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https://www.readbyqxmd.com/read/29154107/aripiprazole-in-treatment-of-gilles-de-la-tourette-syndrome-new-therapeutic-option
#1
REVIEW
Piotr Janik, Natalia Szejko
Aripiprazole is a dopamine D2- and serotonin 5-hydroxytryptamine (5-HT)1A receptor partial agonist and 5-HT2A receptor antagonist primarily used for the treatment of schizophrenia, bipolar disorder or depression with psychotic ideation. However, recently a number of new possible indications have been suggested, among them Gilles de la Tourette syndrome (GTS). In two randomized, double-blind, placebo-controlled studies in children and adolescents with GTS has been confirmed the efficacy of aripiprazole in tic reduction...
November 9, 2017: Neurologia i Neurochirurgia Polska
https://www.readbyqxmd.com/read/29145495/regulatory-mechanism-of-ccn2-production-by-serotonin-5-ht-via-5-ht2a-and-5-ht2b-receptors-in-chondrocytes
#2
Ayaka Hori, Takashi Nishida, Shogo Takashiba, Satoshi Kubota, Masaharu Takigawa
Serotonin (5-hydroxytryptamine: 5-HT) is recognized as a neurotransmitter in the central nerve system and as a regulator of systemic blood pressure in the peripheral tissues. Recently, it was reported that 5-HT2 receptors (5-HT2Rs) were expressed in cartilage tissues lacking both vessels and neurons, suggesting possible novel functions of 5-HT during cartilage development and regeneration. Our previous data indicated that CCN family protein 2/connective tissue growth factor (CCN2/CTGF) plays a central role in cartilage development and regeneration...
2017: PloS One
https://www.readbyqxmd.com/read/29135714/ritanserin-a-serotonin-2-receptor-antagonist-inhibits-functional-recovery-after-cerebral-infarction
#3
Kenmei Mizutani, Shigeru Sonoda, Hideaki Wakita
It has been suggested that serotonin (5-HT) may be implicated in functional recovery after stroke; however, the underlying molecular mechanisms remain unknown. Here, the role of 5-HT was verified using ritanserin, a potent 5-HT2A receptor antagonist, and protein expression and modification were analyzed to further understand the association between paralysis recovery and molecular mechanisms in the brain. Experimental cerebral cortex infarctions were induced by photothrombosis in rats. Voluntary exercise was initiated 2 days after surgery...
November 10, 2017: Neuroreport
https://www.readbyqxmd.com/read/29128144/the-antipsychotic-drug-brexpiprazole-reverses-phencyclidine-induced-disruptions-of-thalamocortical-networks
#4
Hanna E van den Munkhof, Jørn Arnt, Pau Celada, Francesc Artigas
Brexpiprazole (BREX), a recently approved antipsychotic drug in the US and Canada, improves cognitive dysfunction in animal models, by still largely unknown mechanisms. BREX is a partial agonist at 5-HT1A and D2 receptors and antagonist at α1B- and α2C-adrenergic and 5-HT2A receptors all with a similar potency. The NMDA receptor antagonist phencyclidine (PCP), used as pharmacological model of schizophrenia, activates thalamocortical networks and decreases low frequency oscillations (LFO; <4 Hz). These effects are reversed by antipsychotics...
November 8, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29120849/genetic-analysis-of-impulsive-personality-traits-examination-of-a-priori-candidates-and-genome-wide-variation
#5
Joshua C Gray, James MacKillop, Jessica Weafer, Kyle M Hernandez, Jianjun Gao, Abraham A Palmer, Harriet de Wit
Impulsive personality traits are heritable risk factors and putative endophenotypes for addiction and other psychiatric disorders involving disinhibition. This study examined the genetic basis of impulsive personality traits, defined as scores on the Barratt Impulsiveness Scale (BIS-11) and the UPPS-P Impulsive Behavior Scale (UPPS-P). In 983 healthy young adults of European ancestry, the study examined genetic variation in relation to a combined phenotype of seven subscales based on high phenotypic intercorrelations...
November 8, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/29111677/novel-bivalent-5-ht2a-receptor-antagonists-exhibit-high-affinity-and-potency-in-vitro-and-efficacy-in-vivo
#6
Claudia A Soto, Matthew J Shashack, Robert G Fox, Marcy J Bubar, Kenner C Rice, Cheryl S Watson, Kathryn A Cunningham, Scott R Gilbertson, Noelle C Anastasio
The 5-HT2A receptor (5-HT2AR) plays an important role in various neuropsychiatric disorders, including substance use disorder and schizophrenia. Homodimerization of this receptor has been suggested, but tools that allow direct assessment of the relevance of the 5-HT2AR:5-HT2AR homodimer in these disorders are necessary. We chemically modified the selective 5-HT2AR antagonist M100907 to synthesize a series of homobivalent ligands connected by ethylene glycol linkers of varying lengths that may be useful tools for probing 5-HT2AR:5-HT2AR homodimer function...
November 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29111111/anti-aggregation-effect-of-aroxyalkyl-derivatives-of-2-methoxyphenylpiperazine-is-due-to-their-5-ht2a-and-%C3%AE-2-adrenoceptor-antagonistic-properties-a-comparison-with-ketanserin-sarpogrelate-prazosin-yohimbine-and-arc239
#7
Monika Kubacka, Grzegorz Kazek, Magdalena Kotańska, Barbara Filipek, Anna Maria Waszkielewicz, Szczepan Mogilski
Serotonin (5-HT) and adrenaline acting at platelet 5-HT2A-serotoninergic and α2-adrenergic receptors are involved in platelet aggregation. We have evaluated the antagonistic potency at 5-HT2A, α2A-, and α2B-adrenoceptors as well as an anti-aggregation effect of aroxyalkyl derivatives of 2-methoxyphenylpiperazine and compared them with ketanserin, sarpogrelate, prazosin, yohimbine and ARC239 (2-[2-[4-(o-methoxyphenyl)-piperazin-1-yl]-ethyl]-4,4-dimethyl-1,3-(2H,4H)-isoquinolindione). Functional bioassays at cells expressing human receptors, revealed studied compounds to be moderate antagonists of 5-HT2A and α2-adrenoceptors, with around 2-7 times stronger antagonistic effect at α2B subtype than α2A subtype...
October 27, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29106549/the-in-vitro-actions-of-loxapine-on-dopaminergic-and-serotonergic-receptors-time-to-consider-atypical-classification-of-this-antipsychotic-drug
#8
Florian Ferreri, Dominique Drapier, Emmanuelle Baloche, Mehemed Ouzid, Luc Zimmer, Pierre-Michel Llorca
Background: The denomination of typical antipsychotic for loxapine has poor relation to current knowledge of the molecule's relevant modes of action. Method: Competition binding experiments were performed on expressed human recombinant receptors in CHO cells and HEK-293 cells for D1 to D5, 5-HT1A, 5-HT2A, 5-HT2C, 5-HT4, 5-HT6, and 5-HT7. In vitro autoradiographies using [ 11C]-Raclopride [18F]-Altanserin [18F]-MPPF [11C]-SB207145 and [18F]-2FNQ1P were measured in brain tissue of a male primate followed by addition of increasing doses of loxapine succinate...
November 2, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29104045/5-ht2a-receptor-is-the-predominant-receptor-mediating-contraction-of-the-isolated-porcine-distal-ureter-to-5-ht-in-young-and-old-animals
#9
Iris Lim, Russ Chess-Williams, Donna Sellers
Isolated ureteral strips develop spontaneous phasic contractile activity which is enhanced by 5-hydroytryptamine (5-HT). The aim of this study was to identify the receptor subtype mediating these responses and to determine whether responses to 5-HT change with age. The frequency of contractions and the overall contractile activity (measured as the area under the curve, AUC) were recorded in strips of porcine distal ureter isolated from young (3 months) and old (2 years) pigs. Responses to 5-HT were examined in the absence and presence of selective 5-HT receptor subtype antagonists...
November 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29098976/pimavanserin-for-the-treatment-of-parkinson-s-disease-psychosis-number-needed-to-treat-number-needed-to-harm-and-likelihood-to-be-helped-or-harmed
#10
Leslie Citrome, James C Norton, Kathy Chi-Burris, George Demos
OBJECTIVE: Our aim was to describe the efficacy and tolerability of pimavanserin, a highly selective serotonin 5-HT2A receptor inverse agonist/antagonist indicated for the treatment of hallucinations and delusions associated with Parkinson's disease psychosis (PDP), using the metrics of number needed to treat (NNT) and number needed to harm (NNH). METHODS: Categorical efficacy and tolerability data were extracted from the clinical trial databases of the double-blind placebo-controlled studies of pimavanserin in persons with PDP...
November 3, 2017: CNS Spectrums
https://www.readbyqxmd.com/read/29057276/genetic-correlates-of-spirituality-religion-and-depression-a-study-in-offspring-and-grandchildren-at-high-and-low-familial-risk-for-depression
#11
Micheline R Anderson, Lisa Miller, Priya Wickramaratne, Connie Svob, Zagaa Odgerel, Ruixin Zhao, Myrna M Weissman
RATIONALE: Possible genetic correlates of spirituality and depression have been identified in community samples. We investigate some of the previously identified candidates in a sample of families at both high and low-risk for depression. METHOD: Offspring and grandchildren of individuals at high and low-risk for depression, participating in a multi-wave thirty-year longitudinal study, were assessed for seven SNPS drawn from four single gene candidates associated with systems implicated in both depression and spirituality: Serotonin (5-HT1B and 5-HT2A), Dopamine (DRD2), Oxytocin (OT) and Monoamine Vesicular Transporter (VMAT1)...
March 2017: Spirituality in Clinical Practice
https://www.readbyqxmd.com/read/29047301/pimavanserin-novel-pharmacotherapy-for-parkinson-s-disease-psychosis
#12
Zeyad T Sahli, Frank I Tarazi
Pimavanserin is the first FDA-approved atypical antipsychotic drug indicated for the treatment of hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Areas covered: This review focuses on the preclinical discovery of pimavanserin. It analyzes the pharmacological, behavioral and molecular mechanisms of pimavanserin and their contribution to the therapeutic advantages of the drug as reported in published preclinical and clinical studies, and product labels. Expert opinion: Pimavanserin exhibits a unique pharmacological profile with nanomolar affinity at serotonin 5-HT2A and 5-HT2C receptors...
October 19, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29037912/early-emergence-of-altered-5-ht2a-receptor-evoked-behavior-neural-activation-and-gene-expression-following-maternal-separation
#13
Ankit Sood, Sthitapranjya Pati, Amrita Bhattacharya, Karina Chaudhari, Vidita A Vaidya
The early stress of Maternal Separation (MS) contributes to the establishment of adult psychopathology. The serotonergic (5-HT) system is implicated during this temporal window in mediating the development of mood-related behaviors. MS is reported to evoke altered 5-HT2A receptor function in adulthood. However, the ontogeny of altered 5-HT2A receptor responsivity following MS remains unknown. Here, we examined 5-HT2A receptor agonist, DOI (1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane) (2mg/kg) evoked responses, namely stereotypical head-twitch behaviors in control and MS Sprague-Dawley rat pups at postnatal day 21 (P21)...
October 14, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/29033796/laminar-and-cellular-distribution-of-monoamine-receptors-in-rat-medial-prefrontal-cortex
#14
REVIEW
Noemí Santana, Francesc Artigas
The prefrontal cortex (PFC) is deeply involved in higher brain functions, many of which are altered in psychiatric conditions. The PFC exerts a top-down control of most cortical and subcortical areas through descending pathways and is densely innervated by axons emerging from the brainstem monoamine cell groups, namely, the dorsal and median raphe nuclei (DR and MnR, respectively), the ventral tegmental area and the locus coeruleus (LC). In turn, the activity of these cell groups is tightly controlled by afferent pathways arising from layer V PFC pyramidal neurons...
2017: Frontiers in Neuroanatomy
https://www.readbyqxmd.com/read/29021191/enhancement-of-phrenic-long-term-facilitation-following-repetitive-acute-intermittent-hypoxia-is-blocked-by-the-glycolytic-inhibitor-2-deoxyglucose
#15
Peter M MacFarlane, Stephane Vinit, Gordon S Mitchell
Moderate acute intermittent hypoxia (mAIH) elicits a form of respiratory motor plasticity known as phrenic long-term facilitation (pLTF). Preconditioning with modest protocols of chronic intermittent hypoxia enhances pLTF, demonstrating pLTF metaplasticity. Since "low dose" protocols of repetitive acute intermittent hypoxia show promise as a therapeutic modality to restore respiratory (and non-respiratory) motor function in clinical disorders with compromised breathing, we tested the hypothesis that preconditioning with a mild repetitive AIH (rAIH) protocol enhances pLTF and hypoglossal (XII) LTF, and whether the enhancement is regulated by glycolytic flux...
October 11, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/29018305/unraveling-complexity-in-the-solid-form-screening-of-a-pharmaceutical-salt-why-so-many-forms-why-so-few
#16
Doris E Braun, Sreenivas R Lingireddy, Mark D Beidelschies, Rui Guo, Peter Müller, Sarah L Price, Susan M Reutzel-Edens
The solid form landscape of 5-HT2a antagonist 3-(4-(benzo[d]isoxazole-3-yl)piperazin-1-yl)-2,2-dimethylpropanoic acid hydrochloride (B5HCl) proved difficult to establish. Many crystalline materials were produced by solid form screening, but few forms readily grew high quality crystals to afford a clear picture or understanding of the solid form landscape. Careful control of crystallization conditions, a range of experimental methods, computational modeling of solvate structures, and crystal structure prediction were required to see potential arrangements of the salt in its crystal forms...
October 4, 2017: Crystal Growth & Design
https://www.readbyqxmd.com/read/29017334/brexpiprazole-a-new-leaf-on-the-partial-dopamine-agonist-branch
#17
Judy Hope, David Castle, Nicholas A Keks
OBJECTIVES: Brexpiprazole is a new dopamine partial agonist antipsychotic in the same class as aripiprazole. This paper will briefly review brexpiprazole and compare it with aripiprazole. CONCLUSIONS: Brexpiprazole and aripiprazole are both partial agonists at dopamine D2, and serotonin 5-HT1A and antagonists at serotonin 5-HT2A and noradrenergic α1B receptors. However, the two drugs are significantly different in potencies at various receptors; neurochemical profiles predict that brexpiprazole may be comparable with aripiprazole in its antipsychotic efficacy but may cause less akathisia, extrapyramidal side effects (EPS) and activation...
October 1, 2017: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
https://www.readbyqxmd.com/read/28987938/tcb-2-7r-3-bromo-2-5-dimethoxy-bicyclo-4-2-0-octa-1-3-5-trien-7-yl-methanamine-a-hallucinogenic-drug-a-selective-5-ht2a-receptor-pharmacological-tool-or-none-of-the-above
#18
REVIEW
Giuseppe Di Giovanni, Philippe De Deurwaerdère
The development of 5-HT2A receptor agonists has been considerably marginalized since the demonstration that the tryptaminergic drugs, LSD and psilocybin, or the phenylakylamine drugs, mescaline and DOI, exert their hallucinogenic properties via the stimulation of 5-HT2A receptors. Nonetheless, the ability of drugs to stimulate 5-HT2A receptors is not necessarily associated with psychedelic experience and the hallucinogenic properties are still not understood. Several studies have increased interest in stimulating 5-HT2A receptors in various CNS diseases...
October 4, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28971230/effects-of-2-bromoterguride-a-dopamine-d2-receptor-partial-agonist-on-cognitive-dysfunction-and-social-aversion-in-rats
#19
Emilia Tarland, Robert T Franke, Heidrun Fink, Heinz H Pertz, Jan Brosda
RATIONALE: 2-Bromoterguride, a dopamine D2 receptor partial agonist with antagonist properties at serotonin 5-HT2A receptors and α2C-adrenoceptors, meets the prerequisites of a putative atypical antipsychotic drug (APD). We recently showed that 2-bromoterguride is effective in tests of positive symptoms of schizophrenia in rats without inducing extrapyramidal side effects or metabolic changes. OBJECTIVE: In continuation of our recent work, we now investigated the effect of 2-bromoterguride on apomorphine and phencyclidine (PCP)-induced disruptions of prepulse inhibition (PPI) of the acoustic startle response, a measure of sensory gating...
October 3, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28965828/activation-of-5-ht2a-receptor-disrupts-rat-maternal-behavior
#20
Jun Gao, Ruiyong Wu, Collin Davis, Ming Li
Serotonin 5-HT2A receptor is widely distributed in the central nervous system and plays an important role in sensorimotor function, emotion regulation, motivation, executive control, learning and memory. We investigated its role in rat maternal behavior, a naturalistic behavior encompassing many psychological functions that the 5-HT2A receptor is involved in. We first showed that activation of 5-HT2A receptor by TCB-2 (a highly selective 5-HT2A agonist, 1, 2.5 or 5.0 mg/kg) disrupted maternal behavior dose-dependently, and this effect was reduced by pretreatment with a 5-HT2A receptor antagonist MDL 100907, but exacerbated by pretreatment with a 5-HT2C receptor antagonist SB242084 and a 5-HT2C receptor agonist MK212, indicating that the maternal disruptive effect of 5-HT2A activation is receptor-specific and can be modulated by 5-HT2C receptor bidirectionally...
September 28, 2017: Neuropharmacology
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