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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
Domenico De Berardis
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...
June 30, 2016: Current Pharmaceutical Design
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
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
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
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
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
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
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
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
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
Carla García-Barba, Laura Medina-Ceja
Fast ripples (FR, 250-600Hz) are field potentials that occur only in those areas capable of generating seizures, such as the hippocampus, and modulation of FR by serotonin has been reported. Therefore, we hypothesized that the receptor antagonists 5HT1A and 5HT2A, B, C will increase FR in rats treated with kainic acid (KA, 0.8μg/0.5μl). For this purpose, the intracranial EEG recordings of the hippocampus from animals treated with KA and the serotonin antagonists WAY100135 and ritanserin (dose 0.2mg/Kg, i...
March 2016: Brain Research Bulletin
Diane C Chugani, Harry T Chugani, Max Wiznitzer, Sumit Parikh, Patricia A Evans, Robin L Hansen, Ruth Nass, James J Janisse, Pamela Dixon-Thomas, Michael Behen, Robert Rothermel, Jacqueline S Parker, Ajay Kumar, Otto Muzik, David J Edwards, Deborah Hirtz
OBJECTIVES: To determine safety and efficacy of the 5HT1A serotonin partial agonist buspirone on core autism and associated features in children with autism spectrum disorder (ASD). STUDY DESIGN: Children 2-6 years of age with ASD (N = 166) were randomized to receive placebo or 2.5 or 5.0 mg of buspirone twice daily. The primary objective was to evaluate the effects of 24 weeks of buspirone on the Autism Diagnostic Observation Schedule (ADOS) Composite Total Score...
March 2016: Journal of Pediatrics
Helene M Savignac, Yvonne Couch, Michael Stratford, David M Bannerman, George Tzortzis, Daniel C Anthony, Philip W J Burnet
The manipulation of the enteric microbiota with specific prebiotics and probiotics, has been shown to reduce the host's inflammatory response, alter brain chemistry, and modulate anxiety behaviour in both rodents and humans. However, the neuro-immune and behavioural effects of prebiotics on sickness behaviour have not been explored. Here, adult male CD1 mice were fed with a specific mix of non-digestible galacto-oligosaccharides (Bimuno®, BGOS) for 3 weeks, before receiving a single injection of lipopolysaccharide (LPS), which induces sickness behaviour and anxiety...
February 2016: Brain, Behavior, and Immunity
Manas R Biswal, Chulbul M Ahmed, Cristhian J Ildefonso, Pingyang Han, Hong Li, Hiral Jivanji, Haoyu Mao, Alfred S Lewin
Chronic oxidative stress contributes to age related diseases including age related macular degeneration (AMD). Earlier work showed that the 5-hydroxy-tryptamine 1a (5HT1a) receptor agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) protects retinal pigment epithelium (RPE) cells from hydrogen peroxide treatment and mouse retinas from oxidative insults including light injury. In our current experiments, RPE derived cells subjected to mitochondrial oxidative stress were protected from cell death by the up-regulation of anti-oxidant enzymes and of the metal ion chaperone metallothionein...
November 2015: Experimental Eye Research
Serena Deiana, Akihito Watanabe, Yuki Yamasaki, Naoki Amada, Tetsuro Kikuchi, Colin Stott, Gernot Riedel
Deficiencies in social activities are hallmarks of numerous brain disorders. With respect to schizophrenia, social withdrawal belongs to the category of negative symptoms and is associated with deficits in the cognitive domain. Here, we used the N-methyl-D-aspartate receptor antagonist dizocilpine (MK-801) for induction of social withdrawal in rats and assessed the efficacy of several atypical antipsychotics with different pharmacological profiles as putative treatment. In addition, we reasoned that the marijuana constituent cannabidiol (CBD) may provide benefit or could be proposed as an adjunct treatment in combination with antipsychotics...
December 2015: Behavioural Pharmacology
María Teresa Rivera-García, Carolina López-Rubalcava, Silvia L Cruz
RATIONALE: Toluene is a misused inhalant with hallucinogenic properties and complex effects. Toluene blocks N-methyl-D-aspartate (NMDA) receptors, releases dopamine (DA), and modifies several neurotransmitter levels; nonetheless, the mechanism by which it produces hallucinations is not well characterized. OBJECTIVES: This study aims (a) to study toluene's effects on the 5-HT2A-mediated head-twitch response (HTR), dopamine (DA), and serotonin (5-HT) tissue levels in discrete brain regions; (b) to compare the actions of toluene, ketamine, and 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI) on HTR; and (c) to study the pharmacological blockade of toluene's and ketamine's effects by selective drugs...
October 2015: Psychopharmacology
Carl D Smith, Christopher C Piasecki, Marcus Weera, Joshua Olszewicz, Joseph S Lonstein
Reports an error in "Noradrenergic alpha-2 receptor modulators in the ventral bed nucleus of the stria terminalis: Effects on anxiety behavior in postpartum and virgin female rats" by Carl D. Smith, Christopher C. Piasecki, Marcus Weera, Joshua Olszewicz and Joseph S. Lonstein (Behavioral Neuroscience, 2013[Aug], Vol 127[4], 582-597). Table 2 should have used the ratio of 5HIAA/serotonin - rather than the inverse - as the indicator of serotonin turnover. Using the correct ratio, differences in serotonin turnover between the postpartum and virgin females are: BSTv - 1...
August 2015: Behavioral Neuroscience
Karolina Pytka, Maria Walczak, Agnieszka Kij, Anna Rapacz, Agata Siwek, Grzegorz Kazek, Adrian Olczyk, Adam Gałuszka, Anna Waszkielewicz, Henryk Marona, Jacek Sapa, Barbara Filipek
Xanthone derivatives have been shown to posses many biological properties. Some of them act within the central nervous system and show neuroprotective or antidepressant-like properties. Taking this into account we investigated antidepressant-like activity in mice and the possible mechanism of action of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one (HBK-11) - a new xanthone derivative. We demonstrated that HBK-11 produced antidepressant-like effects in the forced swim test and tail suspension test, comparable to that of venlafaxine...
October 5, 2015: European Journal of Pharmacology
Richard R Neubig
Guanine nucleotide-binding proteins of the inhibitory (Gi/o) class play critical physiological roles and the receptors that activate them are important therapeutic targets (e.g., mu opioid, serotonin 5HT1a, etc.). Gi/o proteins are negatively regulated by regulator of G protein signaling (RGS) proteins. The redundant actions of the 20 different RGS family members have made it difficult to establish their overall physiological role. A unique G protein mutation (G184S in Gαi/o) prevents RGS binding to the Gα subunit and blocks all RGS action at that particular Gα subunit...
2015: Progress in Molecular Biology and Translational Science
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