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https://www.readbyqxmd.com/read/28624721/assessing-the-role-of-serotonergic-receptors-in-cannabidiol-s-anticonvulsant-efficacy
#1
Madeline C Pelz, Kathleen D Schoolcraft, Chloe Larson, Mitchell G Spring, Hassan H López
Cannabidiol (CBD) is a phytocannabinoid that has demonstrated anticonvulsant efficacy in several animal models of seizure. The current experiment validated CBD's anticonvulsant effect using the acute pentylenetetrazol (PTZ) model. Furthermore, it tested whether CBD reduces seizure activity by interacting with either the serotonergic 5HT1A or 5HT2A receptor. 120 male adolescent Wistar-Kyoto rats were randomly assigned to 8 treatment groups in two consecutive experiments. In both experiments, subjects received either CBD (100mg/kg) or vehicle 60min prior to seizure testing...
June 15, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28594246/a-review-of-vilazodone-exposures-with-focus-on-serotonin-syndrome-effects
#2
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)...
November 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28144708/differential-effects-of-cannabinoid-cb1-inverse-agonists-and-antagonists-on-impulsivity-in-male-sprague-dawley-rats-identification-of-a-possibly-clinically-relevant-vulnerability-involving-the-serotonin-5ht1a-receptor
#3
Peter J McLaughlin, Julia E Jagielo-Miller, Emily S Plyler, Kerry K Schutte, V Kiran Vemuri, Alexandros Makriyannis
RATIONALE: Cannabinoid CB1 inverse agonists hold therapeutic promise as appetite suppressants but have produced suicidal behaviors among a small subpopulation in clinical trials. Anatomical and pharmacological evidence implicate the 5HT1A serotonin receptor in suicide in humans and impulsivity in humans and animals. OBJECTIVE: The objective of the study is to assess whether 5HT1A blockade is necessary for CB1 ligands to produce impulsivity. METHODS: Sprague Dawley rats were administered the CB1 inverse agonist AM 251, the CB1 antagonist AM 6527, or the peripherally restricted antagonist AM 6545, with or without pretreatment with the 5HT1A antagonist WAY 100,635 (WAY) on the paced fixed consecutive number (FCN) task, which measures choice to terminate a chain of responses prematurely...
March 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28139680/ethanol-dependence-abolishes-monoamine-and-girk-kir3-channel-inhibition-of-orbitofrontal-cortex-excitability
#4
Sudarat Nimitvilai, Marcelo F Lopez, Patrick J Mulholland, John J Woodward
Alcohol abuse disorders are associated with dysfunction of frontal cortical areas including the orbitofrontal cortex (OFC). The OFC is extensively innervated by monoamines, and drugs that target monoamine receptors have been used to treat a number of neuropsychiatric diseases, including alcoholism. However, little is known regarding how monoamines affect OFC neuron excitability or whether this modulation is altered by chronic exposure to ethanol. In this study, we examined the effect of dopamine, norepinephrine, and serotonin on lOFC neuronal excitability in naive mice and in those exposed to chronic intermittent ethanol (CIE) treatment...
August 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28114832/exhaustive-comfa-and-comsia-analyses-around-different-chemical-entities-a-ligand-based-study-exploring-the-affinity-and-selectivity-profiles-of-5-ht1a-ligands
#5
COMPARATIVE STUDY
Sara Guariento, Silvia Franchini, Michele Tonelli, Paola Fossa, Claudia Sorbi, Elena Cichero, Livio Brasili
The 5-hydroxytryptamine (5-HT1A) receptors represent an attractive target in drug discovery. In particular, 5-HT1A agonists and partial agonists are deeply investigated for their potential role in the treatment of anxiety, depression, ischaemic brain disorder and more recently, of pain. On the other hand, 5-HT1A antagonists have been revealed promising compounds in cognition disorders and, lately, in cancer. Thus, the discovery of 5HT1A ligands is nowadays an appealing research activity in medicinal chemistry...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28012414/the-effect-of-sertraline-and-8-oh-dpat-on-the-ptz_induced-seizure-threshold-role-of-the-nitrergic-system
#6
Azhdar Heydari, Shima Davoudi
PURPOSE: Serotonin is a key regulatory neurotransmitter in the CNS which plays an important role in seizure through different receptors, especially the 5HT1A subtype. The role of sertraline through the 5HT1A receptor and nitric oxide interaction on the PTZ-induced seizure threshold was investigated in this study. METHOD: In this study, 70 white male mice were randomly divided into 10 groups including intact control, sham-control and eight experimental groups which received sertraline, 8-OH-DPAT, WAY100635, WAY100635+sertraline, WAY100635+8-OH-DPAT, L-NAME, L-NAME+sertraline and L-NAME+8-OH-DPAT...
February 2017: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/27859267/human-motoneurone-excitability-is-depressed-by-activation-of-serotonin-1a-receptors-with-buspirone
#7
Jessica M D'Amico, Annie A Butler, Martin E Héroux, Florence Cotel, Jean-François M Perrier, Jane E Butler, Simon C Gandevia, Janet L Taylor
KEY POINTS: In the adult turtle spinal cord, action potential generation in motoneurones is inhibited by spillover of serotonin to extrasynaptic serotonin 1A (5-HT1A ) receptors at the axon initial segment. We explored whether ingestion of the 5-HT1A receptor partial agonist, buspirone, decreases motoneurone excitability in humans. Following ingestion of buspirone, two tests of motoneurone excitability showed decreases. F-wave areas and persistence in an intrinsic muscle of the hand were reduced, as was the area of cervicomedullary motor evoked potentials in biceps brachii...
March 1, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/27824065/optogenetic-activation-of-serotonergic-terminals-facilitates-gabaergic-inhibitory-input-to-orexin-hypocretin-neurons
#8
Srikanta Chowdhury, Akihiro Yamanaka
Orexin/hypocretin neurons play a crucial role in the regulation of sleep/wakefulness, primarily in the maintenance of wakefulness. These neurons innervate wide areas of the brain and receive diverse synaptic inputs including those from serotonergic (5-HT) neurons in the raphe nucleus. Previously we showed that pharmacological application of 5-HT directly inhibited orexin neurons via 5-HT1A receptors. However, it was still unclear how 5-HT neurons regulated orexin neurons since 5-HT neurons contain not only 5-HT but also other neurotransmitters...
November 8, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27788337/adjunctive-brexpiprazole-for-the-treatment-of-major-depressive-disorder
#9
John L Beyer, Richard H Weisler
The lifetime prevalence of major depressive episodes in the United States is nearly 17%. Clinical trials and clinical effectiveness studies have demonstrated that many patients will fail to achieve remission using traditional monotherapy, contributing to significant morbidity and suffering. Because of this, augmentation strategies have been proposed to improve both treatment response and remission. Areas covered: Brexpiprazole is a second generation antipsychotic (SGA) approved by the US FDA in 2015 as an add-on treatment to an antidepressant medication for the treatment of adults with MDD, based on the results of two large-scale, randomized, placebo-controlled trials...
December 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27453059/the-cb1-antagonist-sr141716a-is-protective-in-permanent-photothrombotic-cerebral-ischemia
#10
Zachary Wilmer Reichenbach, Hongbo Li, Sara Jane Ward, Ronald F Tuma
Modulation of the endocannabinoid system has been shown to have a significant impact on outcomes in animal models of stroke. We have previously reported a protective effect of the CB1 antagonist, SR141716A, in a transient reperfusion mouse model of cerebral ischemia. This protective effect was in part mediated by activation of the 5HT1A receptor. Here we have examined its effect in a mouse model of permanent ischemia induced by photoinjury. The CB1 antagonist was found to be protective in this model. As was the case following transient ischemia reperfusion, SR141716A (5mg/kg) resulted in smaller infarct fractions and stroke volumes when utilized both as a pretreatment and as a post-treatment...
September 6, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27396597/the-novel-antipsychotic-cariprazine-rgh-188-state-of-the-art-in-the-treatment-of-psychiatric-disorders
#11
Domenico De Berardis, Laura Orsolini, Felice Iasevoli, Emiliano Prinzivalli, Andrea de Bartolomeis, Nicola Serroni, Monica Mazza, Alessandro Valchera, Michele Fornaro, Roberta Vecchiotti, Alessandro Carano, Gianna Sepede, Federica Vellante, Ilaria Matarazzo, Maurizio Pompili, Giampaolo Perna, Chiara Conti, Cristina Segura-García, Giovanni Martinotti, Massimo Di Giannantonio
Cariprazine (RGH-188) is a novel antipsychotic drug that exerts partial agonism of dopamine D2/D3 receptors with preferential binding to D3 receptor, antagonism of 5HT2B receptors and partial agonism of 5HT1A. Currently, cariprazine is in late-stage clinical development (phase III clinical trials) in patients with schizophrenia (S) and in patients with bipolar disorder (BD), as well as an adjunctive treatment in patients with Major Depressive Disorder (MDD) and drug-resistant MDD. Cariprazine has completed phase III trials for the acute treatment of schizophrenia and bipolar mania, phase II trials for the bipolar depression and MDD whilst it is undergoing phase III trials as an adjunct to antidepressants...
2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27274197/spotlight-on-brexpiprazole-and-its-potential-in-the-treatment-of-schizophrenia-and-as-adjunctive-therapy-for-the-treatment-of-major-depression
#12
REVIEW
Dawn Bruijnzeel, Rajiv Tandon
Antipsychotic agents, utilized for the treatment of a range of psychiatric disorders, differ substantially in terms of their pharmacology and adverse effect profiles. Incomplete and variable efficacy, differences in safety-tolerability, and highly heterogeneous response across individuals prompt development of new agents. Brexpiprazole is one of the two most recently introduced antipsychotic agents approved for the treatment of schizophrenia and as an adjunct for treatment of major depressive disorder. Its pharmacology, clinical trial data, and efficacy and side effects in comparison with other antipsychotic agents are discussed...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27235743/prenatal-stress-alters-diazepam-withdrawal-syndrome-and-5ht1a-receptor-expression-in-the-raphe-nuclei-of-adult-rats
#13
S Lakehayli, N Said, M El Khachibi, M El Ouahli, S Nadifi, F Hakkou, A Tazi
Early-life events have long-term effects on brain structures and cause behavioral alterations that persist into adulthood. The present experiments were designed to investigate the effects of prenatal stress on diazepam-induced withdrawal syndrome and serotonin-1A (5HT1A) receptor expression in the raphe nuclei of adult offspring. The results of the present study reveal that maternal exposure to chronic footshock stress increased the anxiety-like behavior in the prenatally stressed (PS) animals withdrawn from chronic diazepam (2...
August 25, 2016: Neuroscience
https://www.readbyqxmd.com/read/27150816/distinct-effect-of-5-ht1a-and-5-ht2a-receptors-in-the-medial-nucleus-of-the-amygdala-on-tonic-immobility-behavior
#14
Bruna Balbino de Paula, Christie Ramos Andrade Leite-Panissi
The tonic immobility (TI) response is an innate fear behavior associated with intensely dangerous situations, exhibited by many species of invertebrate and vertebrate animals. In humans, it is possible that TI predicts the severity of posttraumatic stress disorder symptoms. This behavioral response is initiated and sustained by the stimulation of various groups of neurons distributed in the telencephalon, diencephalon and brainstem. Previous research has found the highest Fos-IR in the posteroventral part of the medial nucleus of the amygdala (MEA) during TI behavior; however, the neurotransmission of this amygdaloid region involved in the modulation of this innate fear behavior still needs to be clarified...
July 15, 2016: Brain Research
https://www.readbyqxmd.com/read/27110092/repurposing-an-orally-available-drug-for-the-treatment-of-geographic-atrophy
#15
Chulbul M Ahmed, Manas R Biswal, Hong Li, Pingyang Han, Cristhian J Ildefonso, Alfred S Lewin
PURPOSE: Chronic oxidative stress and subacute inflammation have been implicated as causes of age-related macular degeneration (AMD). In this study, we tested whether an orally available 5-OH-tryptamine (5HT) 1a receptor agonist, xaliproden, could protect against retinal pigment epithelium (RPE) cell damage in culture and in a mouse model of geographic atrophy. METHODS: Paraquat was used to create mitochondrial oxidative stress in ARPE-19 cells, and tumor necrosis factor-α (TNF-α) was used to stimulate the production of inflammatory cytokines in these cells...
2016: Molecular Vision
https://www.readbyqxmd.com/read/27036122/lurasidone-an-antipsychotic-with-antidepressant-effects-in-bipolar-depression
#16
Nicholas A Keks, Judy Hope, David Castle
OBJECTIVE: Lurasidone is a new serotonin-dopamine antagonist atypical antipsychotic which also appears to be effective in bipolar depression. This paper will briefly review the evidence concerning lurasidone. CONCLUSIONS: Lurasidone is an antagonist at dopamine D2, serotonin 5-HT2 and 5-HT7, and partial agonist at 5HT1a receptors; it has no anticholinergic or antihistaminic activity. Rapidly absorbed, it has a half-life of 18 ± 7 hours, will reach steady state in five days and is taken at night with food (absorption is halved on an empty stomach)...
June 2016: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
https://www.readbyqxmd.com/read/26871939/antidyskinetic-effect-of-a2a-and-5ht1a-1b-receptor-ligands-in-two-animal-models-of-parkinson-s-disease
#17
Annalisa Pinna, Wai Kin D Ko, Giulia Costa, Elisabetta Tronci, Camino Fidalgo, Nicola Simola, Qin Li, Mojgan Aghazadeh Tabrizi, Erwan Bezard, Manolo Carta, Micaela Morelli
BACKGROUND: The serotonin 5-HT1A/1B receptor agonist eltoprazine suppressed dyskinetic-like behavior in animal models of Parkinson's disease (PD) but simultaneously reduced levodopa (l-dopa)-induced motility. Moreover, adenosine A2A receptor antagonists, such as preladenant, significantly increased l-dopa efficacy in PD without exacerbating dyskinetic-like behavior. OBJECTIVES: We evaluated whether a combination of eltoprazine and preladenant may prevent or suppress l-dopa-induced dyskinesia, without impairing l-dopa's efficacy in relieving motor signs, in 2 PD models: unilateral 6-hydroxydopamine-lesioned rats and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys...
April 2016: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/26866771/rs6295-c-allele-protects-against-depressive-mood-in-elderly-endurance-athletes
#18
Helmuth Haslacher, Matthias Michlmayr, Delgerdalai Batmyagmar, Thomas Perkmann, Elisabeth Ponocny-Seliger, Vanessa Scheichenberger, Thomas M Scherzer, Sonja Nistler, Alexander Pilger, Peter Dal-Bianco, Johann Lehrner, Lukas Pezawas, Oswald F Wagner, Robert Winker
A single nucleotide variant within the promoter of the 5-hydroxytryptamine1A (5HT1A) receptor, rs6295, is part of a binding site for the transcription factor. We aimed to ascertain whether the rs6295 mediates the effect of exercise on depressive mood in elderly endurance athletes. We prospectively enrolled 55 elderly athletes (marathon runners/bicyclists) and 58 controls. In a controlled, univariate model, an interaction between the [C]-allele and physical activity indicated that only among athletes, the variant resulting in an imperfect NUDR binding site was associated with a lower depression score...
December 2015: Journal of Sport & Exercise Psychology
https://www.readbyqxmd.com/read/26860509/dual-alpha2c-5ht1a-receptor-agonist-allyphenyline-induces-gastroprotection-and-inhibits-fundic-and-colonic-contractility
#19
Zoltán S Zádori, Ágnes Fehér, Viktória E Tóth, Mahmoud Al-Khrasani, László Köles, Szabina Sipos, Fabio Del Bello, Maria Pigini, Klára Gyires
BACKGROUND: Allyphenyline, a novel α2-adrenoceptor (AR) ligand, has been shown to selectively activate α2C-adrenoceptors (AR) and 5HT1A receptors, but also to behave as a neutral antagonist of α2A-ARs. We exploited this unique pharmacological profile to analyze the role of α2C-ARs and 5HT1A receptors in the regulation of gastric mucosal integrity and gastrointestinal motility. METHODS: Gastric injury was induced by acidified ethanol in Wistar rats. Mucosal catalase and superoxide dismutase levels were measured by assay kits...
June 2016: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/26840837/blockade-of-dorsolateral-pontine-5ht1a-receptors-destabilizes-the-respiratory-rhythm-in-c57bl6-j-wild-type-mice
#20
R R Dhingra, M Dutschmann, T E Dick
The neurotransmitter serotonin (5HT) acting via 5HT1a receptors (5HT1aR) is a potent determinant of respiratory rhythm variability. Here, we address the 5HT1aR-dependent control of respiratory rhythm variability in C57BL6/J mice. Using the in situ perfused preparation, we compared the effects of systemic versus focal blockade of 5HT1aRs. Blocking 5HT1aRs in the Kölliker-Fuse nucleus (KFn) increased the occurrence of spontaneous apneas and accounted for the systemic effects of 5HT1aR antagonists. Further, 5HT1aRs of the KFn stabilized the respiratory rhythm's response to arterial chemoreflex perturbations; reducing the recovering time, e...
June 2016: Respiratory Physiology & Neurobiology
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