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https://www.readbyqxmd.com/read/28647281/serotonergic-modulation-of-nicotine-induced-kinetic-tremor-in-mice
#1
Naofumi Kunisawa, Higor A Iha, Yuji Nomura, Misaki Onishi, Nami Matsubara, Saki Shimizu, Yukihiro Ohno
We previously demonstrated that nicotine elicited kinetic tremor by elevating the neural activity of the inferior olive via α7 nicotinic acetylcholine (nACh) receptors. Since α7 nACh receptors reportedly facilitate synaptic monoamine release, we explored the role of 5-HT receptors in induction and/or modulation of nicotine tremor. Treatment of mice with nicotine induced kinetic tremor that normally appeared during movement. The 5-HT1A agonist, 8-hydroxydipropylaminotetraline (8-OH-DPAT), significantly enhanced nicotine-induced tremor and the action of 8-OH-DPAT was antagonized by WAY-100135 (5-HT1A antagonist)...
June 9, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28646910/the-role-of-5-ht-receptors-in-depression
#2
REVIEW
Christine N Yohn, Mark M Gergues, Benjamin Adam Samuels
Depression is a polygenic and highly complex psychiatric disorder that remains a major burden on society. Antidepressants, such as selective serotonin reuptake inhibitors (SSRIs), are some of the most commonly prescribed drugs worldwide. In this review, we will discuss the evidence that links serotonin and serotonin receptors to the etiology of depression and the mechanisms underlying response to antidepressant treatment. We will then revisit the role of serotonin in three distinct hypotheses that have been proposed over the last several decades to explain the pathophysiology of depression: the monoamine, neurotrophic, and neurogenic hypotheses...
June 24, 2017: Molecular Brain
https://www.readbyqxmd.com/read/28646714/synthetic-cathinones-and-stereochemistry-s-enantiomer-of-mephedrone-reduces-anxiety-and-depressant-like-effects-in-cocaine-or-mdpv-abstinent-rats
#3
Helene L Philogene-Khalid, Callum Hicks, Allen B Reitz, Lee-Yuan Liu-Chen, Scott M Rawls
BACKGROUND AND PURPOSE: The neuropharmacological profile of the synthetic cathinone mephedrone (MEPH) is influenced by stereochemistry. Both MEPH enantiomers are monoamine transporter substrates, but R-MEPH is primarily responsible for rewarding effects of MEPH as it produces greater locomotor activation and intracranial self-stimulation than S-MEPH. S-MEPH is a 50-fold more potent 5-HT releaser than R-MEPH and does not place preference in rats. MEPH is also structurally similar to the cathinone derivative bupropion, an antidepressant and smoking cessation medication, suggesting MEPH has therapeutic and addictive properties...
June 13, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28645783/maerua-angolensis-stem-bark-extract-reverses-anxiety-and-related-behaviours-in-zebrafish-involvement-of-gabaergic-and-5-ht-systems
#4
Charles Kwaku Benneh, Robert Peter Biney, Priscilla Kolibea Mante, Augustine Tandoh, Donatus Wewura Adongo, Eric Woode
ETHNOPHARMACOLOGICAL RELEVANCE: Maerua angolensis DC (Capparaceae) has been employed in the management of several central nervous system (CNS) disorders including anxiety. This study evaluated the anxiolytic effects of the petroleum ether/ethyl acetate fraction stem bark extract and its possible mechanism(s) using zebrafish anxiety models. METHODS: Adult zebrafish, tested in the novel tank and light dark tests, have shown by previous authors to be sensitive to the anxiolytic effects of known anxiolytic drugs...
June 20, 2017: Journal of Ethnopharmacology
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
#5
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/28641527/design-synthesis-and-biological-evaluation-of-c-2-substituted-3h-thieno-2-3-d-pyrimidin-4-one-derivatives-as-novel-fgfr1-inhibitors
#6
Ping Guo, Faqing Ye, Zixin Xie, Huan Zhang, Zaikui Zhang, Chao Han, Donghua Cheng, Dan Lin, Yuan Zhang, Xuebao Wang, Xin Guo
BACKGROUND: Thienopyrimidinone is a newly designed, selective fibroblast growth factor receptor 1 (FGFR1) inhibitor with an excellent anticancer effect. OBJECTIVE: The goal of the present study was to design and synthesize better FGFR1 inhibitors through modifications of the lead compound thienopyrimidinone. METHODS: In the present study, a series of C-2 substituted derivatives of thienopyrimidinone, namely L1-L16, were synthesized, and their inhibitory effects on FGFR1 were evaluated...
June 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28637246/effect-of-psilocybin-on-empathy-and-moral-decision-making
#7
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
https://www.readbyqxmd.com/read/28636360/proneurogenic-effects-of-trazodone-in-murine-and-human-neural-progenitors
#8
Valeria Bortolotto, Francesca Mancini, Giorgina Mangano, Rita Salem, Er Xia, Erika Del Grosso, Michele Bianchi, Pier Luigi Canonico, Lorenzo Polenzani, Mariagrazia Grilli
Several antidepressants increase adult hippocampal Neurogenesis (ahNG) in rodents, primates and, potentially, in humans. This effect may at least partially account for their therapeutic activity. The availability of antidepressants whose mechanism of action involves different neurotransmitter receptors represents an opportunity for increasing our knowledge on their distinctive peculiarities and for dissecting the contribution of receptor subtypes in ahNG modulation. The aim of this study was to evaluate, in vitro, the effects of the antidepressant trazodone (TZD) on ahNG by using primary cultures of adult hippocampal Neural Progenitor Cells (ahNPC) and human iPSC-derived NPC...
June 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28628851/spinal-5-ht4-and-5-ht6-receptors-contribute-to-the-maintenance-of-neuropathic-pain-in-rats
#9
Jorge Baruch Pineda-Farias, Paulino Barragán-Iglesias, Alann Valdivieso-Sánchez, Juan Rodríguez-Silverio, Francisco Javier Flores-Murrieta, Vinicio Granados-Soto, Héctor Isaac Rocha-González
BACKGROUND: Nerve injury promotes release of 5-HT at the spinal cord. Once released, 5-HT may produce antinociceptive or pronociceptive effects depending of the nature of 5-HT receptors. The purpose of this study was to investigate the participation of spinal 5-HT4 and 5-HT6 receptors in the maintenance of neuropathic pain in rats. METHODS: Tactile allodynia was measured using von Frey hairs in male Wistar rats subjected to L5-L6 spinal nerve injury. Selective 5-HT4 (GR-113808, 0...
April 4, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28628756/atypical-sympathomimetic-drug-lerimazoline-mediates-contractile-effects-in-rat-aorta-predominantly-by-5-ht2a-receptors
#10
Eldina Rizvić, Goran Janković, Slađana Kostić-Rajačić, Miroslav M Savić
Lerimazoline is a sympathomimetic drug that belongs to the imidazoline class of compounds, and is used as a nasal decongestant. Studies on lerimazoline are rare, and its pharmacological profile is not completely understood. Here, we analyzed the affinity of lerimazoline for dopamine receptor D2, serotonin 5-HT1A and 5-HT2A receptors and α1-adrenoceptor, and investigated lerimazoline contractile effects in isolated rat thoracic aorta. We also determined the effect of several antagonists on the contractile response to lerimazoline, including prazosin (α1-adrenoceptor antagonist), RX 821002 and rauwolscine (α2-adrenoceptor antagonists), JP 1302 (α2C-adrenoceptor antagonist), methiothepin (non-selective 5-HT receptor antagonist), SB 224289 (5-HT1B receptor antagonist), BRL 15572 (5-HT1D receptor antagonist), and ketanserin (5-HT2A receptor antagonist)...
June 19, 2017: Bosnian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28626072/5-ht-causes-splanchnic-venodilation
#11
Bridget Mahon Seitz, Hakan Orer, Teresa Krieger-Burke, Emma S Darios, Janice M Thompson, Gregory D Fink, Stephanie W Watts
Serotonin (5-HT, 5-hydroxytrypamine) causes relaxation of the isolated superior mesenteric vein (SMV), a splanchnic blood vessel, through activation of the 5-HT7 receptor. As part of studies designed to identify the mechanism(s) through which chronic (>24 hours) infusion of 5-HT lowers blood pressure, we test the hypothesis that 5-HT causes an in vitro and in vivo splanchnic venodilation that is 5-HT7 receptor-dependent. In tissue baths for measurement of isometric contraction, the portal vein (PV) and abdominal inferior vena cava (Ab IVC) relaxed to 5-HT and the 5-HT1/7 receptor agonist 5-carboxamidotryptamine (5-CT); relaxation was abolished by the 5-HT7 receptor antagonist SB269970...
June 16, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/28623179/modulation-of-tgf-%C3%AE-smad-and-erk-signaling-pathways-mediates-the-anti-fibrotic-effect-of-mirtazapine-in-mice
#12
Dalia M El-Tanbouly, Walaa Wadie, Rabab H Sayed
Serotonin (5-HT) has been implicated as a key driver of liver fibrosis, acting via 5-HT2 receptor activation in the hepatic stellate cells. The current study was conducted to investigate the effects of mirtazapine, a 5-HT2A antagonist, in a mouse model of liver fibrosis. Mice received thioacetamide (TAA, 150mg/kg/biweekly, ip) for nine successive weeks for induction of liver fibrosis. Administration of mirtazapine significantly improved the plasma aminotransferases, reduced hepatic 5-HT concentration and ameliorated TAA-induced liver fibrosis, as demonstrated by reduced portal blood pressure, liver procollagen I content and α alpha smooth muscle actin expression...
June 13, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28611585/role-of-n-arachidonoyl-serotonin-aa-5-ht-in-sleep-wake-cycle-architecture-sleep-homeostasis-and-neurotransmitters-regulation
#13
Eric Murillo-Rodríguez, Vincenzo Di Marzo, Sergio Machado, Nuno B Rocha, André B Veras, Geraldo A M Neto, Henning Budde, Oscar Arias-Carrión, Gloria Arankowsky-Sandoval
The endocannabinoid system comprises several molecular entities such as endogenous ligands [anandamide (AEA) and 2-arachidonoylglycerol (2-AG)], receptors (CB1 and CB2), enzymes such as [fatty acid amide hydrolase (FAHH) and monoacylglycerol lipase (MAGL)], as well as the anandamide membrane transporter. Although the role of this complex neurobiological system in the sleep-wake cycle modulation has been studied, the contribution of the blocker of FAAH/transient receptor potential cation channel subfamily V member 1 (TRPV1), N-arachidonoyl-serotonin (AA-5-HT) in sleep has not been investigated...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28607170/oxytocin-and-serotonin-brain-mechanisms-in-the-non-human-primate
#14
Lefevre Arthur, Richard Nathalie, Jazayeri Mina, Beuriat Pierre-Aurélien, Fieux Sylvain, Zimmer Luc, Duhamel Jean-René, Sirigu Angela
Oxytocin is increasingly studied for its therapeutic potential in psychiatric disorders which are associated with the deregulation of several neurotransmission systems. Studies in rodents demonstrated that the interaction between oxytocin (OT) and serotonin (5-HT) is critical for several aspects of social behavior. Using PET-scan in humans we have recently found that 5-HT 1A receptor (5-HT1AR) function is modified after intra-nasal oxytocin intake. However, the underlying mechanism between OT and 5-HT remains unclear...
June 12, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28606822/genistein-a-dietary-soy-isoflavone-exerts-antidepressant-like-effects-in-mice-involvement-of-serotonergic-system
#15
Pei Hu, Li Ma, Yan-Gui Wang, Feng Ye, Chuang Wang, Wen-Hua Zhou, Xin Zhao
Genistein, a principal isoflavone property of soybeans, possesses multiple pharmacological activities such as neuroprotection. Recently, it was reported that genistein exerted antidepressant-like effects in animal models, but the mechanism of action remains ambiguous. The purpose of this study was to investigate the antidepressant-like effect of genistein in mice and explore the underlying mechanism(s), using two mouse models of depression, i.e. forced swim test (FST) and tail suspension test (TST). Chronic, but not acute (single dose), genistein treatment (5, 15 or 45 mg/kg, p...
June 9, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28606116/characterization-of-serotonin-induced-inhibition-of-excitatory-synaptic-transmission-in-the-anterior-cingulate-cortex
#16
Zhen Tian, Manabu Yamanaka, Matteo Bernabucci, Ming-Gao Zhao, Min Zhuo
Excitatory synaptic transmission in central synapses is modulated by serotonin (5-HT). The anterior cingulate cortex (ACC) is an important cortical region for pain perception and emotion. ACC neurons receive innervation of projecting serotonergic nerve terminals from raphe nuclei, but the possible effect of 5-HT on excitatory transmission in the ACC has not been investigated. In the present study, we investigated the role of 5-HT on glutamate neurotransmission in the ACC slices of adult mice. Bath application of 5-HT produced dose-dependent inhibition of evoked excitatory postsynaptic currents (eEPSCs)...
June 12, 2017: Molecular Brain
https://www.readbyqxmd.com/read/28598863/characterization-of-the-discriminative-stimulus-effects-of-3-4-methylenedioxypyrovalerone-in-male-sprague-dawley-rats
#17
Michael D Berquist, Lisa E Baker
Recreational use of 3,4-methylenedioxypyrovalerone (MDPV) in the early 2000s prompted numerous scientific investigations of its behavioral and neurochemical effects. The purpose of this study was to further characterize the interoceptive stimulus effects of MDPV using a validated in-vivo drug-detection assay. Male Sprague-Dawley rats were trained to discriminate 0.3 mg/kg MDPV from saline under a fixed ratio 20 (FR 20) schedule of food reinforcement. After stimulus control was established with MDPV (∼35 training sessions), substitution tests were commenced with drugs from several chemical classes, including drugs with predominantly dopaminergic actions [MDPV, D-amphetamine, (+)-methamphetamine, (-)-cocaine], drugs with predominantly serotonergic actions [(+)-lysergic acid diethylamide, (+)-fenfluramine], and drugs with both serotonergic and dopaminergic actions (3,4-methylenedioxymethamphetamine, 4-methylmethcathinone)...
June 8, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28597539/developmental-effects-of-antipsychotic-drugs-on-serotonin-receptor-subtypes
#18
Yong Kee Choi, Matthew P Gardner, Frank I Tarazi
Antipsychotic medications are increasingly prescribed to pediatric and adolescent patients with psychotic diseases in spite of limited knowledge on the long-term effects of dissimilar antipsychotic drugs on developing brain. In this study, we quantified the levels of two major serotonin 5-HT1A , and 5-HT2A receptors in brain regions of developing rats after 3 weeks of treatment with typical (fluphenazine) and atypical (clozapine and olanzapine) antipsychotics, and compared to similarly treated adult rats treated with olanzapine, risperidone and quetiapine examined in previous studies...
June 8, 2017: Synapse
https://www.readbyqxmd.com/read/28585544/serotonin-modulates-a-depression-like-state-in-drosophila-responsive-to-lithium-treatment
#19
Ariane-Saskia Ries, Tim Hermanns, Burkhard Poeck, Roland Strauss
Major depressive disorder (MDD) affects millions of patients; however, the pathophysiology is poorly understood. Rodent models have been developed using chronic mild stress or unavoidable punishment (learned helplessness) to induce features of depression, like general inactivity and anhedonia. Here we report a three-day vibration-stress protocol for Drosophila that reduces voluntary behavioural activity. As in many MDD patients, lithium-chloride treatment can suppress this depression-like state in flies. The behavioural changes correlate with reduced serotonin (5-HT) release at the mushroom body (MB) and can be relieved by feeding the antidepressant 5-hydroxy-L-tryptophan or sucrose, which results in elevated 5-HT levels in the brain...
June 6, 2017: Nature Communications
https://www.readbyqxmd.com/read/28583576/administration-of-huperzine-a-exerts-antidepressant-like-activity-in-a-rat-model-of-post-stroke-depression
#20
Yuan Du, Haiyue Liang, Leiming Zhang, Fenghua Fu
Post-stroke depression (PSD) is the most common mood disorder following a stroke, and is also the main factor limiting recovery and rehabilitation in stroke patients. The present study was aimed to investigate whether Huperzine A (HupA) has antidepressant-like activity in a rat model of PSD, which was developed by middle cerebral artery occlusion followed by an 18-day chronic unpredictable mild stress in conjunction with isolation rearing. The sucrose preference and forced swim tests were used to assess depression-like behavior...
July 2017: Pharmacology, Biochemistry, and Behavior
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