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https://www.readbyqxmd.com/read/29324345/synthesis-and-biological-evaluation-of-a-series-of-multi-target-n-substituted-cyclic-imide-derivatives-with-potential-antipsychotic-effect
#1
Mingshuo Xu, Yu Wang, Feipu Yang, Chunhui Wu, Zhen Wang, Bin Ye, Xiangrui Jiang, Qingjie Zhao, Jianfeng Li, Yongjian Liu, Junchi Zhang, Guanghui Tian, Yang He, Jingshan Shen, Hualiang Jiang
In the present study, a series of multi-target N-substituted cyclic imide derivatives which possessed potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties were synthesized and evaluated as potential antipsychotics. Among these compounds, (3aR,4R,7S,7aS)-2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione hydrochloride (3d) held a promising pharmacological profile. 3d not only showed potent and balanced in vitro activities on D2/5-HT1A/5-HT2A receptors, but also endowed with low to moderate activities on 5-HT2C, H1, α1A, M3 receptors and hERG channel, suggesting a low liability to induce side effects such as weight gain, orthostatic hypotension and QT prolongation...
January 4, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29305656/serotonergic-targets-for-the-treatment-of-l-dopa-induced-dyskinesia
#2
REVIEW
Kathryn Lanza, Christopher Bishop
Dopamine (DA) replacement therapy with L-3,4-dihydroxyphenylalanine (L-DOPA) continues to be the gold-standard treatment for Parkinson's disease (PD). Despite clear symptomatic benefit, long-term L-DOPA use often results in the development of L-DOPA-induced dyskinesia (LID), significantly reducing quality of life and increasing costs for PD patients and their caregivers. Accumulated research has demonstrated that several pre- and post-synaptic mechanisms contribute to LID development and expression. In particular, raphe-striatal hyperinnervation and unregulated DA release from 5-HT terminals is postulated to play a central role in LID manifestation...
January 5, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29302713/psilocybin-disrupts-sensory-and-higher-order-cognitive-processing-but-not-pre-attentive-cognitive-processing-study-on-p300-and-mismatch-negativity-in-healthy-volunteers
#3
Anna Bravermanová, Michaela Viktorinová, Filip Tylš, Tomáš Novák, Renáta Androvičová, Jakub Korčák, Jiří Horáček, Marie Balíková, Inga Griškova-Bulanova, Dominika Danielová, Přemysl Vlček, Pavel Mohr, Martin Brunovský, Vlastimil Koudelka, Tomáš Páleníček
RATIONALE: Disruption of auditory event-related evoked potentials (ERPs) P300 and mismatch negativity (MMN), electrophysiological markers of attentive and pre-attentive cognitive processing, is repeatedly described in psychosis and schizophrenia. Similar findings were observed in a glutamatergic model of psychosis, but the role of serotonergic 5-HT2A receptors in information processing is less clear. OBJECTIVES: We studied ERPs in a serotonergic model of psychosis, induced by psilocybin, a psychedelic with 5-HT2A/C agonistic properties, in healthy volunteers...
January 5, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29291430/the-potential-benefit-of-combined-versus-monotherapy-of-coenzyme-q10-and-fluoxetine-on-depressive-like-behaviors-and-intermediates-coupled-to-gsk-3%C3%AE-in-rats
#4
Sally A Abuelezz, Nevien Hendawy, Yosra Magdy
As a part of the serotoninergic dysfunction implicated in neurobiology of depression, evidence has focused on serotonin (5-HT) receptors downstream signaling intermediates including glycogen synthase kinase-3β (GSK-3β), cAMP response element binding protein (CREB) and brain derived neurotrophic factor (BDNF). Our team previously reported that coenzyme Q10 (CoQ10) exerted antidepressant-like effect in rats exposed to chronic unpredictable mid stress (CUMS) via elevating serotonin levels. However, the effect of CoQ10 has not been elucidated in downstream signaling molecules mediating 5HT receptors' effect involved in depressive disorder hitherto...
December 29, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29281590/quantification-of-5-ht1a-and-5-ht2a-receptor-binding-in-depressed-suicide-attempters-and-non-attempters
#5
J John Mann, Allison V Metts, R Todd Ogden, Chester A Mathis, Harry Rubin-Falcone, Zhiqun Gong, Wayne C Drevets, Jamie Zelazny, David A Brent
No abstract text is available yet for this article.
December 27, 2017: Archives of Suicide Research: Official Journal of the International Academy for Suicide Research
https://www.readbyqxmd.com/read/29277716/further-investigation-of-the-effects-of-5-hydroxytryptamine-8-oh-dpat-and-doi-to-mediate-contraction-and-relaxation-responses-in-the-intestine-and-emesis-in-suncus-murinus
#6
Farideh A Javid, Saeed Afshin-Javid, Charles C Horn
5-HT receptors are implicated in many gastrointestinal disorders. However, the precise role of 5-HT in mediating GI responses in Suncus murnius is still unclear. Therefore in this study, the effects of 5-HT and its agonists were investigated in Suncus. The involvement of 5-HT2C receptors in mediating emesis was also investigated. The ability of 5-HT and its agonists/antagonists at 5-HT1A and 5-HT2 to modify GI motility was investigated in vitro and in vivo. WAY100635 (a 5-HT1A antagonist) inhibited the contraction response to 5-HT in the proximal segments without affecting the maximum response; whilst enhancing the contraction to 5-HT (>30...
December 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29273459/mirtazapine-impairs-acquisition-and-reinstatement-of-cocaine-induced-place-preference-in-rats
#7
Susana Barbosa-Méndez, Maura Matus-Ortega, Salomón Jacinto-Gutiérrez, Alberto Salazar-Juárez
Exposure to cues previously associated with drug use and the environment can trigger intense craving and drug-seeking, often leading to relapse in individuals with substance use disorders. Several studies suggest that the decrease in the effects of the cues and the environment could help maintain abstinence from drug use in individuals abusing drugs. Mirtazapine, an antagonist of the noradrenergic (NE) α2 receptor and the 5-HT2A/C and 5-HT3 receptors has demonstrated efficacy in reducing the rewarding effect of different drugs...
December 19, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29273456/the-antipsychotic-trifluoperazine-reduces-marble-burying-behavior-in-mice-via-d2-and-5-ht2a-receptors-implications-for-obsessive-compulsive-disorder
#8
Nobuaki Egashira, Naoki Kubota, Yu Goto, Takuya Watanabe, Kaori Kubota, Shutaro Katsurabayashi, Katsunori Iwasaki
Trifluoperazine, a typical antipsychotic drug, not only antagonizes dopamine D2 receptors but also enhances serotonin 5-HT2 receptor-mediated behavior. Moreover, trifluoperazine suppresses human purinergic receptor P2X7 responses and calmodulin. However, the effect of trifluoperazine on marble-burying behavior, which has been considered an animal model of obsessive-compulsive disorder (OCD), has not been studied. Here, we examined the effect of trifluoperazine on marble-burying behavior in mice. Oral administration of paroxetine, a selective serotonin reuptake inhibitor, significantly reduced marble-burying behavior without affecting total locomotor activity...
December 19, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29225192/effects-of-the-new-psychoactive-substances-diclofensine-diphenidine-and-methoxphenidine-on-monoaminergic-systems
#9
Dino Luethi, Marius C Hoener, Matthias E Liechti
Diclofensine, diphenidine, and methoxphenidine are new psychoactive substances (NPSs) that recently appeared on the illicit drug market. Pharmacological profiling of such newly emerged drugs is crucial for a better understanding of their psychotropic effects and toxicity. We therefore investigated the potential of these NPSs to inhibit the norepinephrine, dopamine, and serotonin transporters in human embryonic kidney cells stably transfected with the respective transporters. In addition, we determined monoamine transporter and receptor affinities for the substances...
December 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29224968/adjunctive-treatment-with-brexpiprazole-and-escitalopram-reduces-behavioral-stress-responses-and-increase-hypothalamic-npy-immunoreactivity-in-a-rat-model-of-ptsd-like-symptoms
#10
Hagit Cohen, Joseph Zohar, Zeev Kaplan, Jørn Arnt
The study explored effects of brexpiprazole (partial D2/5-HT1A agonist, 5-HT2A and α1B/2C-adrenoceptor antagonist) in rats exposed to predator scent stress (PSS), a proposed model of PTSD-like phenotype. Brexpiprazole (3.0mg/kg, PO), escitalopram (5.0mg/kg, IP) and their combination were administered twice daily for 14 days, starting 14 days after exposure to PSS or sham-PSS, shortly after a situational stress reminder. One day after last treatment behavioral responsivity was assessed. Brexpiprazole+escitalopram-treated rats spent more time in open arms, entered open arms more often and exhibited a lower anxiety index in the elevated plus maze than vehicle-treated, PSS-exposed rats...
January 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29221792/the-serotonin-hallucinogen-5-meo-dmt-alters-cortico-thalamic-activity-in-freely-moving-mice-regionally-selective-involvement-of-5-ht1a-and-5-ht2a-receptors
#11
REVIEW
Maurizio S Riga, Laia Lladó-Pelfort, Francesc Artigas, Pau Celada
5-MeO-DMT is a natural hallucinogen acting as serotonin 5-HT1A/5-HT2A receptor agonist. Its ability to evoke hallucinations could be used to study the neurobiology of psychotic symptoms and to identify new treatment targets. Moreover, recent studies revealed the therapeutic potential of serotonin hallucinogens in treating mood and anxiety disorders. Our previous results in anesthetized animals show that 5-MeO-DMT alters cortical activity via 5-HT1A and 5-HT2A receptors. Here, we examined 5-MeO-DMT effects on oscillatory activity in prefrontal (PFC) and visual (V1) cortices, and in mediodorsal thalamus (MD) of freely-moving wild-type (WT) and 5-HT2A-R knockout (KO2A) mice...
December 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29220382/anatomical-relationships-between-serotonin-5-ht2a-and-dopamine-d2-receptors-in-living-human-brain
#12
Tatsuya Ishii, Yasuyuki Kimura, Masanori Ichise, Keisuke Takahata, Soichiro Kitamura, Sho Moriguchi, Manabu Kubota, Ming-Rong Zhang, Makiko Yamada, Makoto Higuchi, Yoshinori Okubo, Tetsuya Suhara
METHODS: Seven healthy volunteers underwent PET scans with [18F]altanserin and [11C]FLB 457 for 5-HT2A and D2 receptors, respectively. As a measure of receptor density, a binding potential (BP) was calculated from PET data for 76 cerebral cortical regions. A correlation matrix was calculated between the binding potentials of [18F]altanserin and [11C]FLB 457 for those regions. The regional relationships were investigated using a bicluster analysis of the correlation matrix with an iterative signature algorithm...
2017: PloS One
https://www.readbyqxmd.com/read/29217539/inhibition-of-cocaine-and-3-4-methylenedioxypyrovalerone-mdpv-self-administration-by-lorcaserin-is-mediated-by-5-ht2c-receptors-in-rats
#13
Brenda M Gannon, Agnieszka Sulima, Kenner C Rice, Gregory T Collins
Lorcaserin is a serotonin (5-HT)2C receptor-preferring agonist approved by the US Food and Drug Administration to treat obesity. Lorcaserin has been shown to decrease cocaine self-administration in rats and monkeys. Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB 242084), lorcaserin also has effects at 5-HT2A and 5-HT1A receptors and the relative contribution of these receptors to its anti-cocaine effects has not been investigated. The goals of this study were to determine: (1) the potency and effectiveness of lorcaserin to decrease self-administration of cocaine and 3,4-methylenedioxypyrovalerone (MDPV), a common "bath salts" constituent; and (2) the receptor(s) mediating the effects of lorcaserin on cocaine and MDPV self-administration...
December 7, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29215308/the-importance-of-small-polar-radiometabolites-in-molecular-neuroimaging-a-pet-study-with-11c-cimbi-36-labeled-in-two-positions
#14
Annette Johansen, Hanne D Hansen, Claus Svarer, Szabolcs Lehel, Sebastian Leth-Petersen, Jesper L Kristensen, Nic Gillings, Gitte M Knudsen
[11C]Cimbi-36, a 5-HT2A receptor agonist PET radioligand, contains three methoxy groups amenable to [11C]-labeling. In pigs, [11C]Cimbi-36 yields a polar (M1) and a less polar (M2) radiometabolite fraction, while changing the labeling to [11C]Cimbi-36_5 yields only the M1 fraction. We investigate whether changing the labeling position of [11C]Cimbi-36 eliminates M2 in humans, and if this changes the signal-to-background ratio. Six healthy volunteers each underwent two dynamic PET scans; after injection of [11C]Cimbi-36, both the M1 and M2 fraction appeared in plasma, whereas only the M1 appeared after [11C]Cimbi-36_5 injection...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/29210063/opioid-induced-inhibition-of-the-human-serotonin-and-norepinephrine-transporters-in-vitro-link-to-clinical-reports-of-serotonin-syndrome
#15
Anna Rickli, Evangelia Liakoni, Marius C Hoener, Matthias E Liechti
BACKGROUND AND PURPOSE: Opioids may inhibit the serotonin and norepinephrine transporters (SERT and NET, respectively). NET inhibition may contribute to analgesia, and SERT inhibition or interactions with serotonin receptors may cause serotonergic toxicity. However, the effects of different opioids on the human SERT, NET, and serotonin receptors have not been sufficiently studied. EXPERIMENTAL APPROACH: We determined the potencies of different opioids to inhibit the SERT and NET in vitro using human transporter-transfected cells...
December 6, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29198512/understanding-the-role-of-serotonin-in-female-hypoactive-sexual-desire-disorder-and-treatment-options
#16
REVIEW
Harry A Croft
BACKGROUND: The neurobiology of sexual response is driven in part by dopamine and serotonin-the former modulating excitatory pathways and the latter regulating inhibitory pathways. Neurobiological underpinnings of hypoactive sexual desire disorder (HSDD) are seemingly related to overactive serotonin activity that results in underactive dopamine activity. As such, pharmacologic agents that decrease serotonin, increase dopamine, or some combination thereof, have therapeutic potential for HSDD...
December 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29198449/effects-of-flibanserin-on-the-pharmacokinetics-of-a-combined-ethinylestradiol-levonorgestrel-oral-contraceptive-in-healthy-premenopausal-women-a-randomized-crossover-study
#17
Crista Johnson-Agbakwu, Louise Brown, James Yuan, Robert Kissling, David J Greenblatt
PURPOSE: This study aimed to investigate the effect of steady-state exposure to flibanserin, a 5-HT1A agonist/5-HT2A antagonist approved for the treatment of hypoactive sexual desire disorder in premenopausal women, on the single-dose pharmacokinetics of the contraceptive steroids ethinylestradiol and levonorgestrel in healthy premenopausal women. METHODS: Healthy female volunteers (N = 24) received 2 single doses of a combined oral contraceptive containing ethinylestradiol 30 μg and levonorgestrel 150 μg, either alone (reference) or preceded by treatment with flibanserin 100 mg once daily for 14 days (test)...
November 30, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/29185542/pimavanserin-a-novel-therapeutic-option-for-parkinson-disease-psychosis
#18
REVIEW
Trevor Hawkins, Brian D Berman
Purpose of review: In April 2016, the Food and Drug Administration (FDA) approved a first-in-class atypical antipsychotic medication called pimavanserin for the treatment of Parkinson disease psychosis (PDP). We aim to inform readers about its indications, effectiveness, and safety profile. Recent findings: Pimavanserin acts as an inverse agonist at serotonin 5-HT2A receptors and has negligible effects on other receptors, thereby avoiding the D2 receptor antagonism that can potentially worsen motor symptoms...
April 2017: Neurology. Clinical Practice
https://www.readbyqxmd.com/read/29167644/lsd-increases-primary-process-thinking-via-serotonin-2a-receptor-activation
#19
Rainer Kraehenmann, Dan Pokorny, Helena Aicher, Katrin H Preller, Thomas Pokorny, Oliver G Bosch, Erich Seifritz, Franz X Vollenweider
Rationale: Stimulation of serotonin 2A (5-HT2A) receptors by lysergic acid diethylamide (LSD) and related compounds such as psilocybin has previously been shown to increase primary process thinking - an ontologically and evolutionary early, implicit, associative, and automatic mode of thinking which is typically occurring during altered states of consciousness such as dreaming. However, it is still largely unknown whether LSD induces primary process thinking under placebo-controlled, standardized experimental conditions and whether these effects are related to subjective experience and 5-HT2A receptor activation...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29162966/a-qsar-model-of-olanzapine-derivatives-as-potential-inhibitors-for-5-ht2a-receptor
#20
Pooja Mitra, Aishwarya Rastogi, Mayank Rajpoot, Ajay Kumar, Vivek Srivastava
Schizophrenia is a complex, chronic mental disorder, affecting about 21 million people worldwide. It is characterized by symptoms, including distortions in thinking, perception, emotions, disorganized speech, sense of self and behavior. Recently, a numbers of marketed drugs for Schizophrenia are available against dopamine D2 and serotonin 5-HT2A receptors. Here, we docked Olanzapine derivatives (collected from literature) with 5-HT2A Receptor using the program AutoDock 4.2. The docked protein inhibitor complex structure was optimized using molecular dynamics simulation for 5ps with the CHARMM-22 force field using NAMD (NAnoscale Molecular Dynamics program) incorporated in visual molecular dynamics (VMD 1...
2017: Bioinformation
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