the Chinese Han population. METHODS: The -1438G/A polymorphism of 249 female AN patients, 228 matched healthy controls, and 198 trios was genotyped using SNaP shot assay. Psychopathological traits of eating-disordered behaviors in AN subjects were examined using the Chinese version of the Eating Disorder Examination Questionnaire...
June 22, 2017: Asia-Pacific Psychiatry: Official Journal of the Pacific Rim College of Psychiatrists
https://www.readbyqxmd.com/read/28637246/effect-of-psilocybin-on-empathy-and-moral-decision-making
#20
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
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